h3 antagonist binding: Topics by WorldWideScience.org

The (--)(/sup 3/H)dihydroalprenolol binding to rat adipocyte membranes: an explanation of curvilinear Scatchard plots and implications for quantitation of beta-adrenergic sites

A study was made of the kinetics of L-(/sup 3/H)quinuclidinyl benzilate binding with membrane-bound muscarine cholinoreceptors from the rat brain. Determination was made of the rate constants of this process, and constants as a function of ligand concentration was investigated, indicating that there is a complex mechanism of interaction of antagonists with muscarine receptor. With up to 3.5 nM concentrations of L-(/sup 3/H)quinuclidinyl benzilate, the binding reaction occurs in two stages: rapid equilibrated binding is followed by a slow process of conformational isomerization of the receptor-ligand complex. At higher ligand concentrations, there is additional drastic increase in constant of rate of ligand binding a new plateau is reached. Such dependence of rate constant on ligand concentration is indicative of the cooperative nature of interaction between ...

1985-01-01

3

Synthesis, structural activity-relationships, and biological evaluation of novel amide-based allosteric binding site antagonists in NR1A/NR2B N-methyl-d-aspartate receptors

In rat adipocyte membranes, both beta-adrenergic agonists and beta-adrenergic antagonists competed with (--)(/sup 3/H)dihydroalprenolol for high affinity (KD 2-4 nM) and low capacity binding sites. The antagonists but not the agonists competed with (--)(/sup 3/H)dihydroalprenolol for lower affinity and higher capacity sites. The present studies were performed in order to characterize the adipocyte beta-adrenergic receptor and distinguish it from low affinity, higher capacity sites which were heat-labile and not stereoselective. When isoproterenol was used to define the nonspecific binding, saturation studies showed a single binding site with a capacity of approximately 100 fmol/mg membrane protein (corresponding to approximately 50,000 sites/adipocyte). Binding was saturated by 10 nM (--)(/sup 3/H)dihydroalprenolol. Approximate KD's of 204 nM were ...

1982-09-01

4

British Library Electronic Table of Contents (United Kingdom)

The synthesis and structure-activity relationship analysis of a novel class of amide-based biaryl NR2B-selective NMDA receptor antagonists are presented. Some of the studied compounds are potent, selective, non-competitive, and voltage-independent antagonists of NR2B-containing NMDA receptors. Like the founding member of this class of antagonists (ifenprodil), several interesting compounds of the series bind to the amino terminal domain of the NR2B subunit to inhibit function. Analogue potency is modulated by linker length, flexibility, and hydrogen bonding opportunities. However, unlike previously described classes of NR2B-selective NMDA antagonists that exhibit off-target activity at a variety of monoamine receptors, the compounds described herein show much diminished effects against the...

2009-01-01

5

New tools for human fat cell alpha-2A adrenoceptor characterization. Identification on membranes and on intact cells using the new antagonist (3H)RX821002

Developments of PET radioligands for NMDA receptors

The pharmacology of the alpha-2 adrenoceptor of the human adipocyte was improved by using some new alpha-2 antagonists from different chemical families (imidazolines, benzazepines and benzofuroquinolizines) in biological and binding assays. Moreover, investigations were also carried out to define the binding properties of a new imidazolinic antagonist, RX821002 (2-(2-methoxy-1,4-benzodioxan-2yl)-2-imidazoline), which could be a potential radioligand. (3H)RX821002 binding was very rapid and reversible. Saturation isotherms indicated that (3H)RX821002 labeled, with high affinity, a homogeneous population of noninteracting binding sites with a mean Kd of 0.98 +/- 0.05 nM (n = 6). The binding of (3H)RX821002 on the human fat cell alpha-2 adrenoceptor displayed a specificity which is strictly similar to that obtained with (3H)rauwolscine and ...

1990-01-01

6

ATRX ADD domain links an atypical histone methylation recognition mechanism to human mental-retardation syndrome

Aim: There has been a great demand for developments of the radioligands to visualize the N-methyl-D-aspartate (NMDA) receptors by PET/SPECT. We have recently synthesized two C-11 labeled antagonists for the glycine-binding site on NMDA receptors. The aim of this work is to examine for their in vitro and in vivo binding characteristics, and to evaluate their potentials as PET radioligands for the NMDA receptors. Materials and methods: Two C-11 labeled 4-hydroxy-2-quinolones (1 and 2) were synthesized by conventional methylation of the corresponding phenols with ["1"1C]methyl iodide. In vitro and ex vivo quantitative autoradiographs with imaging plate, as well as animal PET, were employed in order to evaluate their in vitro and in vivo binding to the NMDA receptors. Results: The compound 1 showed the specific binding to rat brain slices with higher localization in the hippocampus and ...

2002-09-01

7

Characterization of histamine H_1-receptor binding peptides in guinea pig brain using ["1"2"5I]iodoazidophenpyramine, an irreversible specific photoaffinity probe

ATR-X (alpha-thalassemia/mental retardation, X-linked) syndrome is a human congenital disorder that causes severe intellectual disabilities. Mutations in the ATRX gene, which encodes an ATP-dependent chromatin-remodeler, are responsible for the syndrome. Approximately 50% of the missense mutations in affected persons are clustered in a cysteine-rich domain termed ADD (ATRX-DNMT3-DNMT3L, ADD{sub ATRX}), whose function has remained elusive. Here we identify ADD{sub ATRX} as a previously unknown histone H3-binding module, whose binding is promoted by lysine 9 trimethylation (H3K9me3) but inhibited by lysine 4 trimethylation (H3K4me3). The cocrystal structure of ADD{sub ATRX} bound to H3{sub 1-15}K9me3 peptide reveals an atypical composite ...

2011-07-19

8

Kinetics of in vivo binding of antagonist to muscarinic cholinergic receptor in the human heart studied by Positron Emission Tomography

Aminophenpyramine, a derivative of mepyramine (pyrilamine), a typical antagonists of histamine at its H_1 receptor was synthesized and converted into ["1"2"5I]iodoazidophenpyramine, a potential photoaffinity probe for the H_1 receptor. In the dark, reversible binding of this probe to cerebellar membranes occurred with a K/sub d/ of 1.2 x 10"-"1"1 M and a B/sub max/ of 240 fmol/mg of protein and was inhibited by various H_1-receptor antagonists with the expected potencies. These features establish the compound as one of the most potent H_1-receptor antagonists known so far. Upon IV irradiation, 5% of the bound radioactivity was covalently incorporated into cerebellar membrane polypeptides as shown by standard NaDodSO_4/PAGE. Two bands of 47 and 56 kDa were consistently labeled, labeling being prevented by various H_1-receptor antagonists with the expected potencies and ...

9

The structure of myostatin:follistatin 288: insights into receptor utilization and heparin binding

Positron Emission Tomography (PET) was used to analyze in vivo antagonist binding to human myocardial muscarinic cholinergic receptor. The methiodide salt of the muscarinic antagonist, quinuclidinyl benzilate (MQNB), was labeled with the positron emitter, Carbon-11, and injected intravenously to 8 normal subjects. /sup 11/C-MQNB concentration was determined in vivo in the ventricular septum from 40 cross-sectional images acquired at the same transverse level over a period of 70 minutes. In 4 subjects, various amounts of unlabeled atropine were rapidly injected at 20 minutes to study whether atropine competitively inhibited MQNB. The kinetics of binding of /sup 11/C-MQNB were not the same in vivo and in vitro. The apparent dissociation rate of /sup 11/C-MQNB in vivo was much slower (by 1 to 2 orders of magnitude) than that observed in vitro with /sup 3/H-QNB. After atropine injection, /sup 11/C-MQNB ...

1984-08-27

10

Novel high-throughput screening system for identifying STAT3-SH2 antagonists

Myostatin is a member of the transforming growth factor-{beta} (TGF-{beta}) family and a strong negative regulator of muscle growth. Here, we present the crystal structure of myostatin in complex with the antagonist follistatin 288 (Fst288). We find that the prehelix region of myostatin very closely resembles that of TGF-{beta} class members and that this region alone can be swapped into activin A to confer signalling through the non-canonical type I receptor Alk5. Furthermore, the N-terminal domain of Fst288 undergoes conformational rearrangements to bind myostatin and likely acts as a site of specificity for the antagonist. In addition, a unique continuous electropositive surface is created when myostatin binds Fst288, which significantly increases the affinity for heparin. This translates into stronger interactions with the cell surface and enhanced myostatin degradation in the presence of either ...

2009-09-29

11

Physical Characteristics and Antagonistic Effect of Ampelomyces

Constitutive activation of the oncogenic transcription factor STAT3 frequently occurs in various human malignancies. STAT3 activation involves dimerization via intermolecular pTyr-SH2 interaction. Thus, antagonizing this interaction is a feasible approach to inhibit STAT3 activation for cancer therapy. In order to identify selective STAT3 inhibitors, we developed a biochemical HTS system based on AlphaScreen technology, which measures the abilities of test compounds to antagonize pTyr-SH2 interactions. We screened our chemical libraries using this system and identified 5,15-diphenylporphyrin (5,15-DPP) as a selective STAT3-SH2 antagonist. Selective inhibition of STAT3 nuclear translocation and DNA biding activity was observed in cells treated with 5,15-DPP. IL-6-dependent dimerization of STAT3, c-myc promoter binding and c-myc protein expression were all suppressed by 5,15-DPP, whereas no decrement in either expression or phosphorylation level ...

2009-03-13

12

Light-dependent regulation of DEL1 is determined by the antagonistic action of E2Fb and E2Fc.

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2009-12-01

13

Anti-muscarinic actions of mitoxantrone in isolated heart muscles of guinea pigs.

Endoreduplication represents a cell cycle variant during which multiple rounds of DNA replication occur without subsequent chromosome separation and cytokinesis, resulting into a cellular increase of the DNA content. Although the DNA ploidy level of cells is controlled by external stimuli such as light, currently limited knowledge is available on how environmental signals regulate the endoreduplication cycle at the molecular level. Previously, we have demonstrated that the conversion from the mitotic cell cycle into an endoreduplication cycle is mediated by the atypical E2F transcription factor DEL1 that operates as a repressor of endocycle onset. Here, we identified DEL1 as a transcriptional target of the classical E2Fb and E2Fc transcription factors that antagonistically control DEL1 transcript levels through competition for a single E2F cis-acting binding site. Correspondingly with the reported opposite effect of light on the E2Fb and E2Fc ...

2011-09-01

14

Local chromatin structure of heterochromatin regulates repeatedDNA stability, nucleolus structure, and genome integrity

A hypotheses that mitoxantrone is a competitive antagonist at muscarinic cholinergic receptors was examined in guinea-pig hearts. In isolated left atrial muscle preparations, electrically paced at 2 Hz, the muscarinic agonist, carbachol, caused a concentration-dependent decrease in developed tension. Mitoxantrone caused a parallel right-ward shift of the concentration-response curve for carbachol. Schild plots for the effect of mitoxantrone on the carbachol concentration-response relationship were linear with a slope of 0.88 which was not significantly different from the unity. The right-ward shift of the carbachol concentration-response relationship by mitoxantrone significantly reversed after an additional incubation with a mitoxantrone-free solution, although the reversal was incomplete after a 2-h incubation in the mitoxantrone-free solution. Mitoxantrone caused a concentration-dependent displacement of specific [3H]quinuclidinyl benzilate ...

2000-10-27

15

Kinetic analysis of transport and opioid receptor binding of ( sup 3 H)(-)-cyclofoxy in rat brain in vivo: Implications for human studies

Heterochromatin constitutes a significant portion of the genome in higher eukaryotes; approximately 30% in Drosophila and human. Heterochromatin contains a high repeat DNA content and a low density of protein-encoding genes. In contrast, euchromatin is composed mostly of unique sequences and contains the majority of single-copy genes. Genetic and cytological studies demonstrated that heterochromatin exhibits regulatory roles in chromosome organization, centromere function and telomere protection. As an epigenetically regulated structure, heterochromatin formation is not defined by any DNA sequence consensus. Heterochromatin is characterized by its association with nucleosomes containing methylated-lysine 9 of histone H3 (H3K9me), heterochromatin protein 1 (HP1) that binds H3K9me, and Su(var)3-9, which methylates ...

2007-05-05

16

Short-term regulation of muscarinic acetylcholine receptors: An assessment utilizing mouse brain and mouse neuroblastoma cells

(3H)Cyclofoxy (CF: 17-cyclopropylmethyl-3,14-dihydroxy-4,5-alpha-epoxy-6-beta-fluoromorp hinan) is an opioid antagonist with affinity to both mu and kappa subtypes that was synthesized for quantitative evaluation of opioid receptor binding in vivo. Two sets of experiments in rats were analyzed. The first involved determining the metabolite-corrected blood concentration and tissue distribution of CF in brain 1 to 60 min after i.v. bolus injection. The second involved measuring brain washout for 15 to 120 s following intracarotid artery injection of CF. A physiologically based model and a classical compartmental pharmacokinetic model were compared. The models included different assumptions for transport across the blood-brain barrier (BBB); estimates of nonspecific tissue binding and specific binding to a single opiate receptor site were found to be essentially the same with both models. The nonspecific ...

1991-03-01

17

Development of gamma-emitting, receptor binding radiotracers for imaging the brain and pancreas

The effects of muscarinic agonists and diisopropylfluorophosphate (DFP) on muscarinic receptor density and muscarinic receptor-mediated responses was assessed in mouse brain and mouse neuroblastoma cells (clone N1E-115). Utilizing the antagonist ({sup 3}H)quinuclidinyl benzilate (({sup 3}H)QNB), there was no difference in the maximal binding capacity (B{sub max}) or equilibrium dissociation constant (K{sub d}) between untreated and 24 hour DFP-treated mice. However, one administration of DFP produced a 24% and 33% decrease in B{sub max} measured by ({sup 3}H)N-methylscopolamine (({sup 3}H)NMS) after 18 and 24 hours which was rapidly reversible within 36 hours after DFP treatment. The loss of ({sup 3}H)NMS binding sites following acute DFP treatment was not accompanied by a change in a particular muscarinic receptor binding conformation. Furthermore, the magnitude of muscarinic receptor-mediated ...

1988-01-01

18

UHRF1, a modular multi-domain protein, regulates replication-coupled crosstalk between DNA methylation and histone modifications

This progress report covers period from Nov. 1, 1989 to Aug. 31, 1990. The long term objective was to develop receptor-binding radiotracers for SPECT or PET imaging of CNS or peripheral nervous system. The specific chemistry aims, as understood on the basis of past findings, were: to synthesize and develop a more polar analogs of 4IQNB, possessing similar binding characteristics but eliminated more rapidly from the surrounding tissues and the target organ, to design a method of introducing a technetium chelating group onto a molecule or cholinergic agent without drastic lowering of its apparent affinity, to synthesize and develop radiotracers based on m-AChR antagonists selective for one of the subtypes of the receptor. The chemistry service aims were to prepare and characterize (R,R)- and (R,S)-4IQNB and derivatives, to provide the triazene intermediate to other investigators, and to provide ({sup 123}I)4IQNB for in vivo ...

1990-01-01

19

In vitro assessment of the agonist properties of the novel 5-HT_1_A receptor ligand, CUMI-101 (MMP), in rat brain tissue

Cytosine methylation in DNA is a major epigenetic signal, and plays a central role in propagating chromatin status during cell division. However the mechanistic links between DNA methylation and histone methylation are poorly understood. A multi-domain protein UHRF1 (ubiquitin-like, containing PHD and RING finger domains 1) is required for DNA CpG maintenance methylation at replication forks, and mouse UHRF1-null cells show enhanced susceptibility to DNA replication arrest and DNA damaging agents. Recent data demonstrated that the SET and RING associated (SRA) domain of UHRF1 binds hemimethylated CpG and flips 5-methylcytosine out of the DNA helix, whereas its tandom tudor domain and PHD domain bind the tail of histone H3 in a highly methylation sensitive manner. We hypothesize that UHRF1 brings the two components (histones and DNA) carrying appropriate markers (on the tails of ...

2009-01-01

20

Characterization of the xanthine-binding site on R/sub a/ and R/sub i/ subtypes of the adenosine receptor

Introduction: Development of agonist positron emission tomography (PET) radioligands for the 5-HT neurotransmitter system is an important target to enable the understanding of human 5-HT function in vivo. ["1"1C]CUMI-101, proposed as the first 5-HT_1_A receptor agonist PET ligand, has been reported to behave as a potent 5-HT_1_A agonist in a cellular system stably expressing human recombinant 5-HT_1_A receptors. In this study, we investigate the agonist properties of CUMI-101 in rat brain tissue. Methods: ["3"5S]-GTP#gamma#S binding studies were used to determine receptor function in HEK (human embryonic kidney) 293 cells transfected with human recombinant 5-HT_1_A receptors and in rat cortex and rat hippocampal tissue, following administration of CUMI-101 and standard 5-HT1A antagonists (5-HT, 5-CT and 8-OH-DPAT). Results: CUMI-101 behaved as an agonist at human recombinant 5-HT_1_A receptors (pEC_5_0 9.2). However, CUMI-101 did not show ...

2011-02-01

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cap alpha. -2 adrenergic receptor: a radiohistochemical study

Methylxanthines and their derivatives are antagonists at cell surface adenosine receptors. They report here a systematic study of xanthine structure-activity relationships which compares potency at two adenosine receptor subtypes, R/sub a/ and R/sub i/. Adenylate cyclase stimulation (R/sub a/ in platelet membranes) and inhibition (R/sub i/ in adipocyte membranes) were used as models of receptor activation. K/sub i/ values were obtained by Schild analysis. The orders of potency of the xanthines to attenuate the effects of adenosine analogues were similar to those previously reported. Earlier work utilizing radioligand binding (R/sub i/ and (/sup 3/H) cAMP formation (R/sub a/) claimed that IIX and PACPX are at least 10 and 400 fold, respectively, more potent at R/sub i/ than at R/sub a/. However, in their assays which utilize modulation of receptor-coupled adenylate cyclase, the xanthines show little specificity for either adenosine receptor ...

1986-05-01

22

Structure-activity relationships of anthraquinones on the suppression of DNA-binding activity of the aryl hydrocarbon receptor induced by 2,3,7,8-tetrachlorodibenzo-p-dioxin.

..cap alpha..-2 adrenergic agents have been shown to influence blood pressure, heart rate and other physiological and behavioral functions through interactions with adrenergic pathways within the central nervous system. Pharmacologically relevant ..cap alpha..-1 adrenergic receptors were biochemically characterized and radiohistochemically analyzed in intact tissue sections of the rat and human central nervous system. The anatomical distribution of the ..cap alpha..-2 receptors, labeled with the agonist (/sup 3/H)para-aminoclonidine, verified the concept that ..cap alpha..-2 receptors are closely associated with adrenergic nerve terminals and that ..cap alpha..-2 agents can influence autonomic and endocrine function through an action in the central nervous system. Since ..cap alpha..-2 agonists can influence sympathetic outflow, ..cap alpha..-2 binding sites were closely analyzed in the intermediolateral cell column of the thoracic spinal cord. The transport of ...

1984-01-01

23

Radiolabelled D2 agonists as prolactinoma imaging agents

Anthraquinones are widely present in plant kingdom, and clinically used as laxatives. Environmental contaminants, dioxins, develop various adverse effects through transformation of a cytosolic aryl hydrocarbon receptor (AhR). We investigated the effects of 18 anthraquinones and 7 of their structurally related compounds on transformation of the AhR estimated by its DNA-binding activity in the cell-free system. 1,4-Dihydroxyanthraquinone (quinizarin), 1,5-dihydroxyanthraquinone (anthrarufin), 1,8-dihydroxyanthraquinone (danthron), and 5-hydroxy-1,4-naphthoquinone (juglone) strongly suppressed DNA-binding activity of the AhR induced by 0.1 nM 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), with their IC(50) values around 1 muM. On the other hand, anthraquinone, 2,6-dihydroxyanthraquinone (anthraflavic acid), and 2-hydroxy-1,4-naphthalendione (lawsone) showed moderate effects. Quantitative structure-activity relationships analysis demonstrated that ...

2009-03-01

24

High-precision Penning-Trap measurements of light-ion masses

During the past year, further studies on mAChR were conducted. These studies included verification of the difference in pituitary distribution based on ligand charge. The pituitary localization of TRB. A neutral mAChR ligand, was verified. The lack of QNB blockade of TRB uptake was tested by blockage with scopolamine, another mAChR antagonist and by testing the effect in a different strain of rat. Neither scopolamine or change of rat strain had any effect. We concluded that TRB uptake in pituitary is not a receptor-mediated process. Further studies were conducted with an additional quaternized mAChR ligand: MQNB. Pituitary localization of MQNB, like MTRB, could be blocked by pretreatment with QNB. We have tentatively concluded that permanent charge on a mAChR antagonist changes the mechanism of uptake in the pituitary. Time course studies and the effects of DES on myocardial uptake are reported. A brief report on preliminary results of ...

1989-08-01

25

Adsorption and dissociation of water on the (0001) surface of double hexagonal close packed americium

The UW-Penning Trap Mass Spectrometer (PTMs) is ideally suited for high precision measurements of atomic masses throughout the periodic table upon using highly-stripped ions. However, at the present time, this device has been applied extensively to the light elements ("1H, "2H, "3H, "3He, "4He, "1"2C, "1"3C, "1"4N, "1"6O) due to their fundamental importance. Atomic masses follow immediately from a comparison with some multiply-charged carbon ion, after correcting for the lost electrons and their corresponding binding energies. For instance, the most recent C"5"+/C"6"+ comparison yielded a discrepancy of -0.30(33) ppb, limited only by the magnetic field instability for a 40-h run. The initial emphasis on hydrogen has now produced a 1-ppb value for the proton's atomic mass and similar work with deuterium has yielded a 2.5-ppb value for the neutron's atomic mass. However, the most ...

1993-04-12

26

Succession of Indigenous Pseudomonas spp. and Actinomycetes on Barley Roots Affected by the Antagonistic Strain Pseudomonas fluorescens DR54 and the Fungicide Imazalil

Ab initio total energy calculations within the framework of density functional theory have been performed for water molecule adsorption on the (0001) surface of double hexagonal packed americium using a full-potential all-electron linearized augmented plane wave plus local orbitals method (FP-L/APW+lo). Subsequent partial dissociation (OH+H) and complete dissociation (H+O+H) of the water molecule have been examined. The completely dissociated H+O+H configuration exhibit the strongest binding with the surface (3.35 eV), followed by partially dissociated species OH+H (2.23 eV), with all molecular H_2O configurations showing weak physisorption (0.366 eV). For molecular adsorptions, the flat lying orientation of the water molecule if found to be more favorable for majority of the cases. In the case of partial dissociation (OH+H), the vertical orientation of OH molecule with O facing the surface adsorbed at a h3 adsorption site ...

2009-06-01

27

ProteoChip-based Library Screening of Integrin ${\\alpha}5{\\beta}1$ Antagonists from Korean Medicinal Plant Extracts

In recent years, the interest in the use of bacteria for biological control of plant-pathogenic fungi has increased. We studied the possible side effects of coating barley seeds with the antagonistic...Full Text Available

2001-03-01

28

Comparison of Microbial Fungicides in Antagonistic Activities Related to the Biological Control of Phytophthora Blight in Chili Pepper Caused by Phytophthora capsici

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2007-12-01

29

Aggregation of silica nanoparticles directed by adsorption of lysozyme.

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2010-12-01

30

Salt modulates the stability and lipid binding affinity of the adipocyte lipid-binding proteins

The interaction of the globular protein lysozyme with silica nanoparticles of diameter 20 nm was studied in a pH range between the isoelectric points (IEPs) of silica and the protein (pH 3-11). The adsorption affinity and capacity of lysozyme on the silica particles is increasing progressively with pH, and the adsorbed protein induces bridging aggregation of the silica particles. Structural properties of the aggregates were studied as a function of pH at a fixed protein-to-silica concentration ratio which corresponds to a surface concentration of protein well below a complete monolayer in the complete-binding regime at pH > 6. Sedimentation studies indicate the presence of compact aggregates at pH 4-6 and a loose flocculated network at pH 7-9, followed by a sharp decrease of aggregate size near the IEP of lysozyme. The structure of the bridged silica aggregates was studied by cryo-transmission electron microscopy ...

2011-07-20

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Radioiodination of 3-quinuclidinyl benzilate using a no-carrier-added concentration of iodine-125/sodium-iodine

Adipocyte lipid-binding protein (ALBP or aP2) is an intracellular fatty acid-binding protein that is

2003-01-01

32

Nuclear Medicine Program progress report for quarter ending September 30, 1992

3-Quinuclidinyl benzilate (QNB) is a potent muscarinic antagonist that binds to muscarinic acetylcholine receptors. Iodination of QNB is difficult because it contains rings that are deactivated, while phenol rings are activated. The purpose of this research is to develop an appropriate method for the iodination of QNB at no-carrier-added concentrations of /sup 125/I/NaI. Phenol was chose as the test compound for direct iodination by adding chloramine T and nonradioactive sodium iodide to the phenol in a phosphate buffer and methanol system. A simple method to radioiodinate QNB at several concentrations was developed in situ in the presence of QNB, thallic trifluoroacetate /sup 125/I/NaI, /sup 127/I/NaI, and aluminium chloride. Using milligram amounts of QNB (7.12 x 10/sup -6/ moles), three reaction steps were involved: QNB was reacted with thallic trifluoroacetate at 60/sup 0/C for 24 hours, then radioactive /sup 125/I/NaI and aluminium ...

1986-01-01

33

B chain is a functional subunit of beta-bungarotoxin for inducing apoptotic death of human neuroblastoma SK-N-SH cells.

The radioiodination and in vivo evaluation of p-iodocaramiphen a muscarinic antagonist which binds with high affinity to the M[sub 1] receptor subtype in vitro are described. Biodistribution studies in female Fischer rats demonstrated that [[sup 125]I]-piodocaraminphen had significant cerebral localization, but the uptake did not demonstrate specific uptake in those cerebral regions rich in muscarinic receptors, and radioactivity washed out rapidly from the brain. In addition there was no significant blockage of activity when the rats were preinjected with quinuclidinyl benzilate. These results suggest that p-iodocaramiphen is not a good candidate for the in vivo study of M[sub 1] muscarinic receptor populations by SPECT. Because of the widespread interest and expected importance of the availability of large amounts of tungsten-188 required for the tungsten-188/rhenium-188 generator systems, we have investigated the large-scale production of ...

1992-12-01

34

Magnetization and magnetic susceptibilities of GdH_3, HoH_3, ErH_3 and YbH_3

beta-Bungarotoxin (beta-Bgt), a presynaptic phospholipase A(2) (PLA(2)) neurotoxin isolated from the venom of Bungarus multicinctus, consists of A chain and B chain. The goal of the present study is to explore the functional contribution of the two subunits to the toxicity of beta-Bgt. beta-Bgt was found to induce apoptotic death of SK-N-SH cells via elevating intracellular Ca(2+) and intracellular ROS production. Moreover, an activation of p38 MAPK was associated with the cytotoxicity of beta-Bgt. SB202190 (p38 MAPK inhibitor), N-acetylcysteine (antioxidant reagent), 1,2-bis(2-aminophenoxy)ethane-N,N,N,N-tetraacetic acid (BAPTA) (Ca(2+) chelator) and the inhibitors of Ca(2+) release from intracellular depots (ruthenium red and 2-aminoethoxydiphenyl borate) effectively attenuated the cytotoxicity of beta-Bgt. In sharp contrast to the inability of A chain, B chain was able to induce cytotoxic effects on SK-N-SH cells as beta-Bgt did. Abolishment of PLA(2) activity did not significantly ...

2007-10-13

35

Transformation of Verapamil by Cunninghamella blakesleeana

The magnetic susceptibility of powdered samples of HoH_3, ErH_3, GdH_3 and YbH_3 have been measured in the temperature range from 4.2 to 1.2 K. Two broad, local maxima are observed in the variation of chi versus T for GdH_3, with maxima in (delta chi/delta T) versus T at 1.8 K and 3.3 K. The inverse susceptibilities for HoH_3 and ErH_3 both obey a Curie--Weiss law over a limited range (4.2 to 2.6 K and 4.2 to 2 K, respectively) with values for the Weiss constant of -4.25 K and -1.11 K, and effective moments of 8.6 and 7.7 Bohr magnetons, respectively. The susceptibility of YbH_3 is independent of temperature over the range investigated. High-field ...

1976-03-29

36

Theoretical and practical considerations on the problem of metal--metal interaction.

A filamentous fungus, Cunninghamella blakesleeana AS 3.153, was used as a microbial model of mammalian metabolism to transform verapamil, a calcium channel antagonist. The metabolites...Full Text Available

2004-05-01

37

TNF-alpha antagonist therapy modify the tuberculin skin test response

The interaction between two metals, which can be either synergistic or antagonistic, implies that the behavior of one is changed by the presence of the other. Possible mechanisms of these interactions,...Full Text Available

1978-08-01

38

British Library Electronic Table of Contents (United Kingdom)

Tumour necrosis factor-alpha (TNF-?) antagonist drugs have been associated with increased risk of tuberculosis (TB). Tuberculin skin test (TST) is the most frequently used tool for identification of latent TB infection. We herein aimed to analyse the effect of TNF-? antagonists on the TST responses in a prospective study. The study group consisted of 182 patients (99 female, 83 male) who received TNF-? antagonists for various rheumatic disorders. All patients were evaluated with TST along with other parameters on the day of referral and on the 12th month visit. For those patients with a response of <5?mm induration at the initial evaluation, the TST was repeated to observe the booster effect. Out of 182 patients, 87 patients (48%) had a negative (0?4?mm) and 95 (52%) had a positive (?5?mm)...

2011-01-01

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Regulation of Senescence in Cancer and Aging

Albumin binding of photobilirubin II.

Senescence is regarded as a physiological response of cells to stress, including telomere dysfunction, aberrant oncogenic activation, DNA damage, and oxidative stress. This stress response has an antagonistically...Full Text Available

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Role of intrathecal tachykinins for micturition in unanaesthetized rats with and without bladder outlet obstruction.

Photobilirubin II, a stereoisomer of bilirubin, binds to human serum albumin at a single binding site (K = 2.2 x 10(6)M-1), presumably the high-affinity bilirubin-binding site. Binding in the secondary...Full Text Available

1983-07-01

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Effects of the cannabinoid antagonist SR141716 (rimonabant) and d-amphetamine on palatable food and food pellet intake in non-human primates

1. The effects on micturition of RP 67,580, a selective NK1 receptor antagonist, and SR 48,968, a highly, potent antagonist at NK2 receptor sites, given intrathecally (i.t.) or intra-arterially (i.a.)...Full Text Available

1994-09-01

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A randomized trial of microdose leuprolide acetate protocol versus luteal phase ganirelix protocol in predicted poor responders

The purpose of this study was to determine if a cannabinoid CB₁ receptor antagonist would selectively decrease consumption of highly palatable food in non-human primates. The CB₁...Full Text Available

2007-04-01

43

British Library Electronic Table of Contents (United Kingdom)

We performed a randomized trial to compare IVF outcomes in 54 poor responder patients undergoing a microdose leuprolide acetate (LA) protocol or a GnRH antagonist protocol incorporating a luteal phase E2 patch and GnRH antagonist in the preceding menstrual cycle. Cancellation rates, number of oocytes retrieved, clinical pregnancy rates (PR), and ongoing PRs were similar between the two groups.

2011-01-01

44

Plasminogen Binding and Activation at the Surface of Helicobacter pylori CCUG 17874

Ophidian envenomation strategies and the role of purines.

The binding of iodine-labelled plasminogen to Helicobacter pylori CCUG 17874 was characterized. Inhibition of the binding was observed after preincubation of H. pylori...Full Text Available

1998-10-01

45

Polyadenylated H3 histone transcripts and H3 histone variants in alfalfa.

Snake envenomation employs three well integrated strategies: prey immobilization via hypotension, prey immobilization via paralysis, and prey digestion. Purines (adenosine, guanosine and inosine) evidently play a central role in the envenomation strategies of most advanced snakes. Purines constitute the perfect multifunctional toxins, participating simultaneously in all three envenomation strategies. Because they are endogenous regulatory compounds in all vertebrates, it is impossible for any prey organism to develop resistance to them. Purine generation from endogenous precursors in the prey explains the presence of many hitherto unexplained enzyme activities in snake venoms: 5'-nucleotidase, endonucleases (including ribonuclease), phosphodiesterase, ATPase, ADPase, phosphomonoesterase, and NADase. Phospholipases A(2), cytotoxins, myotoxins, and heparinase also participate in purine liberation, in addition to their better known functions. Adenosine contributes to prey immobilization ...

2002-04-01

46

A Role for Set1/MLL-Related Components in Epigenetic Regulation of the Caenorhabditis elegans Germ Line

Histone H3 mRNAs were found in polyA(+) fractions of total RNA prepared from alfalfa plants, calli and somatic embryos. The sequence analysis of cDNAs revealed the presence of a polyA tail on independent...Full Text Available

1989-04-25

47

In vitro competitive adhesion and production of antagonistic compounds by lactic acid bacteria against fish pathogens

The methylation of lysine 4 of Histone H3 (H3K4me) is an important component of epigenetic regulation. H3K4 methylation is a consequence of transcriptional activity, but also has been shown to contribute...Full Text Available

2011-03-01

48

British Library Electronic Table of Contents (United Kingdom)

The present study describes the screening of five lactic acid bacteria (LAB) for use as probiotics based on their competitive adhesion and production of antagonistic substances against some fish pathogens. A reduction of adhesion of all pathogenic strains tested was obtained with three of the LAB strains (Lactococcus lactis subsp. lactis CLFP100, Lactococcus lactis subsp. cremoris CLFP102 and Lactobacillus curvatus CLFP150). With the exception of fish pathogens Flavobacterium psychrophilum and Renibacterium salmoninarum that were not inhibited by LAB strains, production of antagonistic compounds by all tested LAB was observed against at least one of the indicator strains. Based on mucus adhesion, competitive exclusion, and suppression of fish pathogen growth, the selected LAB strains can b...

2007-01-01

49

Selective estrogen receptor modulator (SERM) for the treatment of osteoporosis in postmenopausal women: focus on lasofoxifene

Reduction of IgG in nonhuman primates by a peptide antagonist of the neonatal Fc receptor FcRn

Selective estrogen receptor modulators (SERMs) represent a class with a growing number of compounds that act as either estrogen receptor agonists or antagonists in a tissue-specific manner. This article...Full Text Available

2010-01-01

50

RU486 did not exacerbate cytokine release in mice challenged with LPS nor in db/db mice

The neonatal Fc receptor FcRn provides IgG molecules with their characteristically long half-lives in vivo by protecting them from intracellular catabolism and then returning them to...Full Text Available

2008-02-19

51

Progressive ratio performance following challenge with antipsychotics, amphetamine, or NMDA antagonists in adult rats treated perinatally with phencyclidine

BackgroundGlucocorticoids down-regulate cytokine synthesis and suppress inflammatory responses. The glucocorticoid receptor (GR) antagonist RU486 may exacerbate the inflammatory...Full Text Available

52

Pharmacokinetics and tolerability of zibotentan (ZD4054) in subjects with hepatic or renal impairment: two open-label comparative studies

RationalePrevious research has shown that rats exposed perinatally to phencyclidine (PCP) exhibited neuroanatomical abnormalities and altered cognition. In addition...Full Text Available

2004-12-01

53

Novel Analogs and Stereoisomers of the Marine Toxin Neodysiherbaine with Specificity for Kainate Receptors

BackgroundZibotentan (ZD4054) is a specific endothelin A (ET_A) receptor antagonist being investigated for the treatment of prostate cancer. As zibotentan is eliminated...Full Text Available

54

Misreporting of myocardial infarction end points: results of adjudication by a central clinical events committee in the PARAGON-B trial. Second Platelet IIb/IIIa Antagonist for the Reduction of Acute Coronary Syndrome Events in a Global Organization Network Trial.

Antagonists for kainate receptors (KARs), a family of glutamate-gated ion channels, are efficacious in a number of animal models of neuropathologies, including epilepsy, migraine pain, and anxiety....Full Text Available

2008-02-01

55

Micturition in conscious rats with and without bladder outlet obstruction: role of spinal alpha 1-adrenoceptors.

PMID:11835026

2002-02-01

56

Human placental transport of cimetidine.

1. In normal rats and rats with bladder hypertrophy secondary to outflow obstruction, undergoing continuous cytometry, we examined the responses to the selective alpha 1-adrenoceptor antagonist doxazosin...Full Text Available

1996-03-01

57

Effects of a growth hormone-releasing hormone antagonist on telomerase activity, oxidative stress, longevity, and aging in mice

This study addresses the mechanism of transport of the H2-receptor antagonist, cimetidine, by the human placenta. A 4-h recycling perfusion of a single placental cotyledon of normal, term, human placenta...Full Text Available

1987-11-01

58

Cardiovascular Safety of Degarelix: Results From a 12-Month, Comparative, Randomized, Open Label, Parallel Group Phase III Trial in Patients With Prostate Cancer

Both deficiency and excess of growth hormone (GH) are associated with increased mortality and morbidity. GH replacement in otherwise healthy subjects leads to complications, whereas individuals with...Full Text Available

2010-12-21

59

Brg1 Is Required for Cdx2-Mediated Repression of Oct4 Expression in Mouse Blastocysts

PurposeWe assessed the cardiovascular safety profile of degarelix, a new gonadotropin-releasing hormone antagonist.Materials...Full Text Available

2010-12-01

60

Antidepressant-Like Effects of ?-Opioid Receptor Antagonists in Wistar Kyoto Rats

During blastocyst formation the segregation of the inner cell mass (ICM) and trophectoderm is governed by the mutually antagonistic effects of the transcription factors Oct4 and Cdx2. Evidence indicates...Full Text Available

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61

Antagonistic crosstalk between APC and HIF-1?

The Wistar Kyoto (WKY) rat strain is a putative genetic model of comorbid depression and anxiety. Previous research showing increased κ-opioid receptor (KOR)...Full Text Available

2010-02-01

62

Antagonistic Gcn5-Hda1 interactions revealed by mutations to the Anaphase Promoting Complex in yeast

Most colorectal cancers have mutations in the tumor suppressor APC. The best-understood function of APC is its participation in a protein complex that regulates the availability of β-catenin....Full Text Available

2011-05-15

63

Antagonist HIV-1 Gag Peptides Induce Structural Changes in HLA B8

BackgroundHistone post-translational modifications are critical for gene expression and cell viability. A broad spectrum of histone lysine residues have been identified in yeast...Full Text Available

64

Adenomatous Polyposis Coli and Hypoxia-inducible Factor-1? Have an Antagonistic Connection

In the cellular immune response, recognition by CTL-TCRs of viral antigens presented as peptides by HLA class I molecules, triggers destruction of the virally infected cell (Townsend, A.R.M., J. Rothbard,...Full Text Available

1996-12-01

65

A population pharmacokinetic meta-analysis of maraviroc in healthy volunteers and asymptomatic HIV-infected subjects

The tumor suppressor adenomatous polyposis coli (APC) is mutated in the majority of colorectal cancers and is best known for its role as a scaffold in a Wnt-regulated protein complex that determines...Full Text Available

2010-11-01

66

Binding the Mammalian High Mobility Group Protein AT-hook 2 to AT-Rich Deoxyoligonucleotides: Enthalpy-Entropy Compensation

AimsTo develop a population pharmacokinetic model for maraviroc, a noncompetitive CCR5 antagonist, after oral administration of tablets to healthy volunteers and asymptomatic HIV-infected...Full Text Available

2008-04-01

67

FALP studies of dissociative recombination: the intriguing case of the (H_3"+ + e) reaction

HMGA2 is a DNA minor-groove binding protein. We previously demonstrated that HMGA2 binds to AT-rich DNA with very high binding affinity where the binding of HMGA2 to poly(dA-dT)₂ is enthalpy-driven...Full Text Available

2009-05-20

68

The binding of polyribosomes to smooth and rough endoplasmic-reticulum membranes (Short Communication)

The primary purpose of this short paper is to present a brief report on what we believe is state-of-the-art regarding the measurements of the dissociative recombination coefficient for the important interstellar ion H_3"+ at and near to thermal energies. However, theory has consistently indicated that dissociative recombination of H_3"+ should be inefficient at low energies. We do not try to present a detailed historical development of this topic here, but we rather refer the reader to our very recent papers and those of others. (author).

1994-03-20

69

In vitro protein binding of cefonicid and cefuroxime in adult and neonatal sera.

In vitro the binding of polyribosomes to smooth endoplasmic-reticulum membranes is more sensitive to ionic strength than is the binding to rough endoplasmic-reticulum membranes. Polyribosomes...Full Text Available

1973-04-01

70

Fatty Acid- and Retinoid-binding Proteins Have Distinct Binding Pockets for the Two Types of Cargo*

The levels of in vitro protein binding of cefonicid and cefuroxime in human adult and neonatal sera were compared. Binding parameters for each drug were determined within the concentration range of...Full Text Available

1993-06-01

71

Drug-binding properties of human alpha-foetoprotein.

Parasitic nematodes cause serious diseases in humans, animals, and plants. They have limited lipid metabolism and are reliant on lipid-binding proteins to acquire these metabolites from their hosts....Full Text Available

2009-12-18

72

Characterization of discrete classes of binding sites of human serum albumin by application of thermodynamic principles.

The drug-binding properties of human alpha-foetoprotein (alpha FP) were investigated by a fluorescence-spectral method. Human alpha FP was shown to bind to albumin's site I marker (warfarin, phenylbutazone),...Full Text Available

1985-10-01

73

Albumin binding of insulins acylated with fatty acids: characterization of the ligand-protein interaction and correlation between binding affinity and timing of the insulin effect in vivo.

The binding interactions of four ligands differing in acid-base properties with human serum albumin (HSA) were examined as a function of temperature. Binding to HSA decreased with increasing temperature...Full Text Available

1994-08-15

74

A hypothetical model for the peptide binding domain of hsp70 based on the peptide binding domain of HLA.

Albumin is a multifunctional transport protein that binds a wide variety of endogenous substances and drugs. Insulins with affinity for albumin were engineered by acylation of the epsilon-amino group...Full Text Available

1995-12-15

75

NATIONALAIIVISBRY COMMITTEE Ffltt AERONAUTICS - NASA Technical ...

The sequences of the peptide binding domains of 33 70 kd heat shock proteins (hsp70) have been aligned and a consensus secondary structure has been deduced. Individual members showed no significant...Full Text Available

1991-05-01

76

Modeling of the Three-Body Effects in the Neutral Trimers in the Quartet State by ab initio Calculations. H3, Na3, and Na2B.

Watkins,. Charles. E. : Effect of Aspect. Ratio on the Air ...... Grover,. H. 3. ; Bishop,. S. M. ; and. Jackson,. L. R. : Fatigue. Strengths of Aircraft ...

77

Czech Academy of Sciences Repository

Full Text Available

2003-01-01

78

The interaction of trazodone with rat brain muscarinic cholinoceptors.

The hepcidin-binding site on ferroportin is evolutionarily conserved

The muscarinic receptor binding of trazodone, a new nontricyclic antidepressant, was compared with established tricyclic antidepressants. The ability to inhibit the binding of [3H]-quinuclidinyl benzilate...Full Text Available

1980-01-01

79

Spatial Relationships between Drug Binding Sites on the ...

SummaryMammalian iron homeostasis is regulated by the interaction of the liver-produced peptide hepcidin and its receptor, the iron transporter ferroportin. Hepcidin binds to...Full Text Available

2008-08-01

80

Effects of the. cap alpha. -adrenoceptor antagonists phentolamine, phenoxybenzamine, and Idazoxan on sympathetic blood flow control in the periodontal ligament of the cat

... determination of the molar extinction coefficients, e, were measured by the Lowry method with native a-toxin as a standard. Binding Kinetics. ...

1987-10-15

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81

Effects of the cannabinoid antagonist SR141716 (rimonabant) and d-amphetamine on palatable food and food pellet intake in non-human primates

Blood flow changes in the periodontal ligament (PDL) were measured indirectly by monitoring the local clearance of /sup 125/I/sup -/ during electric sympathetic nerve stimulation or close intra-arterial infusions of either noradrenaline (NA) or adrenaline (ADR) before and after administration of phentolamine (PA), phenoxybenzamine (PBZ) or Idazoxan (RX). At the doses used in the present study, PA was the only antagonist that significantly reduced the blood flow decrease seen on activation of sympathetic fibers, although PBZ also reduced this response. Idazoxan, however, did not induce the consistent effect on blood flow decreases seen on sympathetic activation. All three ..cap alpha..-adrenoceptor antagonists almost abolished the effects of exogenously administered NA and ADR. The results suggest the presence of functional post-junctional adrenoceptors of both the ..cap alpha.. 1 and ..cap alpha.. 2 subtypes in the sympathetic regulation of the ...

1988-01-01

82

British Library Electronic Table of Contents (United Kingdom)

The purpose of this study was to determine if a cannabinoid CB1 receptor antagonist would selectively decrease consumption of highly palatable food in non-human primates. The CB1 receptor antagonist SR141716 (rimonabant; 0.12?1.0?mg/kg, i.m.) and the stimulant anorectic drug d-amphetamine (0.12?1.0?mg/kg, i.m.) were administered to non-food deprived baboons for the purpose of measuring the effect of each drug on consumption of the normal diet, and a large single meal of a high-carbohydrate candy. Four male and four female baboons had access to food 24?h each day, but they had to complete a two phase operant procedure in order to eat. Responding on one lever during a 30-min appetitive phase was required before animals could start a consumption phase, where responding on another lever led to...

2007-01-01

83

Antigenic drift in influenza virus H3 hemagglutinin from 1968 to 1980: multiple evolutionary pathways and sequential amino acid changes at key antigenic sites.

An improved synthesis of [5'-"3H]-3'-azido-3'-deoxythymidine, tritiated Zidovudine

Surveys of the antigenic properties of a wide range of variants of the H3N2 (Hong Kong) influenza virus subtype have revealed complex patterns of variants cocirculating during each of the main epidemic...Full Text Available

1983-10-01

84

Quantitative RT-PCR Expression Analysis of Lipodepsipeptides Synthetase and Defence-related Genes in Orange Fruit in Response to Antagonist-pathogen Interaction

[5'-"3H]-3'-Azido-3'-deoxythymidine (3) was prepared at a specific activity of 14.0 Ci/mmol by a two-step synthetic sequence involving controlled oxidation of the unlabelled compound (1) to the 5'-aldehyde (2) followed by reduction with ["3H]-NaBH_4. Purification was performed by preparative TLC. The radiochemical purity was 99.2%. (author).

85

British Library Electronic Table of Contents (United Kingdom)

Abstract Strains of Pseudomonas syringae are effective in controlling postharvest diseases of citrus fruits, and antagonistic activity has been correlated with in vitro production of lipodepsipeptides. Additionally, biocontrol agents can induce a range of defence mechanisms of resistance in citrus tissue that result in a broad spectrum of metabolic modifications, such as systemic acquired resistance, induced systemic resistance and production of reactive oxygen species. The aim of this study was to evaluate the expression of syringomycin (syrB1) and syringopeptin (sypA) synthetase genes from P.syringae pv. syringae biocontrol strains in vitro on different culture media and in vivo on citrus fruits (Citrus sinensis cv. Tarocco) during the interaction with Penicillium digitatum by quantitati...

2011-01-01

86

Inflammatory spine disease as a cause of back pain

Effect of the GnRH antagonist, acyline, on canine testicular characteristics.

The aim of this review is to evaluate the role of inflammatory spine disease in patients with chronic back pain. The contribution of imaging modalities for the diagnostic evaluation of back pain is discussed. A systematic literature search based on the classification of seronegative spondyloarthropathies and rheumatoid arthritis was performed. The results of this search and the experiences in a large collective of rheumatological patients are analyzed. The prevalence of rheumatoid arthritis (1-2%) is comparable to that of spondyloarthropathies (1.9%). The etiology of these entities is not fully elucidated. Magnetic resonance imaging is increasingly used for early detection and surveillance of therapy with TNF-#alpha# antagonists. Bone marrow edema, which is only detectable with MRI, represents an early sign of inflammation. Therapy with TNF-#alpha# antagonists is based on clinical and laboratory criteria, and signs of inflammation in MRI. MRI ...

2006-06-01

87

The fatty acid analogue 11-(dansylamino)undecanoic acid is a fluorescent probe for the bilirubin-binding sites of albumin and not for the high-affinity fatty acid-binding sites.

The primary objective was to assess the effects and clinical safety of a single high-dose of the third generation GnRH antagonist, acyline, on testicular characteristics in male dogs. Seven dogs were followed up weekly for six, 2-week periods (-2, -1, 1, 2, 3 and 4). At the end of the second period, they were given acyline (330 microg/kg sc). Responses to treatment varied among individual animals. Testicular consistency and scrotal diameter were slightly diminished (P>0.05) in Periods 1, 2, and 3. Libido and erection decreased during Periods 1 and 2 (Pdecreased semen quality with no adverse effects. PMID:17586037

2007-06-21

88

NMR assignment of the cAMP-binding domain A of the PKA regulatory subunit

1. The fluorescent fatty acid probe 11-(dansylamino)undecanoic acid (DAUDA) binds with high affinity to bovine and human serum albumin (BSA and HSA) at three sites. 2. The Kd of the primary binding...Full Text Available

1990-08-15

89

A Monoclonal Antibody That Specifically Binds Chitosan In Vitro and In Situ on Fungal Cell Walls

No abstract prepared.

2006-12-15

90

Reinforcing Effects of ?-Receptor Agonists in Rats Trained to Self-Administer Cocaine

Full Text Available

2010-08-01

91

In vivo modulation of murine serum tumour necrosis factor and interleukin-6 levels during endotoxemia by oestrogen agonists and antagonists.

σ-Receptor (σR) antagonists have been reported to block certain effects of psychostimulant drugs. The present study examined the effects of σR ligands in rats trained to self-administer...Full Text Available

2010-02-01

92

Dopamine D3 and D2 Receptor Mechanisms in the Abuse-Related Behavioral Effects of Cocaine: Studies with Preferential Antagonists in Squirrel Monkeys

Oestrogen has been reported to modulate tumour necrosis factor (TNF), interleukin (IL)-1 and IL-6 cytokine levels in human mononuclear cell cultures. In the present study, the effects of exogenous oestrogen...Full Text Available

1995-09-01

93

Discrimination between UTP- and P2-purinoceptor-mediated depolarization of rat superior cervical ganglia by 4,4'-diisothiocyanatostilbene-2,2'- disulphonate (DIDS) and uniblue A.

Dopamine (DA) D3 and D2 receptor mechanisms are implicated in cocaine's abuse-related behavioral effects, but the relative contribution of the two receptor subtypes is only partially characterized....Full Text Available

2010-08-01

94

Characterization of a Novel Small Molecule Subtype Specific Estrogen-Related Receptor ? Antagonist in MCF-7 Breast Cancer Cells

1. Using a grease-gap recording technique we have investigated the effects of some antagonists of P2-purinoceptors on the depolarization of the rat isolated superior cervical ganglion evoked by 100...Full Text Available

1995-06-01

95

Blockade of catecholamine-induced growth by adrenergic and dopaminergic receptor antagonists in Escherichia coli O157:H7, Salmonella enterica and Yersinia enterocolitica

BackgroundThe orphan nuclear receptor estrogen-related receptor α (ERRα) is a member of the nuclear receptor superfamily. It was identified through a search for genes...Full Text Available

96

Affinity purification of sequence-specific DNA binding proteins.

BackgroundThe ability of catecholamines to stimulate bacterial growth was first demonstrated just over a decade ago. Little is still known however, concerning the nature of the putative...Full Text Available

97

A study of the distribution of schistosomicidal drug H-3-7505 in mice

We describe a method for affinity purification of sequence-specific DNA binding proteins that is fast and effective. Complementary chemically synthesized oligodeoxynucleotides that contain a recognition site for a sequence-specific DNA binding protein are annealed and ligated to give oligomers. This DNA is then covalently coupled to Sepharose CL-2B with cyanogen bromide to yield the affinity resin. A partially purified protein fraction is combined with competitor DNA and subsequently passed through the DNA-Sepharose resin. The desired sequence-specific DNA binding protein is purified because it preferentially binds to the recognition sites in the affinity resin rather than to the nonspecific competitor DNA in solution. For example, a protein fraction that is enriched for transcription factor Sp1 can be further purified 500- to 1000-fold by two sequential affinity chromatography steps to give Sp1 of an ...

1986-08-01

98

Growth of mammary epithelial cells in breast-cancer biopsies correlates with EGF binding

The authors have studied the distribution of H-3 labelled schistosomicidal drug in mice by autoradiography. The H-3-labelled substances were found in liver and kidney and in successfully decreasing amounts in brain, lung, heart, fat, testis, pancreas and spleen. In various cells the silver granules were present mainly in the cytoplasms but a few in the nucleus. After administration of this labelled schistosomicidal drug, the mice were killed and studied in groups successively at 4, 8, 24 hrs. No difference in the distribution of silver granules were observed. This fact indicated that, this drug was rapidly absorbed and highly concentrated with a long duration of reservation in liver. All of these favours the schistosomicidal effect of the drug. As this drug was highly concentrated in the cytoplasm of liver cells, that might provide a pathophysiologic basis for the explanation of jaundice in the clinical ...

1985-05-01

99

An erythrocyte-specific DNA-binding factor recognizes a regulatory sequence common to all chicken globin genes

In order to understand the role of EGF in the development of human mammary epithelial tissue, we analysed the binding of /sup 125/I-EGF to sections of breast cancer biopsies. A mean specific /sup 125/I-EGF binding of 8.9 fmol per mg protein was estimated in thin sections of 17 breast cancer biopsies. Microautoradiographic analysis of /sup 125/I-EGF binding to the tissue sections was applied to demonstrate that EGF was bound predominantly to mammary epithelial cells. The binding was clearly correlated to the number of mitoses of mammary epithelial cells in the same samples. The highest EGF binding and proliferation rates were found in biopsies from breast cancer with axillary lymph-node metastases.

1987-03-15

100

Identification of a Novel Inhibitor of Coactivator-associated Arginine Methyltransferase 1 (CARM1)-mediated Methylation of Histone H3 Arg-17*

The authors have identified a protein present only in erythroid cells that binds to two adjacent sites within an enhancer region of the chicken {beta}-globin locus. Mutation of the sites, so that binding by the factor can no longer be detected in vitro, leads to a loss of enhancing ability, assayed by transient expression in primary erythrocytes. Binding sites for the erythroid-specific factor (Eryf1) are found within regulatory regions for all chicken globin genes. A strong Eryf1 binding site is also present within the enhancer of at least one human globin gene, and proteins from human erythroid cells (but not HeLa cells) bind to both the chicken and the human sites.

1988-08-01

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101

Chronic Cocaine-Induced H3 Acetylation and Transcriptional Activation of CaMKII? in the Nucleus Accumbens Is Critical for Motivation for Drug Reinforcement

Methylation of the arginine residues of histones by methyltransferases has important consequences for chromatin structure and gene regulation; however, the molecular mechanism(s) of methyltransferase...Full Text Available

2010-03-05

102

On-line partial discharge measurements and off-line dielectric spectroscopy measurements of six 115 kV XLPE cable systems

The regulation of gene expression in the brain reward regions is known to contribute to the pathogenesis and persistence of drug addiction. Increasing evidence suggests that the regulation of gene transcription...Full Text Available

2010-03-01

103

Understanding Enzyme Activity Using Single Molecule Tracking (Poster)

This paper reported on a study in which partial discharge (PD) measurements were performed on 6 underground transmission cable circuits to determine the effectiveness of PD measurements on fluid fill cables. The cables were between 37 and 56 years old. PD activity was detected from the terminations of H11L and H3L Cable 2. However, for cables from H3L Basin TS to Mill Street junction, PD activity was detected originating from within the main cable insulation.

2009-07-01

104

The human peripheral subunit-binding domain folds rapidly while overcoming repulsive Coulomb forces

This poster describes single-molecule tracking and total internal reflection fluorescence microscopy. It discusses whether the carbohydrate-binding module (CBM) moves on cellulose, how the CBM binds to cellulose, and the mechanism of cellulosome assembly.

2009-06-01

105

The ATP-Binding Cassette Transporter ABCA4: Structural and Functional Properties and Role in Retinal Disease

Peripheral subunit binding domains (PSBDs) are integral parts of large multienzyme complexes involved in carbohydrate metabolism. PSBDs facilitate shuttling of prosthetic groups between different catalytic...Full Text Available

2010-09-01

106

Strategies for the uses of lanthanide NMR shift probes in the determination of protein structure in solutio. Application to the EF calcium binding site of carp parvalbumin.

ATP-binding cassette transporters (ABC transporters) utilize the energy of ATP hydrolysis to translocate an unusually diverse set of substrates across cellular membranes. ABCA4, also known as...Full Text Available

2010-01-01

107

Serum protein binding and the role of increased alpha 1-acid glycoprotein in moderately obese male subjects.

The homologous sequences observed for many calcium binding proteins such as parvalbumin, troponin C, the myosin light chains, and calmodulin has lead to the hypothesis that these proteins have homologous...Full Text Available

1980-10-01

108

Semi-empirical formula for #LAMBDA#-binding energies in ground states of light hypernuclei

Serum protein and lipid concentrations as well as the serum protein binding of propranolol, diazepam and phenytoin were measured in normal weight and obese volunteers. Concentrations of alpha 1-acid...Full Text Available

1984-12-01

109

Role of serum carrier proteins in the peripheral metabolism and tissue distribution of thyroid hormones in familial dysalbuminemic hyperthyroxinemia and congenital elevation of thyroxine-binding globulin.

Starting with a #LAMBDA#-nucleus potential, a semi-empirical formula, which gives a fairly satisfactory account of the ground state #LAMBDA#-binding energy of light hypernuclei, if the very light nuclei are ignored has been obtained. (author).

110

Relative potencies for barbiturate binding to the Torpedo acetylcholine receptor.

To investigate the role of thyroxine-binding globulin (TBG) and albumin in the availability of thyroid hormones to peripheral tissues, comprehensive kinetic studies of thyroxine (T4) and triiodothyronine...Full Text Available

1987-08-01

111

Recurrent miscarriage and variant alleles of mannose binding lectin, tumour necrosis factor and lymphotoxin ? genes

1. The structural requirements of an allosteric barbiturate binding site on acetylcholine receptor-rich membranes isolated from Torpedo electroplaques have been characterized by the ability of fourteen...Full Text Available

1990-11-01

112

Receptor Binding Sites and Antigenic Epitopes on the Fiber Knob of Human Adenovirus Serotype 3

Variant alleles of the mannose binding lectin (MBL) gene are associated with increased susceptibility to infection and polymorphisms of tumour necrosis factor and lymphotoxin alpha genes (TNF, LTA)...Full Text Available

2001-12-01

113

Protein Damage by Reactive Electrophiles: Targets and Consequences

The adenovirus fiber knob causes the first step in the interaction of adenovirus with cell membrane receptors. To obtain information on the receptor binding site(s), the interaction of labeled cell...Full Text Available

1998-11-01

114

Plasma protein binding of phenytoin in 100 epileptic patients.

It has been sixty years since the Millers first described the covalent binding of carcinogens to tissue proteins. Protein covalent binding was gradually overshadowed by the emergence of DNA...Full Text Available

2008-01-01

115

Pharmacokinetics and protein binding of ceftriaxone during pregnancy.

The plasma protein binding of phenytoin was investigated in 100 epileptic patients, using equilibrium dialysis at 37 degrees C. The unbound fractions of phenytoin in plasma formed a skewed distribution,...Full Text Available

1982-08-01

116

Perceptual training narrows the temporal window of multisensory binding

The purpose of the present work was to study the pharmacokinetics and the protein binding (free fraction of the drug) of ceftriaxone (CTX) during pregnancy. Nine pregnant women (ages, 20 to 34 years)...Full Text Available

1993-01-01

117

Partial Characterization of Cadmium-Binding Protein from Roots of Tomato ¹

The brain’s ability to bind incoming auditory and visual stimuli depends critically on the temporal structure of this information. Specifically, there exists a temporal window of audiovisual...Full Text Available

2009-09-30

118

PAS Domain of the Aer Redox Sensor Requires C-Terminal Residues for Native-Fold Formation and Flavin Adenine Dinucleotide Binding

Cd-binding protein was extracted from tomato roots and purified on QAE-Sephadex A-25 and on Sephadex G-75 in 1 molar KCl buffer. The protein preparation was light brown and contained predominantly Cd...Full Text Available

1986-07-01

119

MultiRTA: A simple yet reliable method for predicting peptide binding affinities for multiple class II MHC allotypes

The Aer protein in Escherichia coli is a membrane-bound, FAD-containing aerotaxis and energy sensor that putatively monitors the redox state of the electron transport system. Binding...Full Text Available

2004-10-01

120

Mammalian end binding proteins control persistent microtubule growth

BackgroundThe binding of peptide fragments of antigens to class II MHC is a crucial step in initiating a helper T cell immune response. The identification of such peptide epitopes...Full Text Available

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121

Lectin Binding of the Major Polar Tube Protein (PTP1) and its Role in Invasion

End binding proteins (EBs) are highly conserved core components of microtubule plus-end tracking protein networks. Here we investigated the roles of the three mammalian EBs in controlling microtubule...Full Text Available

2009-03-09

122

Insertion of a Bulky Rhodium Complex into a DNA Cytosine-Cytosine Mismatch: An NMR Solution Study

... 2003)050[0600:LBOTMP]2.0.CO;2 Lectin Binding of the Major Polar Tube Protein (PTP1) ... PTP1. We, therefore, undertook a study ...

123

Increase in phorbol ester binding in liver microsomes after chronic administration of phenobarbital

The bulky octahedral complex, Rh(bpy)₂chrysi³⁺ (chrysi = 5, 6- chrysenequinone diimine), binds single base mismatches in a DNA duplex with micromolar binding affinities...Full Text Available

2007-10-10

124

Fluorine-19 NMR Chemical Shift Probes Molecular Binding to Lipid Membranes

The effect of chronic administration of phenobarbital on the binding of phorbol-12,13-dibutyrate (({sup 3}H)PDBu), an activator of protein kinase C (PKC), was examined in rat liver microsomes. A significant increase in the number of binding sites was observed in microsomes of Fisher 344 rats. However, no change appeared in liver cytosol binding of PDBu. Consequently, a translocation process of PKC is unlikely. The increase in ({sup 3}H)PDBu binding in liver microsomes is significant 24 h. after one injection of phenobarbital and reaches its maximum in 2 days. In other strains of rats (ACI and lean Zucker), significant differences were found in the increase of ({sup 3}H)PDBu binding in microsomes. Fisher 344 were the most sensitive, lean Zucker rats, the least sensitive. Those results parallel the pentoxy-resorufin O demethylase activity in the microsomes of the same animals. EC{sub ...

1991-03-15

125

Evidence that cell surface heparan sulfate is involved in the high affinity thrombin binding to cultured porcine aortic endothelial cells.

The binding of amphiphilic molecules to lipid bilayers is followed by ¹⁹F NMR using chemical shift and line shape differences between the solution and membrane-tethered states of...Full Text Available

2008-05-22

126

Ethylene Regulates Monomeric GTP-Binding Protein Gene Expression and Activity in Arabidopsis1

It has been postulated that thrombin binds to endothelial cells through, at least in part, cell surface glycosaminoglycans such as heparan sulfate, which could serve as antithrombin cofactor on the...Full Text Available

1985-04-01

127

Effect of Protein Binding on the Pharmacological Activity of Highly Bound Antibiotics?

Ethylene rapidly and transiently up-regulates the activity of several monomeric GTP-binding proteins (monomeric G proteins) in leaves of Arabidopsis as determined by two-dimensional gel electrophoresis...Full Text Available

2003-04-01

128

E2f binding-deficient Rb1 protein suppresses prostate tumor progression in vivo

During antibiotic drug development, media are frequently spiked with either serum/plasma or protein supplements to evaluate the effect of protein binding. Usually, previously reported serum or plasma...Full Text Available

2008-11-01

129

Determinants of the plasma protein binding of theophylline in health.

Mutational inactivation of the RB1 tumor suppressor gene initiates retinoblastoma and other human cancers. RB1 protein (pRb) restrains cell proliferation by binding...Full Text Available

2011-01-11

130

Comparative Structural Analysis of Lipid Binding START Domains

1 The plasma protein binding of theophylline was determined after addition of [14C]-theophylline (15 micrograms/ml) to plasma from 24 healthy drug-free volunteers and equilibrium dialysis for 2 h at...Full Text Available

1983-04-01

131

Cleavage of sterol regulatory element binding proteins (SREBPs) by CPP32 during apoptosis.

BackgroundSteroidogenic acute regulatory (StAR) protein related lipid transfer (START) domains are small globular modules that form a cavity where lipids and lipid hormones bind....Full Text Available

132

Cation Involvement in Telomestatin Binding to G-Quadruplex DNA

Cellular cholesterol homeostasis is controlled by sterol-regulated proteolysis of membrane-bound transcription factors called sterol-regulatory element binding proteins (SREBPs). CPP32, a cysteine protease,...Full Text Available

1996-03-01

133

Capture of genomic DNA on glass microscope slides

The binding mode of telomestatin to G-quadruplex DNA has been investigated using electrospray mass spectrometry, by detecting the intact complexes formed in ammonium acetate. The mass measurements show...Full Text Available

134

Biotin binders selected from a random peptide library expressed on phage.

It is well known that DNA strands bind to silica surfaces in the presence of high concentrations of chaotropic salts. We developed simple methods to evaluate binding and recovery of DNA on flat...Full Text Available

2007-06-15

135

Binding of a Fluorescent Lipid Amphiphile to Albumin and its Transfer to Lipid Bilayer Membranes

Recombinant biotin-binding phages were affinity-selected from a random peptide library expressed on the surface of filamentous phage. Phage binding to biotinylated proteins was half-maximally inhibited...Full Text Available

1993-08-01

136

Being a binding site: Characterizing residue composition of binding sites on proteins

Kinetics and thermodynamics of the binding of a fluorescent lipid amphiphile, Rhodamine Green™-tetradecylamide (RG-C_14:0), to bovine serum albumin were characterized in an equilibrium...Full Text Available

2003-01-01

137

Application of the PM6 semi-empirical method to modeling proteins enhances docking accuracy of AutoDock

The Protein Data Bank contains the description of more than 45,000 three-dimensional protein and nucleic-acid structures today. Started to exist as the computer-readable depository of crystallographic...Full Text Available

138

A global optimization algorithm for protein surface alignment

BackgroundMolecular docking methods are commonly used for predicting binding modes and energies of ligands to proteins. For accurate complex geometry and binding energy estimation,...Full Text Available

139

Uptake of Heavy Metal Ions by Water Dropwort (Oenanthe stolonifera DC.) and Identification of Its Heavy Metal-Binding Protein

BackgroundA relevant problem in drug design is the comparison and recognition of protein binding sites. Binding sites recognition is generally based on geometry often combined with...Full Text Available

140

Towards a realistic model of Fe-Cu-Fe spin valve systems using tight-binding methods

Full Text Available

1996-12-01

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141

The use of phenol-formaldehyde resin binding for sample preparation in activation analysis

Full text: Magnetic multilayer materials are becoming technologically important as they provide a more efficient means of magnetic reading and storage through utilisation of their giant magnetoresistance and oscillatory magnetic coupling. This study presents preliminary tight-binding calculations with a view of developing a consistent tight-binding model of `spin valve` Fe-Cu-Fe tri-layer materials. Further work involves using a self-consistent tight-binding approach to obtain a more accurate picture of this system and a better understanding of surface effects at the Fe-Cu interface 1 fig., 4 refs.

1996-12-31

142

Cholera toxin binding sites in yeast triggers biochemical pathway

(1974). Hungary Kolomiytsev, MA Dundua, V.Yu. Pachulia, NV Bagdavadze,

143

Binding of metal-"2"1"1At complexes to biomolecules - a new method of preparation of astatine radiopharmaceuticals

... e Biologia Molecular (SBBq), Sao Paulo, SP (Brazil) 217 p. APPLIED LIFE

1998-05-23

144

The effect of ethanol on "3"5-S-TBPS binding to mouse brain membranes in the presence of chloride

Page 1. RADIOCHEMISTRY, STABLE ISOTOPES, NUCLEAR ANALYTICAL

1991-11-01

145

Structural basis of binding of fluorescent, site-specific dansylated amino acids to human serum albumin

The effect of in vitro and in vivo administration of ethanol on the binding of "3"5S-t-butyl-bicyclophosphorothionate ("3"5S-TBPS) to cortical brain membranes of C57B1 mice was investigated using KCl (100 mM) containing assay media. The in vitro addition of ethanol produced a dose-dependent inhibition of basal "3"5S-TBPS binding. In the presence of chloride ions, GABA and pentobarbital had a biphasic action (stimulation followed by inhibition) on "3"5S-TBPS binding, whereas diazepam only stimulated the binding. Ethanol reduced the stimulatory effects of GABA and pentobarbital in a dose-dependent manner, but had no effect on the enhancement of "3"5S-TBPS binding produced by diazepam. "3"5S-TBPS binding to cortical brain membranes was inhibited by the putative Cl"- channel blocking agent DIDS. This inhibitory action of DIDS was significantly, and dose-dependently ...

146

Peculiarity of counterion - polyion interactions in aqueous solutions of copolymers of acrylamide with cadmium acrylate

Human serum albumin (HSA) has two primary binding sites for drug molecules. These sites selectively bind different dansylated amino acid compounds, which—due to their intrinsic fluorescence—have...Full Text Available

2011-04-01

147

A heteromeric complex containing the centromere binding factor 1 and two basic leucine zipper factors, Met4 and Met28, mediates the transcription activation of yeast sulfur metabolism.

Binding of Cd/sup 2 +/ ions in aqueous solutions of statistical copolymers of acrylamide with cadmium acrylate with different content of ionogenic groups in copolymers was investigated by polarography, conductometry, viscometry and dialysis. It is shown that the degree of binding of Cd/sup 2 +/ ions increases with increasing of the content of ionogenic groups in the copolymer and with decreasing of ionic strength of the solution. The values of the degree of binding of Cd/sup 2 +/ ions obtained by polarography and dialysis show satisfactory agreement.

1984-02-01

148

Functional domain analysis of glass, a zinc-finger-containing transcription factor in Drosophila.

Transcription activation of sulfur metabolism in yeast is dependent on two DNA binding factors, the centromere binding factor 1 (Cbf1) and Met4. While the role of Met4 was clearly established by showing...Full Text Available

1996-05-15

149

Low-level microwave irradiations affect central cholinergic activity in the rat

The glass gene is required for proper photo-receptor differentiation during development of the Drosophila eye glass codes for a DNA-binding protein containing five zinc fingers that we show is a transcriptional activator. A comparison of the sequences of the glass genes from two species of Drosophila and a detailed functional domain analysis of the Drosophila melanogaster glass gene reveal that both the DNA-binding domain and the transcriptional-activation domain are highly conserved between the two species. Analysis of the DNA-binding domain of glass indicates that the three carboxyl-terminal zinc fingers alone are necessary and sufficient for DNA binding. We also show that a deletion mutant of glass containing only the DNA-binding domain can behave in a dominant-negative manner both in vivo and in a cell culture assay that measures transcriptional activation. PMID:7604032

1995-07-01

150

Aging, tumor suppression and cancer: High-wire act!

Sodium-dependent high-affinity choline uptake was measured in various regions of the brains of rats irradiated for 45 min with either pulsed or continuous-wave low-level microwaves (2,450 MHz; power density, 1 mW/cm2; average whole-body specific absorption rate, 0.6 W/kg). Pulsed microwave irradiation (2-microseconds pulses, 500 pulses/s) decreased choline uptake in the hippocampus and frontal cortex but had no significant effect on the hypothalamus, striatum, and inferior colliculus. Pretreatment with a narcotic antagonist (naloxone or naltrexone; 1 mg/kg i.p.) blocked the effect of pulsed microwaves on hippocampal choline uptake but did not significantly alter the effect on the frontal cortex. Irradiation with continuous-wave microwaves did not significantly affect choline uptake in the hippocampus, striatum, and hypothalamus but decreased the uptake in the frontal cortex. The effect on the frontal cortex was not altered by pretreatment with narcotic ...

1987-01-01

151

Variation in the binding of /sup 125/I-labeled interferon-beta ser to cellular receptors during growth of human renal and bladder carcinoma cells in vitro

Evolutionary theory holds that aging is a consequence of the declining force of natural selection with age. We discuss here the evidence that among the causes of aging in complex multicellular organisms, such as mammals, is the antagonistically pleiotropic effects of the cellular responses that protect the organism from cancer. Cancer is relatively rare in young mammals, owing in large measure to the activity of tumor suppressor mechanisms. These mechanisms either protect the genome from damage and/or mutations, or they elicit cellular responses--apoptosis or senescence--that eliminate or prevent the proliferation of somatic cells at risk for neoplastic transformation.We focus here on the senescence response, reviewing its causes, regulation and effects. In addition, we describe recent data that support the idea that both senescence and apoptosis may indeed be the double-edged swords predicted by the evolutionary hypothesis of antagonistic ...

2004-08-15

152

Comparison of angiotensin II and SAR1, Ile8-AII binding to solubilized receptors in the bovine adrenal

Studies of various established human bladder and renal carcinoma cell lines cultured in vitro demonstrated the presence of specific, saturable, high affinity binding sites for /sup 125/I-labeled human interferon Beta ser IFN-beta ser). This recombinant produced interferon labeled with approximately one atom of /sup 125/I/molecule of IFN expressed minimal or no loss of antiviral activity. A single class of binding sites (1000-2000/cell) with an affinity constant of 10(10)-10(11) L/M was measured at 4 degrees C for cells exhibiting widely different sensitivity to the antiproliferative effect of IFN-beta ser. Major fluctuations in the binding of /sup 125/I-labeled IFN-beta ser to cellular receptors were observed during in vitro proliferation of four of five cell lines examined. A significant decrease (P less than 0.001) in specific binding was observed 48 h after cultures were established. Cell cycle ...

1987-09-01

153

Identification of proteins important for tetracycline (TC) binding to ribosomes by single protein omission reconstitution (SPORE) experiments

Derivatives of angiotensin with a sarcosine substitution at the carboxy terminus and an aliphatic amino acid substitution at the amino terminus have been shown to be competitive ligands for the angiotensin receptor. Scatchard plots derived from saturation isotherm data in bovine adrenal particulates consistently demonstrate three to five times the number of binding sites for "1"2"5I-Sarl,Ile8-AII ("1"2"5I-SI-AII) than for "1"2"5I-AII in experiments in which the two ligands are run side-by-side. A significant difference between "1"2"5I-AII and "1"2"5I-SI-AII binding to detergent solubilized angiotensin receptors was observed. Of the "1"2"5I-AII binding sites, about 85-90% were recovered upon solubilization. In contrast, the recovery of "1"2"5I-SI-AII binding sites was only 4-5%. To determine whether binding sites labeled in the soluble state represent biologically significant AII ...

1986-04-13

154

Competition by inhibitory oligonucleotides prevents binding of CpG to C-terminal TLR9

TC inhibits protein synthesis in E. coli by interfering with aminoacyl-tRNA binding to the ribosomal A site, and there is strong evidence that such inhibition results from TC binding to a high affinity site on the 30S subunit. The SPORE approach has been used to define those 30S proteins that are potentially important for high affinity TC binding, measured as the (/sup 3/H)-TC co-sedimenting with the reconstitution particle through a sucrose density gradient. Reverse phase-HPLC has been used both to prepare ribosomal proteins and to analyze the protein content of reconstituted particles. The results obtained so far show that protein S7, as well as some proteins linked to S7 in the 30S assembly map, are important for TC binding, whereas other ribosomal proteins are not. These results are in very good accord with their earlier photoaffinity labeling studies that strongly implicated S7 as forming part of ...

1987-05-01

155

British Library Electronic Table of Contents (United Kingdom)

Abstract TLR9 recognizes unmethylated CpG-containing DNA commonly found in bacteria. Synthetic oligonucleotides containing CpG-motifs (CpG ODNs) recapitulate the activation of TLR9 by microbial DNA, whereas inversion of the CG dinucleotide within the CpG motif to GC (GpC ODNs) renders such ODNs inactive. This difference cannot be attributed to binding of ODNs to the full-length TLR9 ectodomain, as both CpG and GpC ODNs bind comparably. Activation of murine TLR9 requires cleavage into an active C-terminal fragment, which binds CpG robustly. We therefore compared the ability of CpG and GpC ODNs to bind to full-length and C-terminal TLR9, and their impact on the cleavage of TLR9. We found that CpG binds better to C-terminal TLR9 when compared with GpC, despite comparably low binding of both O...

2011-01-01

156

Prosocial effects of nicotine and ethanol in adolescent rats through partially dissociable neurobehavioral mechanisms

Third phase formation in the extraction of phosphotungstic acid by TBP in n-octane

The widespread use of tobacco and alcohol among adolescents might be related to the ability of nicotine and ethanol to facilitate social interactions. To investigate the neurobehavioral mechanisms underlying the prosocial effects of nicotine and ethanol, we focused on social play behavior, the most characteristic social activity in adolescent rats. Social play behavior is rewarding, and it is modulated through opioid, cannabinoid and dopaminergic neurotransmission, which are also involved in the reinforcing properties of nicotine and ethanol. We found that nicotine and ethanol increased social play, without affecting locomotion or social exploration. Their effects depended on the level of social activity of the partner, and were comparable in familiar and unfamiliar environments. At doses that increased social play, nicotine and ethanol had no anxiolytic effects in the elevated plus-maze. By contrast, the prototypical anxiolytic drug diazepam reduced social play at doses that reduced ...

2009-08-05

157

Probing the H"3 vertex in e"+e"-, #gamma#e, and #gamma##gamma# collisions for light and intermediate Higgs bosons

The solvent extraction of 12-phosphotungstic acid, also known as 12-tungstophosphoric acid-H_3PW_1_2O_4_0, the so-called Keggin heteropolyacid - by 0.73 M (20%v/v) tri-n-butyl phosphate (TBP) in n-octane under conditions comparable to those used previously for the extraction of conventional inorganic mineral acids is described. A simplified phase diagram for the pentanary system comprised of H_3PW_1_2O_4_0, HNO_3, H_2O, TBP, and n-octane reveals an extremely low initial concentration of H_3PW_1_2O_4_0 (1.1 mM) at the LOC (limiting organic concentration) condition, far lower than the most effective third-phase-forming inorganic acid, namely HClO_4. The results from small-angle neutron scattering (SANS) indicate that the interparticle attraction energy - U(r) calculated through application of the Baxter sticky sphere model to the SANS data at the LOC condition - ...

2010-08-30

158

Molar extinction coefficients of some fatty acids

We study double Higgs boson production at future linear colliders while paying special attention to the option of high-energy and high-luminosity photon beams. The main purpose is to examine the feasibility of e"+e"-, #gamma#e, and #gamma##gamma# colliders in order to establish bounds on the value of triple Higgs coupling, which could be crucial for understanding a spontaneous breaking mechanism. We consider mainly those cases of light and intermediate Higgs bosons, including an analysis of the electroweak backgrounds. The mass range M_H#approx#M_Z is discussed separately. It is shown that for a light Higgs boson the H"3 coupling can be visible, even at a future linear e"+e"- collider at 500 GeV. For an intermediate Higgs boson, a collider with TeV energies is suitable for investigations. We estimate the bounds on the anomalous H"3 coupling which can be experimentally established at future linear ...

159

Electrochemical and conversion electron Moessbauer study of corrosion induced by acid rain

The attenuation of gamma rays in some fatty acids, viz. formic acid (CH_2O_2), acetic acid (C_2H_4O_2), propionic acid (C_3H_6O_2), butyric acid (C_4H_8O_2), n-hexanoic acid (C_6H_1_2O_2), n-caprylic acid (C_8H_1_6O_2), lauric acid (C_1_2H_2_4O_2), myristic acid (C_1_4H_2_8O_2), palmitic acid (C_1_6H_3_2O_2), oleic acid (C_1_8H_3_4O_2) and stearic acid (C_1_8H_3_6O_2), has been measured at the photon energies 81, 356, 511, 662, 1173 and 1332 keV. Experimental values for the molar extinction coefficient, the effective atomic number and the electron density have been derived and compared with theoretical calculations. There is good agreement between experiment and theory.

2002-10-01

160

A study of electrochemically-induced corrosion of low carbon steel in a medium modelling acid rain

The passivation of low carbon steel was studied in aqueous solution of 0.5M Na[sub 2]SO[sub 4]+0.001M NaHSO[sub 3] (pH 3.5, 6.5 and 8.5) which can be considered as a model of acid rain. The used conversion electron Moessbauer spectroscopy (CEMS) with the complementary electrochemical investigations proved that the sulfite ions induce pitting corrosion at pH 3.5 and 6.5, while the measurements showed much weaker pitting at pH 8.5. The compositions and thicknesses of the passive films formed during the electrochemical treatments are determined from the CEM spectra. Only [gamma]-FeOOH was found on the surface of the samples at pH 6.5 and 8.5. Nevertheless, at pH 3.5 the sextet belonging to Fe[sub 3]C appears in the spectra, and also FeSO[sub 4].H[sub 2]O could be detected in low concentration. (orig.).

1993-04-01

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161

A novel photodiode made of hybrid organic/inorganic nanocomposite

Complementary electrochemical, spectrophotometric and electron microsopic investigations were made in addition to the conversion electron Moessbauer spectroscopic (CEMS) measurements to learn more about the mechanism of corrosion of low carbon steel samples in aqueous sulfate and sulfite containing sulfate solutions (pH 3.5, 6.5 and 8.5). Passivation of iron in pure sulfate solution was studied in detail in earlier papers. In the present work, we used a solution containing both sulfate and sulfite anions to obtain more information about the effect of acid rain on low carbon steel samples. The compositions and thicknesses of the passive films formed due to the electrochemical treatments were determined from the CEM spectra. [gamma]-FeOOH was found in each case on the surface of the samples; nevertheless, at pH 3.5 the sextet belonging to Fe[sub 3]C appears in the CEM spectra, and also FeSO[sub 4] . H[sub ...

1994-11-01

162

Radioiodination of chicken luteinizing hormone without affecting receptor binding potency

Novel hybrid organic/inorganic nanocomposites made of metal oxide and conjugated polymer nanocomposite and its application in bulk-heterojunction solar cells were studied. The composite was composed of different concentrations of strontium titanate (SrTiO_3) and polyaniline doped phosphoric acid. The optimum concentration of strontium titanate was found to be 0.2 v/v. An inorganic-organic photovoltaic device with a structure of Ag/Pani-H_3PO_4-SrTiO_3/Al has been fabricated. The ideality factor value of the diode was found to be 1.8. This n value of the diode implies a deviation from ideal junction behaviour. The barrier height #phi#_b value for the diode was found to be 0.56 eV. The Ag/Pani-H_3PO_4-SrTiO_3/Al diode shows a photovoltaic behaviour with a maximum open-circuit voltage V_o_c of 2.49 V, and short-circuit current I_s_c of 5.6 mA under light illumination #lambda# = 460 nm. The conversion ...

2009-08-07

163

Protein binding assay for hyaluronate

By improving the currently used lactoperoxidase method, we were able to obtain radioiodinated chicken luteinizing hormone (LH) that shows high specific binding and low nonspecific binding to a crude plasma membrane fraction of testicular cells of the domestic fowl and the Japanese quail, and to the ovarian granulosa cells of the Japanese quail. The change we made from the original method consisted of (1) using chicken LH for radioiodination that was not only highly purified but also retained a high receptor binding potency; (2) controlling the level of incorporation of radioiodine into chicken LH molecules by employing a short reaction time and low temperature; and (3) fractionating radioiodinated chicken LH further by gel filtration using high-performance liquid chromatography. Specific radioactivity of the final {sup 125}I-labeled chicken LH preparation was 14 microCi/micrograms. When specific binding ...

1989-12-01

164

Mechanism of adenylate kinase. Dose adenosine 5'-triphosphate bind to the adenosine 5'-monophosphate site

A relatively quick and simple assay for hyaluronate was developed using the specific binding protein, hyaluronectin. The hyaluronectin was obtained by homogenizing the brains of Sprague-Dawley rats, and then centrifuging the homogenate. The resulting supernatant was used as a source of crude hyaluronectin. In the binding assay, the hyaluronectin was mixed with (/sup 3/H)hyaluronate, followed by an equal volume of saturated (NH/sub 4/)/sub 2/SO/sub 4/, which precipitated the hyaluronectin and any (/sup 3/H)hyaluronate associated with it, but left free (/sup 3/H)hyaluronate in solution. The mixture was then centrifuged, and the amount of bound (/sup 3/H)hyaluronate in the precipitate was determined. Using this assay, the authors found that hyaluronectin specifically bound hyaluronate, since other glycosaminoglycans failed to compete for the binding protein. In addition, the interaction between hyaluronectin and hyaluronate ...

1986-11-01

165

Interaction of thyroid hormone and hemoglobin: nature of the interaction and effect of hemoglobin on thyroid hormone radioimmunoassay

Although the subtrate binding properties of adenylate kinase (AK) have been studied extensively by various biochemical and biophysical techniques, it remains controversial whether uncomplexed adenosine 5'-triphosphate (ATP) binds to the adenosine 5'-monophosphate (AMP) site of AK. The authors present two sets of experiments which argue against binding of ATP to the AMP site. (a) /sup 31/P nuclear magnetic resonance titration of ATP with AK indicated a 1:1 stoichiometry on the basis of changes in coupling constants and line widths. This ruled out binding of ATP to both sites. (b) ATP and MgATP were found to behave similarly by protecting AK from spontaneous inactivation while AMP showed only a small degree of protection. Such inactivation could also be protected or reversed by dithioerythritol and is most likely due to oxidation of sulfhydryl groups, one of which (cysteine-25) is ...

1987-10-06

166

Analysis of the roles of E6 binding to E6TP1 and nuclear localization in the human papillomavirus type 31 life cycle

Gel filtration of human erythrocyte (RBC) lysate incubated with labeled thyroxine (Tu) or triiodothyronine (Tt) revealed co-elution of a major iodothyronine-binding fraction (R-2) and hemoglobin. Solutions of purified human hemoglobin and Tt also showed co-elution of hormone and hemoglobin. Because hematin and protoporphyrin were shown to bind labeled Tt, the oxygen-binding site on hemoglobin was excluded as the site of iodothyronine-hemoglobin interaction. Analysis of hormone binding by heme and globin moieties showed Tt binding to be limited to the heme fraction. Addition of excess unlabeled Tt to hemoglobin or heme incubated with labeled Tt indicated 75% to 90% of hormone binding was poorly dissociable. These observations suggested that the presence of hemoglobin in RBC lysate or in serum could influence the measurement of Tu and Tt by specific ...

167

British Library Electronic Table of Contents (United Kingdom)

The E6 oncoproteins of high-risk human papillomaviruses provide important functions not only for malignant transformation but also in the productive viral life cycle. E6 proteins have been shown to bind to a number of cellular factors, but only a limited number of analyses have investigated the effects of these interactions on the viral life cycle. In this study, we investigated the consequences of HPV 31 E6 binding to E6TP1, a putative Rap1 GAP protein. HPV 16 E6 has been shown to bind as well as induce the rapid turnover of E6TP1, and similar effects were observed with HPV 31 E6. Mutation of amino acid 128 in HPV 31 E6 was found to abrogate the ability to bind and degrade E6TP1 but did not alter binding to another ?-helical domain protein, E6AP. When HPV 31 genomes containing mutations a...

2007-01-01

168

Molecular dynamics simulations of aqueous ionic clusters using polarizable water

The structure of receptor-associated protein (RAP)

The solvation properties of a chlorine ion in small water clusters are investigated using state-of-the-art statistical mechanics. The simulations employ the polarizable water model developed recently by Dang [J. Chem. Phys. [bold 97], 2659 (1992)]. The ion--water interaction potentials are defined such that the successive binding energies for the ionic clusters, and the solvation enthalpy, bulk vertical binding energy, and structural properties of the aqueous solution agree with the best available results obtained from experiments. Simulated vertical electron binding energies of the ionic clusters Cl[sup [minus

1993-11-01

169

Surface oxidation of Co2+ and its dependence on ligand coordination number in silica polyamine composites

The receptor-associated protein (RAP) is a molecular chaperone that binds tightly to certain newly synthesized LDL receptor family members in the endoplasmic reticulum (ER) and facilitates their delivery...Full Text Available

2007-08-01

170

British Library Electronic Table of Contents (United Kingdom)

Coordination of CoCl2 solutions to the silica polyamine composite, WP-1, made with the branched polymer polyethylenimine (PEI) shows irreversible binding resulting from surface oxidation of the Co2+-Co3+. This is not the case for the silica polyamine composite BP-1 made with the linear polymer polyallylamine where reversible binding and no oxidation is observed. These observations suggested that oxidation of the cobalt was related to the greater coordination number available with the branched polyamine relative to the linear polyamine. A study of the kinetics of cobalt binding to WP-1 indicated initial loading of Co2+ at relatively low coordination number followed by desorption of Co2+ leading to oxidation and irreversible binding. Exclusion of oxygen from the composite-cobalt solution mix...

2010-01-01

171

Structure and Characterization of Nicotinic Acetylcholine ...

Structural alterations in the seminiferous tubules of rats treated with immunosuppressor tacrolimus

... the ct-neurotoxin from Dendroaspis viridis venom (a-DTX) , which binds to four sites on the AcChR molecule (Conti-Tronconi & Raftery 1986). ...

1991-11-07

172

Some ABCA3 mutations elevate ER stress and initiate apoptosis of lung epithelial cells

BackgroundTacrolimus (FK-506) is an immunosuppressant that binds to a specific immunophilin, resulting in the suppression of the cellular immune response during transplant rejection....Full Text Available

173

Mutations in RNA Binding Protein Gene Cause Familial Dilated Cardiomyopathy

BackgroundABCA3 transporter (ATP-binding cassette transporter of the A subfamily) is localized to the limiting...Full Text Available

2011-01-01

174

Heparin binding sites on Ross River virus revealed by electron cryo-microscopy

ObjectivesWe sought to identify a novel gene for dilated cardiomyopathy (DCM).BackgroundDCM is a heritable, genetically...Full Text Available

2009-09-01

175

Energy level schemes and binding energies for nuclei in the region of 140

Cell surface glycosaminoglycans play important roles in cell adhesion and viral entry. Laboratory strains of two alphaviruses, Sindbis and Semliki Forest virus, have been shown to utilize heparan sulfate as an attachment receptor, whereas Ross River virus (RRV) does not significantly interact with it. However, a single amino acid substitution at residue 218 in the RRV E2 glycoprotein adapts the virus to heparan sulfate binding and expands the host range of the virus into chicken embryo fibroblasts. Structures of the RRV mutant, E2 N218R, and its complex with heparin were determined through the use of electron cryo-microscopy and image reconstruction methods. Heparin was found to bind at the distal end of the RRV spikes, in a region of the E2 glycoprotein that has been previously implicated in cell-receptor recognition and antibody binding.

2005-02-20

176

Effect of radioiodine on hyaluronate-binding activity during prenatal rat brain development

Russian 1987. p. 99-100. USSR Sabalyauskas, L.Yu. Vanagas, VV Guseva,

1987-04-14

177

Development of Methods for Obtaining Position Image and Chemical Binding Information from Flow Experiments of Porous Media

Russian 1997 p. 263-264 Russian Federation Tkach, VL Ushakova, GA

178

Dependence of impurity binding energy on nitrogen and indium concentrations for shallow donors in a GaInNAs/GaAs quantum well under intense laser field

Existing oil reservoirs might be more fully exploited if the properties of the flow of oil and water in porous media were better known. In laboratory experiments it is important to collect as much information as possible to make a descriptive model of the system, including position imaging and chemical binding information. This thesis develops nuclear methods for obtaining position image and chemical binding information from flow experiments of porous media. A combined positron emission tomography and single photon emission computed tomography system to obtain position images, and a time-differential perturbed angular correlation system to obtain chemical binding information, have been built and thoroughly tested. 68 refs., 123 figs., 14 tabs.

1998-12-01

179

British Library Electronic Table of Contents (United Kingdom)

Within the framework of the effective-mass approximation, using a variational method, we have calculated the effect of intense laser radiation on the binding energy of the shallow-donor impurities in a Ga1- x In x N y As1- y /GaAs single quantum well for different nitrogen and indium mole concentrations. Our numerical results show that the binding energy strongly depends on the laser intensity and frequency (via the laser dressing parameter) and it also depends on the nitrogen and indium concentrations. Impurity binding energy under intense laser fields can be tuned by changing the nitrogen and indium mole fraction.

2011-01-01

180

Characterization of lymphocyte receptors for glycosaminoglycans.

Carbohydrate-specified endocytosis: localization of ligand in the lysosomal compartment.

This paper describes attempts to isolate and characterize glycosaminoglycan (GAG)-binding molecules on the surface of lymphocytes and lymphoma cell lines and relate their expression to splenic and lymph...Full Text Available

1991-02-01

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181

BzpF is a CREB-like transcription factor that regulates spore maturation and stability in Dictyostelium

Carbohydrate-directed endocytosis is mediated by a receptor, the hepatic binding protein; it is responsible for the clearance of galactose-terminated glycoproteins from the circulation. This process...Full Text Available

1981-11-01

182

British Library Electronic Table of Contents (United Kingdom)

The cAMP response element-binding protein (CREB) is a highly conserved transcription factor that integrates signaling through the cAMP-dependent protein kinase A (PKA) in many eukaryotes. PKA plays a critical role in Dictyostelium development but no CREB homologue has been identified in this system. Here we show that Dictyostelium utilizes a CREB-like protein, BzpF, to integrate PKA signaling during late development. bzpF^- mutants produce compromised spores, which are extremely unstable and germination defective. Previously, we have found that BzpF binds the canonical CRE motif in vitro. In this paper, we determined the DNA binding specificity of BzpF using protein binding microarray (PBM) and showed that the motif with the highest specificity is a CRE-like sequence. BzpF is necessary to ...

2011-01-01

183

Biosorption of heavy metal ions on Rhodobacter sphaeroides and Alcaligenes eutrophus H16

Acetylcholine Receptor Binding Characteristics of Snake and ...

A fundamental study of the application of bacteria to the recovery of toxic heavy metals from aqueous environments was carried out. The biosorption characteristics of cadmium and lead ions were determined with purple nonsulfur bacteria, Rhodobacter sphaeroides and hydrogen bacteria, Alcaligenes eutrophus H16 that were inactivated by steam sterilization. A simplified version of the metal binding model proposed by Plette et al. was used for the description of meal binding data. The results showed that the biosorption of bivalent metal ions to whole cell bodies of the bacteria was due to monodentate binding to two different types of acidic sites: carboxilic and phosphatic-type sites. The number of metal binding sites of A. eutrophus was 2.4-fold larger than that of R. sphaeroides.

1998-01-15

184

... Naja oxiana neurotoxin 1, Bungarus multicinctus or-bungarotoxin) and short-chain group (Naja naja atra cobrotoxin, Naja oxiana neurotoxin 11. ...

2011-05-13

185

m0307466.imq

The Trithorax group protein Lid is a trimethyl histone H3K4 demethylase required for dMyc-induced cell growth

7&vO BoXl &&td b?f09 `B"Bc ,.q~ G$)ED$O/ Kbwj6rNd CB7"l& KSeU jt#C G"U#V f*,njThh J$,H 3 R!!Z!"" +Jqf el\\V& bb?q~n dS:{ OX[1 HZxR j.$Cs 0B? ...

186

The Myc oncoprotein is a potent inducer of cell growth, cell cycle progression, and apoptosis. While many direct Myc target genes have been identified, the molecular determinants of Myc’s transcriptional...Full Text Available

2007-03-01

187

Sinterable powders

Novel inorganic hydrogen-bonded crystals with nonlinear optical properties

A description is given of sinterable powders and methods of producing sintered products using such powders. The powders consist of (a) a particulate ceramic material, e.g. SiC, having specified particle size and surface area; (b) a carbon source material, e.g. sugar or a phenol-formaldehyde resin; and (c) a residue from a solution of H3BO3, B2O3, or mixtures of these as sintering aid. (U.K.).

188

Direct interband dipole-transition selection rules for the O/sub h//sup 3/ space-group compounds

Four inorganic hydrogen-bonded crystals with second-order nonlinear properties have been discovered: K_4LiH_3(SO_4)_4, Na_2SeO_4#centre dot#H_2SeO_3#centre dot#H_2O, Cs_1_,_5Li_1_,_5H(SO_4)_2 and NH_4HSeO_4. (author)

2000-01-01

189

Reduction of cadmium toxicity to green microalga Stichococcus bacillaris by manganese

The irreducible representations associated with states of dipole symmetry have been calculated for the space groups O/sub h//sup 3/, the space group with the correct symmetry for A-15 phase compounds. Also assembled are the character tables of the O/sub h/3 group. Thus all thedirect interband dipole-transition selection rules for A-15 compounds can easily be determined.

1983-07-01

190

Histone deacetylase inhibitors and transforming growth factor-b induce 15-hydroxyprostaglandin dehydrogenase expression in human lung adenocarcinoma cells

Investigations of cadmium toxicity to microorganisms are now more concerned with the interactions of cadmium with different environmental factors and other metals. The interactions are complex and have not been thoroughly studied yet. Metal interactions may assume the form of synergism characterized by increase in toxicity, but also of antagonism in which one metal reduces the toxicity of another. Apart from cadmium interactions with such toxic metals as mercury and lead, interactions of cadmium with the essential trace elements seem to be very interesting because it has been assumed that algal cells take up cadmium by the system transporting these elements. A previous study showed that cadmium transport into Stichococcus bacillaris cells was inhibited by Mn/sup 2 +/ ions. Thus, it can be supported that there exist some possibilities of using those ions antagonistic to cadmium as counterposition. Showing those possibilities was the aim of the present paper.

1988-12-01

191

British Library Electronic Table of Contents (United Kingdom)

Histone deacetylase (HDAC) inhibitors have been actively exploited as potential anticancer agents. To identify gene targets of HDAC inhibitors, we found that HDAC inhibitors such as sodium butyrate, scriptaid, apicidin and oxamflatin induced the expression of 15-hydroxyprostaglandin dehydrogenase (15-PGDH), a potential cyclooxygenase-2 (COX-2) antagonist and tumor suppressor, in a time and concentration dependent manner in A549 and H1435 lung adenocarcinoma cells. Detailed analyses indicated that HDAC inhibitors activated the 15-PGDH promoter-luciferase reporter construct in transfected A549 cells. A representative HDAC inhibitor, scriptaid, and its negative structural analog control, nullscript, were further evaluated at the chromatin level. Scriptaid but not nullscript induced a signific...

2006-01-01

192

Environmental analysis of endocrine disrupting effects from hydrocarbon contaminants in the ecosystem. 1997 annual progress report

Endophytic fungus Trichothecium roseum LZ93 antagonizing pathogenic fungi in vitro and its secondary metabolites

'The overall objective of the basic research grant is to characterize the potential of common hydrocarbon contaminants in ecosystems to act as endocrine disruptors. The three major lines of research include (1) a biotechnology based screening system to identify potential hormone mimics and antagonists; (2) an animal screening system to identify biomarkers of endocrine effects. and (3) a literature review to identify compounds at a variety of DOE sites that need to be examined for endocrine disrupting effects. By relating results obtained from this research project to contamination problems at various DOE sites. CBR will provide data and information on endocrine disrupting contaminants to DOE for consideration in risk analyses for determining clean-up levels and priorities needed at the sites.'

1997-01-01

193

British Library Electronic Table of Contents (United Kingdom)

The endophytic fungus Trichothecium roseum LZ93 from Maytenus hookeri was found to antagonize other pathogenic fungi in vitro. To identify which compound contributed substantially to the antagonism, we fermented the strain and purified its fermentation products. Eleven compounds were obtained, including two trichothecenes, five rosenonolactones, two cardiotonic cyclodepsipeptides, and two sterols. Compound 11?-hydroxyrosenonolactone (1) was assigned according to 1D and 2D-NMR data for the first time. At the same time, the 1H and 13C-NMR assignments for 6?-hydroxyrosenonolactone (2) were revised. Of all of them, only trichothecin (6) showed strong antifungal activity. Based on our observations of the antagonistic activity and the other experimental results, we suggest that the antifungal co...

2010-01-01

194

Development of a detailed kinetic model for gasoline surrogate fuels

Capsaicin-induced avoidance behavior in the terrestrial Gastropoda Megalobulimus abbreviatus: Evidence for TRPV-1 signaling and opioid modulation in response to chemical noxious stimuli

A detailed chemical kinetic model to describe the autoignition of gasoline surrogate fuels is presented consisting of the fuels iso-octane, n-heptane, toluene, diisobutylene and ethanol. Model predictions have been compared with shock tube ignition delay time data for surrogates of gasoline over practical ranges of temperature and pressure, and the model has been found to be sensitive to both changes in temperature and pressure. Moreover, the model can qualitatively predict the observed synergistic and antagonistic non-linear blending behaviour in motor octane number (MON) for different combinations of primary reference fuels (PRFs) and non-PRFs by correlating calculated autoignition delay times from peak pressures and temperatures in the MON test to experimental MON values. The reasons for the blending behaviour are interpreted in terms autoignition chemistry. 37 refs., 11 figs., 4 tabs.

2008-08-15

195

British Library Electronic Table of Contents (United Kingdom)

The aim of this study was to measure the nociceptive response (avoidance latency) of the land snail Megalobulimus abbreviatus (N=8 in each group) after topical capsaicin exposure (0.1% and 0.5% in 20% ethanol) and to compare it to a well-studied stressful (50??C) thermal stimulus model. We also tested if ruthenium red, and capsazepine, respectively nonselective and selective TRPV1 receptor antagonists, could modify both capsaicin- and thermal-evoked responses. Finally, animals were pretreated with morphine, naloxone or morphine plus naloxone prior to capsaicin stimuli. Latencies were measured when the animal lifted its head?foot complex 1?cm from the substrate. Data were compared using ANOVA and LSD post hoc, and the Student T Test (pM. abbreviatus.

2007-01-01

196

Afferent mechanisms of microwave-induced biological effects. Annual report, 1 June 1985-31 May 1986

Synthesis of /sup 14/C-labeled 10,11-epoxyfarnesyl diazoacetate, a potential photoaffinity labeling reagent for insect juvenile hormone binding proteins

Effects of 2450-MHz circularly polarized microwave irradiation on central nervous system functions were studied. Pulsed (microsecond, 500 pps) microwaves decreased high-affinity sodium-dependent choline uptake in the hippocampus and frontal cortex of the rat. The effect on hippocampal choline uptake was blocked by pretreatment with narcotic antagonists. Continuous-wave microwaves of the same power density decreased choline uptake in the frontal cortex only. Furthermore, it was found that the effects of pulsed microwaves on central cholinergic activity are classically conditionable to cues in the exposure environment. The hypothesis that some of the neurological effects of pulsed microwave irradiation are caused by its effect on the auditory system was investigated. Effects of pink noise and pulsed microwaves were compared.

1986-07-01

197

Specific Sequence Motif of 8-Cys Repeats of TGF-? Binding Proteins, LTBPs, Creates a Hydrophobic Interaction Surface for Binding of Small Latent TGF-?

The synthesis of (/sup 14/C)-10,11-Epoxy-(2E,6E)-farnesyl diazoacetate in one vessel, starting from (/sup 14/C)-glyoxylic acid, is described. This compound is useful as a potential photoaffinity labeling agent for juvenile hormone binding sites.

1982-04-01

198

Quantitative pharmacological analysis of 2-125I-iodomelatonin binding sites in discrete areas of the chicken brain

Transforming growth factor (TGF)-βs are secreted in large latent complexes consisting of TGF-β, its N-terminal latency-associated peptide (LAP) propeptide, and latent TGF-β...Full Text Available

2000-08-01

199

Polyunsaturated Fatty Acids Selectively Suppress Sterol Regulatory Element-binding Protein-1 through Proteolytic Processing and Autoloop Regulatory Circuit*

The authors have localized and characterized 2-125I-iodomelatonin binding sites in the chicken brain using in vitro quantitative autoradiography. Binding sites were widely distributed throughout the chicken brain, predominantly in regions associated with the visual system. The specific binding of 2-125I-iodomelatonin to discrete chicken brain areas was found to be saturable, reversible, and of high affinity. The specific binding of 2-125I-iodomelatonin (75 pm) was quantitated for 40 identifiable brain regions. Eight brain regions were chosen for binding characterization and pharmacological analysis: optic tectum, Edinger-Westphal nucleus, oculomotor nucleus, nucleus rotundus, ventral supraoptic decussation, ventrolateral geniculate nucleus, neostriatum, and ectostriatum. These regions showed no rostral-caudal gradient in 2-125I-iodomelatonin specific binding, ...

1991-09-01

200

New mechanism for methicillin resistance in Staphylococcus aureus: clinical isolates that lack the PBP 2a gene and contain normal penicillin-binding proteins with modified penicillin-binding capacity.

Sterol regulatory element-binding protein (SREBP)-1 is a key transcription factor for the regulation of lipogenic enzyme genes in the liver. Polyunsaturated fatty acids (PUFA) selectively suppress hepatic...Full Text Available

2010-04-09

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201

Nature of the short-range interaction between noble gas atoms and metal surfaces

Seventeen clinical isolates of Staphylococcus aureus (from the United States and Europe) selected for low (borderline)-level methicillin resistance (MIC of methicillin, 2 to 4 micrograms/ml; MIC of...Full Text Available

1989-11-01

202

NMR of a synthetic peptide spanning the triphosphate binding site of adenosine 5'-triphosphate in actin

I propose that an interpretation of the interaction of noble gas atoms with metal surfaces as predominantly physisorbing provides the best explanation for the systematics of their binding energies and surface dipoles, as well as for the tendency of noble gas atoms to bind in low coordinated sites. In the present context physisorption is defined as a process driven by the overlap of the electrostatic atomic potentials of the interacting species. (orig.)

2007-06-15

203

Mice With a Deletion in the Gene for CCAAT/Enhancer-Binding Protein ? are Protected Against Diet-Induced Obesity

The amino acid residues 114-118 in actin were found to be implicated strongly in the binding of nucleotide, and as would be expected for such an important binding site, they are located in a completely conserved region of the actin sequence. A 19-residue peptide with the actin sequence 106-124 was synthesized in order to span the putative triphosphate binding site. Proton NMR spectra of the actin peptide 114-118 in the presence and absence of ATP indicated that Arg-116 and Lys-118 are particularly involved in binding ATP. A strong binding of ATP to the peptide 106-124 also was measured. Tripolyphosphate bound to the peptide 106-124 somewhat more weakly than ATP. Binding involved residues 115-118 and 121-124, indicating the presence of a reverse turn between these segments. Proton resonances were assigned by using two-dimensional double quantum correlated ...

1987-03-10

204

Interaction of Extracellular Domain 2 of the Human Retina-specific ATP-binding Cassette Transporter (ABCA4) with All-trans-retinal*

The CCAAT/enhancer-binding protein β (C/EBPβ) is required for adipocyte differentiation and maturation. We have studied the role of the transcription factor, C/EBPβ,...Full Text Available

2007-01-01

205

Influence of the high-affinity growth hormone (GH)-binding protein on plasma profiles of free and bound GH and on the apparent half-life of GH. Modeling analysis and clinical applications.

The retina-specific ATP-binding cassette (ABC) transporter, ABCA4, is essential for transport of all-trans-retinal from the rod outer segment discs in the retina and is associated with...Full Text Available

2010-06-18

206

High-affinity lead binding proteins in rat kidney cytosol mediate cell-free nuclear translocation of lead

The discovery of a specific high-affinity growth hormone (GH) binding protein (GH-BP) in plasma adds complexity to the dynamics of GH secretion and clearance. Intuitive predictions are that such a protein...Full Text Available

1993-02-01

207

High-affinity lead binding proteins in rat kidney cytosol mediate cell-free nuclear translocation of lead

The PbII binding characteristics of the previously reported PbII binding proteins of rat kidney cytosol were investigated further. Saturation and Scatchard analysis of /sup 203/Pb binding in whole cytosol and in 40% saturated ammonium sulfate precipitated fractions disclosed a class of relatively high-affinity sites with an apparent Kd of approximately 50 nM and binding capacities of approximately 41 and 9 pmol/mg of protein, respectively. Two /sup 203/Pb binding proteins with approximate molecular masses of 63K and 11.5K daltons and a high molecular weight component (greater than 200K) were isolated by Sepharose-6B column chromatography. The time course of association of /sup 203/Pb with cytosol and the 63K protein showed maximum binding at 18 hr which was stable up to 25 hr at 4 degrees C. The approximate half-time dissociation rate (T 1/2) of specifically ...

1985-02-01

208

Decreased serum protein binding of diazepam and its major metabolite in the neonate during the first postnatal week relate to increased free fatty acid levels.

The PbII binding characteristics of the previously reported PbII binding proteins of rat kidney cytosol were investigated further. Saturation and Scatchard analysis of "2"0"3Pb binding in whole cytosol and in 40% saturated ammonium sulfate precipitated fractions disclosed a class of relatively high-affinity sites with an apparent Kd of approximately 50 nM and binding capacities of approximately 41 and 9 pmol/mg of protein, respectively. Two "2"0"3Pb binding proteins with approximate molecular masses of 63K and 11.5K daltons and a high molecular weight component (greater than 200K) were isolated by Sepharose-6B column chromatography. The time course of association of "2"0"3Pb with cytosol and the 63K protein showed maximum binding at 18 hr which was stable up to 25 hr at 4 degrees C. The approximate half-time dissociation rate (T 1/2) of specifically bound ...

209

Decreased binding of drugs and dyes to plasma proteins from rats with acute renal failure: effects of ureter ligation and intramuscular injection of glycerol.

The protein binding of diazepam (D) and its major active metabolite N-desmethyl diazepam (DD) was investigated in vitro in the serum of 14 mothers at birth, 21 foetuses at birth, in 100 neonates between...Full Text Available

1984-01-01

210

Characterization of hyaluronate binding proteins isolated from 3T3 and murine sarcoma virus transformed 3T3 cells

1 The decreased binding of drugs and dyes to plasma proteins from male and female rats with acute renal failure has been investigated using equilibrium dialysis at 37 degrees C. 2 Acute renal failure...Full Text Available

1979-06-01

211

Binding of Ru(bpy)₂(eilatin)²⁺ to Matched and Mismatched DNA

A hyaluronic acid binding fraction was purified from the supernatant media of both 3T3 and murine sarcoma virus (MSV) transformed 3T3 cultures by hyaluronate and immunoaffinity chromatography. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis resolved the hyaluronate affinity-purified fraction into three major protein bands of estimated molecular weight (M/sub r,e/) 70K, 66K, and 56K which contained hyaluronate binding activity and which were termed hyaluronate binding proteins (HABP). Hyaluronate affinity chromatography combined with immunoaffinity chromatography, using antibody directed against the larger HABP, allowed a 20-fold purification of HABP. Fractions isolated from 3T3 supernatant medium also contained additional binding molecules in the molecular weight range of 20K. This material was present in vanishingly small amounts and was not detected with a silver stain or with (/sup ...

1987-06-02

212

Basic fibroblast growth factor binds to subendothelial extracellular matrix and is released by heparitinase and heparin-like molecules

The DNA-binding properties of Ru(bpy)₂(eilatin)²⁺ have been investigated to determine if the sterically expansive eilatin ligand confers specificity for destabilized single-base...Full Text Available

2008-07-21

213

Assessment of Glucagon-Like Peptide-1 Analogue and Renin Inhibitor on the Binding and Regulation of GLP-1 Receptor in Type 1 Diabetic Rat Hearts

Basic fibroblast growth factor (bFGF) exhibits specific binding to the extracellular matrix (ECM) produced by cultured endothelial cells. Binding was saturable as a function both of time and of concentration of {sup 125}I-bFGF. Scatchard analysis of FGF binding revealed the presence of about 1.5 x 10{sup 12} binding sites/mm{sup 2} ECM with an apparent k{sub D} of 610 nM. FGF binds to heparan sulfate (HS) in ECM as evidenced by (i) inhibition of binding in the presence of heparin or HS at 0.1-1 {mu}g/mL, but not by chondroitin sulfate, keratan sulfate, or hyaluronic acid at 10 {mu}g/mL, (ii) lack of binding to ECM pretreated with heparitinase, but not with chondroitinase ABC, and (iii) rapid release of up to 90% of ECM-bound FGF by exposure to heparin, HS, or heparitinase, but not to chondroitin sulfate, keratan sulfate, hyaluronic acid, or ...

1989-02-21

214

A region in the cytosolic domain of the epidermal growth factor receptor antithetically regulates the stimulatory and inhibitory guanine nucleotide-binding regulatory proteins of adenylyl cyclase.

This study focuses on the effects of long-term renin-angiotensin system suppression and/or incretin mimetic therapies on the regulation and binding affinity of GLP-1 to its receptor in the coronary...Full Text Available

2011-01-01

215

A Single Domain Llama Antibody Potently Inhibits the Enzymatic Activity of Botulinum Neurotoxin by Binding to the Non-Catalytic Alpha-Exosite Binding Region

Epidermal growth factor (EGF) stimulates adenylyl cyclase in the heart via activation of the stimulatory GTP-binding protein Gs. Therefore, employing peptides corresponding to regions in the cytosolic...Full Text Available

1995-03-14

216

A New Metal-Binding Site for Yeast Phosphoglycerate Kinase as Determined by the Use of a Metal-ATP Analog

Ingestion or inhalation of botulinum neurotoxin (BoNT) results in botulism, a severe and frequently fatal disease. Current treatments rely on antitoxins, which while effective cannot reverse...Full Text Available

2010-04-09

217

["3H]QNB binding and contraction of rabbit colonic smooth muscle cells

Suicide substrate β, γ-bidentate Rh(III)ATP (RhATP) was used to map the metal ion-binding site in yeast phosphoglycerate kinase (PGK). Cleavage of the RhATP-inactivated enzyme with...Full Text Available

1997-02-01

218

Recognition and Detoxification of the Insecticide DDT by Drosophila melanogaster Glutathione S-Transferase D1

The authors used radioligand binding and studies of cell contraction to characterize muscarinic receptors on dispersed smooth muscle cells from rabbit proximal and distal colon. Cells obtained after serial incubations in collagenase were used to measure binding of tritiated quinuclidinyl benzilate (["3H]QNB). At 37 degree C, specific ["3H]QNB binding was saturable and linearly related to cell number. Nonlinear regression analysis was used to determine the affinity of ["3H]QNB for its receptor. The IC_5_0 for the muscarinic agonists bethanechol and oxotremorine were 80 and 0.57 #mu#M, respectively. Hill coefficients were 0.67 for both, suggesting more complex interaction involving receptors of different affinities. In studies of cell contraction, bethanechol stimulated a dose-dependent decrease in cell length with half the maximal contraction occurring at 100 pM. These results suggest that (1) contraction is mediated by ...

1987-01-01

219

Pharmacokinetics of buspirone as determined by ex vivo (/sup 3/H)-DPAT binding

GSTD1 is one of several insect glutathione S-transferases capable of metabolizing the insecticide DDT. Here we use crystallography and NMR to elucidate the binding of DDT and glutathione to GSTD1. The crystal structure of Drosophila melanogaster GSTD1 has been determined to 1.1 {angstrom} resolution, which reveals that the enzyme adopts the canonical GST fold but with a partially occluded active site caused by the packing of a C-terminal helix against one wall of the binding site for substrates. This helix would need to unwind or be displaced to enable catalysis. When the C-terminal helix is removed from the model of the crystal structure, DDT can be computationally docked into the active site in an orientation favoring catalysis. Two-dimensional {sup 1}H,{sup 15}N heteronuclear single-quantum coherence NMR experiments of GSTD1 indicate that conformational changes occur upon glutathione and DDT binding and the residues that ...

2010-06-14

220

Metal Coupled Folding of Cys2His2 Zinc-Finger

Ex vivo (/sup 3/H)-8-hydroxy-2-(di-n-propylamino)-tetraline ((/sup 3/H)-DPAT) binding to the hippocampus has been utilized to determine the pharmacokinetic parameters of buspirone after i.v. and oral administration of this drug to rats. Intravenous buspirone rapidly penetrated the brain as demonstrated by a maximum inhibition of (/sup 3/H)-DPAT binding at 1 min. Elimination of drug from the brain was biphasic, with a first component half-life of 24.8 min and a second component half-life of 96 min. Oral buspirone at 3 times the i.v. dose produced less than one-third the maximum inhibition of (/sup 3/H)-DPAT binding compared to that observed with i.v. buspirone. The pharmacokinetic parameters of buspirone observed in the present study are in agreement with those reported previously. Thus, the ex vivo binding assay could be utilized to determine the bioavailability of the drug to the brain, and its ...

1988-01-01

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221

Identification of the binding domain for NADP"+ of human glucose-6-phosphate dehydrogenase by sequence analysis of mutants

Zinc-fingers, which widely exist in eukaryotic cell and play crucial roles in life processes, depend on the binding of zinc ion for their proper folding. To computationally study the zinc coupled folding of the zinc-fingers, charge transfer and metal induced protonation/deprotonation effects have to be considered. Here, by attempting to implicitly account for such effects in classical molecular dynamics and performing intensive simulations with explicit solvent for the peptides with and without zinc binding, we investigate the folding of the Cys2His2 type zinc-finger motif and the coupling between the peptide folding and zinc binding. We find that zinc ion not only stabilizes the native structure, but also participates in the whole folding process. It binds to the peptide at early stage of folding, and directs or modulates the folding and stabilizations of the component beta-hairpin and alpha-helix. ...

2008-01-01

222

Atrial natriuretic peptide receptor heterogeneity and effects on cyclic GMP accumulation

Human erythrocyte glucose-6-phosphate is normally quite stable in the presence of 10 #mu#M NADP"+. Certain glucose-6-phosphate dehydrogenase variants lose virtually all their activity at this concentration of NADP"+ but are reactivated by 200 #mu#M NADP"+. Such variants presumably have a defect in their NADP"+-binding site. The authors analyzed the sequence of cDNA or genomic DNA from seven unrelated patients with hemolytic anemia due to the inheritance of variants that are reactivated by NADP"+. Six patients had substitutions of one of three adjacent amino acids, and the seventh patient had another amino acid substitution 23 residues downstream. These amino acids are highly conserved, all being present in rat and all but one being found also in Drosophila. The anomalous electrophoretic behavior of some of the variants can be explained by their loss of ability to bind NADP"+. The conclude that the region in which these mutations occur defines ...

223

The p75"N"T"R tumor suppressor induces cell cycle arrest facilitating caspase mediated apoptosis in prostate tumor cells

The effects of atrial natriuretic peptide (ANP), oxytocin (OT) and vasopressin (AVP) on guanylate cyclase activity and cyclic GMP accumulation were examined, since these hormones appear to be intimately associated with blood pressure and intravascular volume homeostasis. ANP was found to increase cyclic GMP accumulation in ten cell culture systems, which were derived from blood vessels, adrenal cortex, kidney, lung, testes and mammary gland. ANP receptors were characterized in intact cultured cells using {sup 125}I-ANP{sub 8-33}. Specific {sup 125}I-ANP binding was saturable and of high affinity. Scratchard analysis of the binding data for all cell types exhibited a straight line, indicating that these cells possessed a single class of binding sites. Despite the presence of linear Scatchard plots, these studies demonstrated that cultured cells possess two functionally and physically distinct ANP-binding ...

1988-01-01

224

Rapid inhibition of vasoconstriction in renal afferent arterioles by aldosterone

The p75 neurotrophin receptor (p75"N"T"R) is a death receptor which belongs to the tumor necrosis factor receptor super-family of membrane proteins. This study shows that p75"N"T"R retarded cell cycle progression by induced accumulation of cells in G0/G1 and a reduction in the S phase of the cell cycle. The rescue of tumor cells from cell cycle progression by a death domain deleted (#DELTA#DD) dominant-negative antagonist of p75"N"T"R showed that the death domain transduced anti-proliferative activity in a ligand-independent manner. Conversely, addition of NGF ligand rescued retardation of cell cycle progression with commensurate changes in components of the cyclin/cdk holoenzyme complex. In the absence of ligand, p75"N"T"R-dependent cell cycle arrest facilitated an increase in apoptotic nuclear fragmentation of the prostate cancer cells. Apoptosis of p75"N"T"R expressing cells occurred via the intrinsic mitochondrial pathway leading to a sequential caspase-9 and ...

2006-03-24

225

DEFF Research Database (Denmark)

Aldosterone has been suggested to elicit vessel contraction via a nongenomic mechanism. We tested this proposal in microdissected, perfused rabbit renal afferent arterioles. Aldosterone had no effect on internal diameter in concentrations from 10(-10) to 10(-5) mol/L, but aldosterone abolished the ability of 100 mmol/L KCl to induce vascular contraction. The inhibitory effect of aldosterone was observed from 1 pmol/L. The inhibitory effect was significant after 5 minutes and maximal after 20 minutes and was fully reversible. Actinomycin D (10(-6) mol/L) prolonged the effect of aldosterone. The effect was abolished by the mineralocorticoid receptor antagonist spironolactone (10(-7) mol/L) but not by the glucocorticoid receptor antagonist mifepristone (10(-6) mol/L). The K+-mediated increase of intracellular calcium concentration in afferent arterioles was not affected by aldosterone. Mineralocorticoid receptor was detected by reverse ...

2003-01-01

226

Prostaglandin (PG) E3 synthesis elicted by adrenergic stimuli in guinea-pig trachea (GPT) is mediated primarily by B2 adrenergic receptors

Prostaglandin (PG) E3 synthesis elicted by adrenergic stimuli in guinea-pig trachea (GPT) is mediated primarily by B2 adrenergic receptors

The purpose of this study was to examine arachidonic acid (AA) metabolism and to characterize the type of adrenergic receptor (AR) involved in the production of the major metabolite of this fatty acid. ({sup 14}C)AA was incubated with GPT-rings and the radiolabelled products were extracted and separated by TLC method. The medium was also assayed for radiolabelled immunoreactive PG's (iPG's) and leukotrienes (LT) B4 and C4 by RIA or Enzyme immunoassay (EIA) after exposure to various AR agonists. ({sup 14}C)AA was incorporated into GPT-rings and metabolized mainly into iPGE2 and smaller amounts into PGF2{alpha}. Trace amounts of PGD2 and 6-keto-PGF1{alpha} but not LTB4 or LTC4 were detected by RIA and/or EIA. Incubation of GPT rings for 15 minutes with isoproterenol and salbutamol resulted in a significant increase of PGE2 synthesis (optimum conc: 10{sup {minus}7}, 10{sup {minus}7}M respectively). In contrast, dobutamine, norepinephrine, phenylnephrine and xylazine (up ...

1990-02-26

227

Effect of systemic blockade of ?(1)-noradrenergic receptors on sex behavior and vaginal-cervical stimulation-induced Fos in female rats.

The purpose of this study was to examine arachidonic acid (AA) metabolism and to characterize the type of adrenergic receptor (AR) involved in the production of the major metabolite of this fatty acid. ["1"4C]AA was incubated with GPT-rings and the radiolabelled products were extracted and separated by TLC method. The medium was also assayed for radiolabelled immunoreactive PG's (iPG's) and leukotrienes (LT) B4 and C4 by RIA or Enzyme immunoassay (EIA) after exposure to various AR agonists. ["1"4C]AA was incorporated into GPT-rings and metabolized mainly into iPGE2 and smaller amounts into PGF2#alpha#. Trace amounts of PGD2 and 6-keto-PGF1#alpha# but not LTB4 or LTC4 were detected by RIA and/or EIA. Incubation of GPT rings for 15 minutes with isoproterenol and salbutamol resulted in a significant increase of PGE2 synthesis (optimum conc: 10"-"7, 10"-"7M respectively). In contrast, dobutamine, norepinephrine, phenylnephrine and xylazine (up to 10"-"6M) did not significantly increase ...

1991-04-21

228

Single protein omission reconstitution studies of tetracycline binding to the 30S subunit of Escherichia coli ribosomes

It is hypothesized that systemic ??-noradrenergic antagonists may interfere with the transmission of sensory stimulation, particularly vaginal--cervical stimulation (VCS), which is crucial for reproductive functioning. To determine if ??-noradrenergic transmission receptor activity is necessary for transmission of sensory information important for VCS-dependent events, we conducted an experiment using prazosin, a ??-noradrenergic receptor antagonist. First, three doses of prazosin (1.0, 0.5 or 0.1 mg/kg) or the 10% ETOH in sesame oil vehicle were administered i.p. and sexual receptivity was assessed 30 min later in ovariectomized, hormone-treated female rats. The 1 mg/kg dose of prazosin significantly inhibited lordosis quotients and lordosis ratings. This dose of prazosin (1.0 mg/kg) was then administered 30 min prior to VCS or control scapular stimulation (CSS) and Fos-IR was examined in the posterodorsal medial amygdala (MeaPD), the medial ...

2010-10-01

229

Functional and physical molecular size of the chicken hepatic lectin determined by radiation inactivation and sedimentation equilibrium analysis

In previous work the authors showed that on photolysis of Escherichia coli ribosomes in the presence of ({sup 3}H)tetracycline (TC) the major protein labeled is S7, and they presented strong evidence that such labeling takes place from a high-affinity site related to the inhibitory action of TC. In this work they use single protein omission reconstitution (SPORE) experiments to identify those proteins that are important for high-affinity TC binding to the 30S subunit, as measured by both cosedimentation and filter binding assays. With respect to both sedimentation coefficients and relative Phe-tRNA{sup Phe} binding, the properties of the SPORE particles they obtain parallel very closely those measured earlier, with the exception of the SPORE particle lacking S13. A total of five proteins, S3, S7, S8, S14, and S19, are shown to be important for TC binding, with the largest effects seen on omission of ...

1990-06-05

230

Distribution of lead-203 in human peripheral blood in vitro

Radiation inactivation and sedimentation equilibrium analysis were used to determine the functional and physical size of the chicken hepatic membrane receptor that binds N-acetylglucosamine-terminated glycoproteins. Purified plasma membranes from chicken liver were irradiated with high energy electrons and assayed for 125I-agalactoorosomucoid binding. Increasing the dose of ionizing radiation resulted in a monoexponential decay in binding activity due to a progressive loss of binding sites. The molecular mass of the chicken lectin, determined in situ by target analysis, was 69,000 +/- 9,000 Da. When the same irradiated membranes were solubilized in Brij 58 and assayed, the binding protein exhibited a target size of 62,000 +/- 4,000 Da; in Triton X-100, the functional size of the receptor was 85,000 +/- 10,000 Da. Sedimentation equilibrium measurements of the purified ...

1990-03-05

231

Computational identification of developmental enhancers:conservation and function of transcription factor binding-site clustersin drosophila melanogaster and drosophila psedoobscura

In-vitro experiments using "2"0"3Pb were performed to identify the lead binding components in human peripheral blood. The distribution of lead in plasma, in the red cell membrane, and within the red cell was also investigated. Studies of the distribution of "2"0"3Pb in the whole blood showed that at a lead concentration of 2.45 #mu#mol/l (50 #mu#g/100 ml) about 94% of lead had been incorporated by the erythrocytes and 6% remained in the plasma. After extraction of lipid by a methanol/chloroform mixture, about 75% of the lead was found to be associated with the protein fraction. The lipid contained about 21% of the "2"0"3Pb, the remainder being in the aqueous plasma. SDS polyacrylamide gel electrophoresis of blood plasma showed that almost 90% of the "2"0"3Pb was present in the albumin fraction; the remainder was likely to be associated with high molecular weight globulins. Several binding sites were identified on the erythrocyte membrane. The ...

232

"1H and "3"1P nuclear magnetic resonance investigation of the interaction between 2,3-diphosphoglycerate and human normal adult hemoglobin

Background The identification of sequences that control transcription in metazoans is a major goal of genome analysis. In a previous study, we demonstrated that searching for clusters of predicted transcription factor binding sites could discover active regulatory sequences, and identified 37 regions of the Drosophila melanogaster genome with high densities of predicted binding sites for five transcription factors involved in anterior-posterior embryonic patterning. Nine of these clusters overlapped known enhancers. Here, we report the results of in vivo functional analysis of 27 remaining clusters. Results We generated transgenic flies carrying each cluster attached to a basal promoter and reporter gene, and assayed embryos for reporter gene expression. Six clusters are enhancers of adjacent genes: giant, fushi tarazu, odd-skipped, nubbin, squeeze and pdm2; three drive expression in patterns unrelated to those of neighboring genes; the ...

2004-08-06

233

ON THE BINDING ENERGY PARAMETER #lambda# OF COMMON ENVELOPE EVOLUTION

High-resolution "1H and "3"1P nuclear magnetic resonance spectroscopy has been used to investigate the binding of 2,3-diphosphoglycerate to human normal adult hemoglobin and the molecular interactions involved in the allosteric effect of the 2,3-diphosphoglycerate molecule on hemoglobin. Individual hydrogen ion NMR titration curves have been obtained for 22-26 histidyl residues of hemoglobin and for each phosphate group of 2,3-diphosphoglycerate with hemoglobin in both the deoxy and carbonmonoxy forms. The results indicate that 2,3-diphosphoglycerate binds to deoxyhemoglobin at the central cavity between the two #beta# chains and the binding involves the #beta#2-histidyl residues. Moreover, the results suggest that the binding site of 2,3-diphosphoglycerate to carbonmonoxyhemoglobin contains the same (or at least some of the same) amino acid residues responsible for binding in the ...

234

Ab initio pseudopotential calculations of carbon impurities in Si

The binding energy parameter #lambda# plays an important role in common envelope evolution. Previous works have already pointed out that #lambda# varies throughout the stellar evolution, though it has been adopted as a constant in most of the population synthesis calculations. We have systematically calculated the binding energy parameter #lambda# for both Population I and Population II stars of masses 1-20 M _s_u_n, taking into account the contribution from the internal energy of stellar matter. We present fitting formulae for #lambda# that can be incorporated into future population synthesis investigations. We also briefly discuss the possible applications of the results in binary evolutions.

2010-06-10

235

Gas and stellar dynamics in NGC 1068. Probing the galactic gravitational potential

Ab initio planewave pseudopotential method is used to study carbon diffusion and pairing in crystalline silicon. The calculation is performed with a 40 Ry planewave cutoff and 2x2x2 special k-point sampling with a supercell of 64 atoms. It is found that substitutional carbon attracts interstitial Si forming a <001> C interstitial with a large binding energy of 1.45 eV. The interstitial carbon is mobile and can migrate with a migration energy of 0.5 eV. The interstitial carbon can bind further to another substitutional carbon forming a substitutional carbon-interstitutional carbon pair with a binding energy of 1.0 eV. This model is used to understand the effect of high C concentration on the transient enhanced diffusion in Si.

1997-11-01

236

Direct solar water splitting cell using water, WO3, Pt, and polymer electrolyte membrane

We present Sauron 2D spectrography of the central 1.5 kpc of the nearby Sey2 galaxy NGC1068, encompassing the well-known NIR inner bar. We have successively disentangled the respective contributions of the ionized gas and stars, thus deriving their 2D distribution and kinematics. The [OIII] and Hbeta emission lines exhibit very different spatial distribution and kinematics, the latter following inner spiral arms with clumps associated with star formation. Strong inwards streaming motions are observed in both the Hbeta and [OIII] kinematics. The stellar kinematics also exhibit clear signatures of a non-axisymmetric tumbling potential, with a twist in both the velocity and h3 fields. We re-examined the long-slit data of Shapiro et al (2003) using pPXF: a strong decoupling of h3 is revealed, and the central decrease in h4 hinted in the Sauron data is confirmed. These data also suggest that NGC1068 is a ...

2006-01-01

237

British Library Electronic Table of Contents (United Kingdom)

A solar water splitting cell composed of WO3, Polymer Electrolyte Membrane (PEM) and Pt was constructed for producing hydrogen from deionized water in sunlight. Spectral responsivity measurements under various temperatures and bias voltages were conducted for the cell using the Incident Photon to Current Efficiency (IPCE) method. For comparison, a known WO3 Photo Electro Chemical (PEC) cell containing H3PO4 electrolyte, WO3/H3PO4/Pt, was tested using the same test method. The WO3/PEM-H2O/Pt cell showed better Quantum Efficiency (QE) performance compared to that obtained from the cell with the chemical electrolyte. For the first time, spectral responsivity of photo water splitting process without bias power was unveiled in the new WO3 cell, demonstrating the self-sustained photo electrolysi...

2009-01-01

238

Extraction of magnesium as the iodide by tributyl phosphate

Effect of pH on the pitting corrosion of austenitic stainless steel in chloride solution

The extraction of magnesium by tributyl phosphate from KI solutions was investigated. With increasing KI and TBP concentrations, the extraction increased. The maximum extraction (82%) was attained at pH 4, and it did not decrease with a further pH increase. With decreasing pH, the extraction decreased because of HI extraction. The magnesium was extracted as the compound MgI/sub 2/ x 4TBP. Complexone III (at pH 3-4) does not affect the extraction of magnesium, which makes it possible to use it to mask other metals.

1987-08-20

239

c-Myc Mediates a Hypoxia-Induced Decrease in Acetylated Histone H4

This paper deals with the pitting corrosion of evaporators in the liquid - radwaste system of nuclear power stations. Corrosion testrs were conducted by the anodic polalization of specimen in the chloride solution. (1) The initiation of the pitting in SUS 304, SUS 316 stainless steels was inhibited by addition of NaOH and H_3BO_3, however, these addition had no effect on the pitting propagation. (2) Inconel 625 had the resitivity against the pitting initiation superior to that of stainless steels, but this was not necessarily in the case of the pitting propagation. (3) It is noticed for pitting prevention that the environmental and material effect on the pitting initiation differed from that on the pitting propagation. (author).

240

Zn, Cu, Cd and Hg binding to metallothioneins in harbour porpoises Phocoena phocoena from the southern North Sea

Global acetylation of histone H4 is a mark of gene transcriptional activation. The c-Myc transcription factor binds to specific DNA sites in cellular chromatin and induces the acetylation of...Full Text Available

2009-10-01

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241

Variant influenza virus hemagglutinin that induces fusion at elevated pH.

BackgroundHarbour porpoises Phocoena phocoena from the southern North Sea are known to display high levels of Zn and Hg in their tissues linked to their nutritional...Full Text Available

242

Validity of Cardiac Markers as Diagnostic and Prognostic Indicators of Complications in Patients undergoing Percutaneous Coronary Intervention

The hemagglutinin (HA) glycoprotein of influenza virus performs two critical roles during infection: it binds virus to cell surface sialic acids, and under mildly acidic conditions it induces fusion...Full Text Available

1986-02-01

243

Using X-ray Microscopy and Hg L₃ XANES to study Hg Binding in the Rhizosphere of Spartina Cordgrass

ObjectivesThe aim of this study was to assess the diagnostic and prognostic value of heart-type fatty acid-binding protein (H-FABP) in elective percutaneous coronary intervention...Full Text Available

2010-04-01

244

Use of the parmbsc0 force field and trajectory analysis to study the binding of netropsin to the DNA fragment (5'CCAATTGG)2 in the presence of excess NaCl salt in aqueous solution

San Francisco Bay has been contaminated historically by mercury from mine tailings as well as contemporary industrial sources. Native Spartina foliosa and non-native S....Full Text Available

2009-10-01

245

British Library Electronic Table of Contents (United Kingdom)

The parmbsc0 force field was applied to study in detail the binding of netropsin, at a salt concentration of 0.28M Na^+, to the minor groove of an 8-mer (5'CCAATTGG)2 DNA duplex forming a netropsin.DNA complex which previously has been characterized by X-ray crystallography, albeit with the use of closely related DNA duplexes. The X-ray structure revealed that the terminal guanidinium and amidinium groups of netropsin interact with the extreme ends of the palindromic AATT sequence of the receptor DNA. The parmbsc0 parameters of B-DNA and AMBER v9 parameters of netropsin generated a stable 6ns molecular dynamics (MD) trajectory for a 1:1 class I binding motif of this complex. Trajectory analysis for the salt and hydration effects on the binding of netropsin to the 8-mer DNA duplex revealed ...

2011-01-01

246

Unconventional Secretion of AcbA in Dictyostelium discoideum through a Vesicular Intermediate?

The Subtilisin-Like Protease AprV2 Is Required for Virulence and Uses a Novel Disulphide-Tethered Exosite to Bind Substrates

The acyl coenzyme A (CoA) binding protein AcbA is secreted unconventionally and processed into spore differentiation factor 2 (SDF-2), a peptide that coordinates sporulation in Dictyostelium...Full Text Available

2010-07-01

247

The Structure of Sucrose Phosphate Synthase from Halothermothrix orenii Reveals Its Mechanism of Action and Binding Mode

Many bacterial pathogens produce extracellular proteases that degrade the extracellular matrix of the host and therefore are involved in disease pathogenesis. Dichelobacter nodosus...Full Text Available

2010-11-01

248

The Specificity of Innate Immune Responses Is Enforced by Repression of Interferon Response Elements by NF-?B p50

Sucrose phosphate synthase (SPS) catalyzes the transfer of a glycosyl group from an activated donor sugar, such as uridine diphosphate glucose (UDP-Glc), to a saccharide acceptor D-fructose 6-phosphate (F6P), resulting in the formation of UDP and D-sucrose-6'-phosphate (S6P). This is a central regulatory process in the production of sucrose in plants, cyanobacteria, and proteobacteria. Here, we report the crystal structure of SPS from the nonphotosynthetic bacterium Halothermothrix orenii and its complexes with the substrate F6P and the product S6P. SPS has two distinct Rossmann-fold domains with a large substrate binding cleft at the interdomain interface. Structures of two complexes show that both the substrate F6P and the product S6P bind to the A-domain of SPS. Based on comparative analysis of the SPS structure with other related enzymes, the donor substrate, nucleotide diphosphate glucose, binds to the ...

2008-01-01

249

The RNA Chaperone Hfq Is Important for Growth and Stress Tolerance in Francisella novicida

The specific binding of transcription factors to cognate sequence elements is thought to be critical for the generation of specific gene expression programs. Members of the nuclear factor κB...Full Text Available

250

Tarantula Huwentoxin-IV Inhibits Neuronal Sodium Channels by Binding to Receptor Site 4 and Trapping the Domain II Voltage Sensor in the Closed Configuration*S?

The RNA-binding protein Hfq is recognized as an important regulatory factor in a variety of cellular processes, including stress resistance and pathogenesis. Hfq has been shown in several bacteria to...Full Text Available

251

Synergistic Operation of the CAR2 (Ornithine Transaminase) Promoter Elements in Saccharomyces cerevisiae

Peptide toxins with high affinity, divergent pharmacological functions, and isoform-specific selectivity are powerful tools for investigating the structure-function relationships of voltage-gated...Full Text Available

2008-10-03

252

Structure of the Taz2 domain of p300: insights into ligand binding

Dal82p binds to the UIS_ALL sites of allophanate-induced genes of the allantoin-degradative pathway and functions synergistically with the GATA family Gln3p and Gat1p transcriptional...Full Text Available

1999-11-01

253

Structural basis of ligand binding by a c-di-GMP riboswitch

CBP and its paralog p300 are histone acetyl transferases that regulate gene expression by interacting with multiple transcription factors via specialized domains. The structure...Full Text Available

2009-12-01

254

Stochastic simulation of the transducin GTPase cycle.

The second messenger signaling molecule bis-(3′-5′)-cyclic dimeric guanosine monophosphate (c-di-GMP) regulates many processes in bacteria, including motility, pathogenesis,...Full Text Available

2009-12-01

255

Species-specific microRNA roles elucidated following astrocyte activation

On rod disc membranes, single photoactivated rhodopsin (R*) molecules catalytically activate many copies of the G-protein (Gt), which in turn binds and activates the effector (phosphodiesterase). We...Full Text Available

1996-12-01

256

Serotonin Transporter Binding and Genotype in the Nonhuman Primate Brain using [C-11]DASB PET

MicroRNAs (miRNAs) are short non-coding RNAs that play a central role in regulation of gene expression by binding to target genes. Many miRNAs were associated with the function of the central nervous...Full Text Available

2011-05-01

257

Roles of lead-binding proteins in mediating lead bioavailability.

The length polymorphism of the serotonin (5-HT) transporter gene promoter region has been implicated in altered 5-HT function and, in turn, neuropsychiatric illnesses, such as anxiety and depression....Full Text Available

2009-10-01

258

Role of Conserved Salt Bridges in Homeodomain Stability and DNA Binding*

The intracellular bioavailability of lead (Pb) at low dosage levels in major target organs such as the kidney and brain appears to be largely determined by complexation with a group of low molecular...Full Text Available

1998-12-01

259

Red Light-Regulated Growth ¹

The sequence information available for homeodomains reveals that salt bridges connecting pairs 19/30, 31/42, and 17/52 are frequent, whereas aliphatic residues at these sites are rare and mainly restricted...Full Text Available

2009-08-28

260

Receptor in group C and G streptococci detects albumin structures present in mammalian species.

We examined the changes in the levels of indoleacetic acid (IAA), IAA esters, and a 22-kilodalton subunit auxin-binding protein (ABP1) in apical mesocotyl tissue of maize (Zea mays...Full Text Available

1991-09-01

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261

Radiation modification of vascular prostheses

The presence of albumin structures with the capacity to bind to a surface receptor in group C and G streptococci was studied in serum samples from 45 mammalian species representing 15 different orders,...Full Text Available

1982-05-01

262

Radiation inactivation target size of rat adipocyte glucose transporters in the plasma membrane and intracellular pools

The radiation method has been employed for the modification of the surface of vascular prostheses by means of acrylamide. As a result of the treatment, the tightness of the prosthesis walls was improved as well as an increase of surface hydrophilicity. Upon autoclaving, stable binding of polyacrylamide to prostheses is achieved. (author).

263

Quantitative Analysis of Endocytosis and Turnover of Epidermal Growth Factor (EGF) and EGF Receptor

The in situ assembly states of the glucose transport carrier protein in the plasma membrane and in the intracellular (microsomal) storage pool of rat adipocytes were assessed by studying radiation-induced inactivation of the D-glucose-sensitive cytochalasin B binding activities. High energy radiation inactivated the glucose-sensitive cytochalasin B binding of each of these membrane preparations by reducing the total number of the binding sites without affecting the dissociation constant. The reduction in total number of binding sites was analyzed as a function of radiation dose based on target theory, from which a radiation-sensitive mass (target size) was calculated. When the plasma membranes of insulin-treated adipocytes were used, a target size of approximately 58,000 daltons was obtained. For adipocyte microsomal membranes, we obtained target sizes of approximately 112,000 and 109,000 daltons prior ...

1987-06-15

264

Quantitation of Antibody to Non-Hemagglutinating Viruses by Single Radial Hemolysis: Serological Test for Human Coronaviruses

Binding of epidermal growth factor (EGF) to the EGF receptor (EGFR) initiates signal transduction, ultimately leading to altered gene expression. Ligand-activated EGFR is also rapidly internalized...Full Text Available

2010-03-01

265

Purification, characterization and binding interactions of the Chinese-cobra (Naja naja atra) serum antitoxic protein CSAP.

A single radial hemolysis test was developed for quantitation of specific antibody to non-hemagglutinating viruses. With the human coronaviruses as models, this test utilizes the binding properties...Full Text Available

1977-06-01

266

Purification of mRNA guanylyltransferase from calf thymus.

The characterization of the single-chain protein in Chinese-cobra (Naja naja atra) blood serum, which yields strong specific protection against the venom of the same snake, is reported. The protein,...Full Text Available

1993-07-15

267

Purification of functional baculovirus particles from silkworm larval hemolymph and their use as nanoparticles for the detection of human prorenin receptor (PRR) binding

mRNA guanylyltransferase has been extensively purified from calf thymus. A GTP-binding assay was used based on the observations by Shuman and Hurwitz (1981) and Venkatesan and Moss (1982) that vaccinia...Full Text Available

1982-01-01

268

Purification and Characterization of a Membrane-Bound Protease from Chlamydomonas reinhardtii 1

BackgroundBaculovirus, which has a width of 40 nm and a length of 250-300 nm, can display functional peptides, receptors and antigens on its surface by their fusion with a baculovirus...Full Text Available

269

Prolonged signaling at the parathyroid hormone receptor by peptide ligands targeted to a specific receptor conformation

In Chlamydomonas reinhardtii y-1, newly synthesized chlorophyll a/b-binding apoproteins are degraded when chlorophylls are not present for assembly of stable light-harvesting...Full Text Available

1992-07-01

270

Prolactin Receptor Signaling Is Essential for Perinatal Brown Adipocyte Function: A Role for Insulin-like Growth Factor-2

The parathyroid hormone receptor (PTHR) is a class B G protein-coupled receptor that plays critical roles in bone and mineral ion metabolism. Ligand binding to the PTHR involves interactions to both...Full Text Available

2008-10-28

271

Profound human/mouse differences in alpha-dystrobrevin isoforms: a novel syntrophin-binding site and promoter missing in mouse and rat

BackgroundThe lactogenic hormones prolactin (PRL) and placental lactogens (PL) play central roles in reproduction and mammary development. Their actions are mediated via binding...Full Text Available

272

Precise temporal control of the eye regulatory gene Pax6 via enhancer-binding site affinity

BackgroundThe dystrophin glycoprotein complex is disrupted in Duchenne muscular dystrophy and many other neuromuscular diseases. The principal heterodimeric partner of dystrophin...Full Text Available

273

Plasma binding of disopyramide and mono-N-dealkyldisopyramide.

How transcription factors interpret the cis-regulatory logic encoded within enhancers to mediate quantitative changes in spatiotemporally restricted expression patterns during animal...Full Text Available

2010-05-15

274

Physiological calcium concentrations regulate calmodulin binding and catalysis of adenylyl cyclase exotoxins

1 Measuring total plasma levels of disopyramide (DP) and the main metabolite mono-N-dealkyldisopyramide (MND) in patients on maintenance therapy with DP has shown concentrations of MND comparable with...Full Text Available

1982-11-01

275

OmpA of Uropathogenic Escherichia coli Promotes Postinvasion Pathogenesis of Cystitis?

Edema factor (EF) and CyaA are calmodulin (CaM)-activated adenylyl cyclase exotoxins involved in the pathogenesis of anthrax and whooping cough, respectively. Using spectroscopic, enzyme kinetic and...Full Text Available

2002-12-16

276

Ocular manifestations of branchio-oculo-facial syndrome: Report of a novel mutation and review of the literature

Type 1 pilus directs bladder epithelial binding and invasion by uropathogenic Escherichia coli (UPEC) in the initial stage of cystitis, but the bacterial determinants of postinvasion...Full Text Available

2009-12-01

277

Nucleocapsid and Matrix Protein Contributions to Selective Human Immunodeficiency Virus Type 1 Genomic RNA Packaging

PurposeTo report unusual ocular manifestations of branchio-oculo-facial syndrome (BOFS) caused by a novel mutation in activating enhancer binding protein 2 alpha (TFAP2A).MethodsFull...Full Text Available

278

Molecular dynamics of a ?B DNA element: base flipping via cross-strand intercalative stacking in a microsecond-scale simulation

The nucleocapsid protein (NC) of retroviruses plays a major role in genomic RNA packaging, and some evidence has implicated the matrix protein (MA) of certain retroviruses in viral RNA binding. To further...Full Text Available

1998-03-01

279

Name of Presentation!

Wastenet

Up-flow anaerobic attached-growth bioreactors filled with pre-treated coir fibres ...coir-fibre arranged in bottle-brush configuration bounded by a novel plastic binding technique ...-three anaerobic filter reactors in series -coir fibre as the bacteria growth media a sedimentation

280

Molecular conformation, receptor binding, and hormone action of natural and synthetic estrogens and antiestrogens.

The sequence-dependent structural variability and conformational dynamics of DNA play pivotal roles in many biological milieus, such as in the site-specific binding of transcription factors to target...Full Text Available

2008-09-01

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281

Molecular basis of FIR-mediated c-myc transcriptional control

The X-ray crystallographic structural determinations of synthetic estrogens and antiestrogens provide reliable information on the global minimum energy conformation of these molecules or a local minimum...Full Text Available

1985-09-01

282

Microfluidic Devices Integrating Microcavity Surface-Plasmon-Resonance Sensors: Glucose Oxidase Binding-Activity Detection

The Far UpStream Element (FUSE) regulatory system promotes a peak in the concentration of c-Myc during cell cycle. First, the FBP transcriptional activator binds to the FUSE DNA element upstream...Full Text Available

2010-09-01

283

Matrix-assisted laser desorption/ionization time-of-flight mass spectrometry assay for organophosphorus toxicants bound to human albumin at Tyr411

We have developed miniature (≈1 μm diameter) microcavity surface-plasmon-resonance sensors (MSPRS), integrated them with microfluidics and tested...Full Text Available

2010-01-01

284

Macrophage-directed immunotherapy as adjuvant to photodynamic therapy of cancer.

Our goal was to determine whether chlorpyrifos oxon, dichlorvos, diisopropylfluorophosphate (DFP), and sarin covalently bind to human albumin. Human albumin or plasma was treated with organophosphorus...Full Text Available

2007-02-15

285

MAPPING THE INITIATOR BINDING TAF2 SUBUNIT IN THE STRUCTURE OF HYDRATED YEAST TFIID

The effect of Photofrin-based photodynamic therapy (PDT) and adjuvant treatment with serum vitamin D3-binding protein-derived macrophage-activating factor (DBPMAF) was examined using a mouse SCCVII...Full Text Available

1997-01-01

286

Lifespan extension by increased expression of the Drosophila homologue of the IGFBP7 tumour suppressor

SummaryThe general transcription factor TFIID is a large multi-subunit complex required for the transcription of most protein-encoding genes by RNA polymerase II. Taking advantage...Full Text Available

2009-03-11

287

Lack of association between polymorphisms in C4b-binding protein and atypical haemolytic uraemic syndrome in the Spanish population

Mammals possess multiple insulin-like growth factor (IGF) binding proteins (IGFBPs), and related proteins, that modulate the activity of insulin/IGF signalling (IIS), a conserved neuroendocrine signalling...Full Text Available

2011-02-01

288

Interaction between various polymerized human albumins and hepatitis B surface antigen.

Dysregulation of the alternative pathway of complement activation, caused by mutations or polymorphisms in the genes encoding factor H, membrane co-factor protein, factor I or factor B, is associated...Full Text Available

2009-01-01

289

Interaction between Bluetongue virus outer capsid protein VP2 and vimentin is necessary for virus egress

A variety of albumin polymers were prepared and tested for binding with hepatitis B surface antigen (HBsAg): synthetic polymers cross-linked by either glutaraldehyde or carbodiimide; heat-aggregated...Full Text Available

1985-09-01

290

Insights into Cdc13 dependent telomere length regulation

BackgroundThe VP2 outer capsid protein Bluetongue Virus (BTV) is responsible for receptor binding, haemagglutination and eliciting host-specific immunity. However, the assembly of...Full Text Available

291

Initial Development and Characterization of PLGA Nanospheres Containing Ropivacaine

Cdc13 is a single stranded telomere binding protein that specifically localizes to the telomere ends of budding yeasts and is essential for cell viability. It caps the ends of chromosomes thus preventing...Full Text Available

292

Inferring transcription factor complexes from ChIP-seq data

Local anesthetics are able to induce pain relief by binding to the sodium channels of excitable membranes, blocking the influx of sodium ions and the propagation of the nervous impulse. Ropivacaine...Full Text Available

2007-12-01

293

Increased expression of cholesterol transporter ABCA1 is highly correlated with severity of dementia in AD hippocampus

Chromatin immunoprecipitation followed by high-throughput sequencing (ChIP-seq) allows researchers to determine the genome-wide binding locations of individual transcription factors (TFs) at high resolution....Full Text Available

2011-08-01

294

Identification of genetic variation and haplotype structure of the canine ABCA4 gene for retinal disease association studies

To gain insight into ATP-binding cassette transporter A1 (ABCA1) function and its potential role in AD pathology, we analyzed the expression of the cholesterol transporter ABCA1...Full Text Available

2010-03-08

295

Identification of Cardiac Myosin-binding Protein C as a Candidate Biomarker of Myocardial Infarction by Proteomics Analysis*

Over 200 mutations in the retina specific member of the ATP-binding cassette transporter super-family (ABCA4) have been associated with a diverse group of human retinal diseases....Full Text Available

2010-10-01

296

Human complement protein C99 is a calcium binding protein

Acute myocardial infarction (AMI) is a common cause of death for which effective treatments are available provided that diagnosis is rapid. The current diagnostic gold standards are circulating cardiac...Full Text Available

2009-12-01

297

Homology of SMP domains to the TULIP superfamily of lipid-binding proteins provides a structural basis for lipid exchange between ER and mitochondria

Human complement protein C9 is shown to be a metalloprotein that binds 1 mol of Ca"2"+/mol of C9 with a dissociation constant of 3 #mu#m as measured by equilibrium dialysis. Incubation with EDTA removes the bound calcium, resulting in a apoprotein with decreased thermal stability. This loss in stability leads to aggregation and, therefore, to loss of hemolytic activity upon heating to a few degrees above the physiological temperature. Heat-induced aggregation of apoC9 can be prevented by salts that stabilize proteins according to the Hofmeister series of lyotropic ions, suggesting that the ion in native C9 may ligand with more than one structural element of domain of the protein. Ligand blotting indicates that the calcium binding site is located in the amino-terminal half of the protein. Removal of calcium by inclusion of EDTA in assay mixtures has no effect on the hemolytic activity of C9, and its capacity to bind to C8 in ...

298

Highly specific antiserum for arginine vasopressin

Mitochondria must uptake some phospholipids from the endoplasmic reticulum (ER) for the biogenesis of their membranes. They convert one of these lipids, phosphatidylserine, to phosphatidylethanolamine,...Full Text Available

2010-08-15

299

High-energy reaction cross sections of light nuclei

A high sensitivity (titer 60-150,000) radioimmunoassay for arginine vasopressin (AVP) has been developed using synthetic AVP as antigen and standard. The specificity of the antiserum has been characterized in detail by measuring the relative binding affinities of 29 analogs and fragments of AVP. In general, single amino acid substitution or deletion in the AVP molecule caused a reduction in binding to the antiserum; binding was further impaired for analogs which had multiple substitutions. ''Ring'' and ''tail'' fragments of the neurohypophysial hormones did not bind to the antiserum, and the only analog which the antiserum could not differentiate from AVP was deamino-AVP. More specifically, the antiserum exhibited the following properties: position 1, no requirement for a position charge at "1/_2 Cys; positions 2 and 3, requirements for #pi#-#pi# interacting pair of aromatic side chains and for Tyr at ...

300

High-Sensitivity Analysis of Naturally Occurring Sugar Chains, Using a Novel Fluorescent Linker Molecule

The high-energy reaction cross sections of Li and Be isotopes are calculated using a simplified Glauber model and densities constrained by the empirical binding energies. We find excellent agreement with experiment, reproducing the large increase for the most neutron-rich nuclei.

1989-03-01

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301

High affinity of lead for fetal haemoglobin.

To analyse the binding of sugar chains to proteins, viruses and cells, the surface plasmon resonance (SPR) technique is very convenient and effective because it is a real-time, non-destructive detection...Full Text Available

2009-07-01

302

Functional and Structural Analysis of a Key Region of the Cell Wall Inhibitor Moenomycin

In-vitro experiments using 203Pb were performed to identify lead-binding components in human haemoglobin. Sephadex A-50 ion-exchange chromatography of haemolysate showed that different types of haemoglobin...Full Text Available

1980-08-01

303

Expression of Fc receptors is suppressed in alveolar macrophages from patients with sarcoidosis.

Moenomycin A (MmA) belongs to a family of natural products that inhibit peptidoglycan biosynthesis by binding to the peptidoglycan glycosyltransferases (PGTs), the enzymes that make the glycan...Full Text Available

2010-07-16

304

Dopamine transporter density in the basal ganglia assessed with {sup 123}I-IPT SPECT in children with attention deficit hyperactivity disorder

To study the expression of Fc receptors in human alveolar macrophages (AM), the cells were collected from 12 healthy controls and 22 patients with sarcoidosis and the activity involved in binding to...Full Text Available

1988-09-01

305

Distribution of lead-203 in human peripheral blood in vitro.

Attention deficit hyperactivity disorder (ADHD) is known as a psychiatric disorder in childhood associated with dopamine dysregulation. We investigated dopamine transporter (DAT) density in children with ADHD in the present study using {sup 123}I-IPT SPECT and postulated that an alteration in DAT density in the basal ganglia (BG) is responsible for dopaminergic dysfunction in children with ADHD. 9 durg-naive children with ADHD and 6 normal children were included in the study. We performed brain SPECT 2 hours after administration of {sup 123}I-IPT and made both quantitative and qualitative analyses for assessment of specific/nonspecific DAT binding ratio in the BG. We investigated the correlation between the severity scores of ADHD symptoms in children with ADHD assessed with ADHD rating scale and specific/nonspecific DAT binding ratio in the BG. Drug-naive children with ADHD showed a significantly incresed specific/nonspecific DAT ...

2002-07-01

306

Dissociation from albumin: a potentially rate-limiting step in the clearance of substances by the liver.

In-vitro experiments using 203Pb were performed to identify the lead binding components in human peripheral blood. The distribution of lead in plasma, in the red cell membrane, and within the red cell...Full Text Available

1980-02-01

307

Detecting microRNA activity from gene expression data

The hepatic uptake rate for certain albumin-bound drugs and metabolites correlates poorly with their equilibrium unbound concentration in the plasma, suggesting that binding equilibrium may not always...Full Text Available

1985-03-01

308

Cyclic Diguanylate Signaling Proteins Control Intracellular Growth of Legionella pneumophila

BackgroundMicroRNAs (miRNAs) are non-coding RNAs that regulate gene expression by binding to the messenger RNA (mRNA) of protein coding genes. They control gene expression by either...Full Text Available

309

Conditional deletion of Abca3 in alveolar type II cells alters surfactant homeostasis in newborn and adult mice

Proteins that metabolize or bind the nucleotide second messenger cyclic diguanylate regulate a wide variety of important processes in bacteria. These processes include motility, biofilm formation, cell...Full Text Available

310

Characterization of the binding sites for dicarboxylic acids on bovine serum albumin.

ATP-binding cassette A3 (ABCA3) is a lipid transport protein required for synthesis and storage of pulmonary surfactant in type II cells in the alveoli. Abca3 was conditionally deleted...Full Text Available

2010-05-01

311

Characterization of a fatty acid and retinol binding protein orthologue from the hookworm Ancylostoma ceylanicum?

Dicarboxylic acids are prominent features of several diseases, including Reye's syndrome and inborn errors of mitochondrial and peroxisomal fatty acid oxidation. Moreover, dicarboxylic acids are potentially...Full Text Available

1991-06-15

312

Cd36, a class B scavenger receptor, functions as a monomer to bind acetylated and oxidized low-density lipoproteins

Hookworms, bloodfeeding intestinal nematodes, infect nearly one billion people in resource limited countries and are a leading cause of anemia and malnutrition. Like other nematodes, hookworms...Full Text Available

2009-12-01

313

Cbk1 regulation of the RNA binding protein Ssd1 integrates cell fate with translational control

Cd36 is a small-molecular-weight integral membrane protein expressed in a diverse, but select, range of cell types. It has an equally diverse range of ligands and physiological functions, which has...Full Text Available

2007-11-01

314

Cadherin Mechanics and Complexation: The Importance of Calcium Binding

SummarySpatial control of gene expression, at the level of both transcription and translation, is critical for cellular differentiation [1-Full Text Available

2009-12-29

315

Both common and specialty mushrooms inhibit adhesion molecule expression and in vitro binding of monocytes to human aortic endothelial cells in a pro-inflammatory environment

E-cadherins belong to a family of membrane-bound, cellular adhesion proteins. Their adhesive properties mainly involve the two N-terminal extracellular domains (EC1 and EC2). The junctions between these...Full Text Available

2005-12-01

316

Binding of PFOS to serum albumin and DNA: insight into the molecular toxicity of perfluorochemicals

BackgroundCardiovascular disease (CVD) is a leading cause of mortality in the United States as well as globally. Epidemiological studies show that regular fruit and vegetable consumption...Full Text Available

317

Bacterial glycolipids and analogs as antigens for CD1d-restricted NKT cells

BackgroundHealth risk from exposure of perfluorochemicals (PFCs) to wildlife and human has been a subject of great interest for understanding their molecular mechanism of toxicity....Full Text Available

318

Association between a specific apolipoprotein B mutation and familial defective apolipoprotein B-100.

The CD1 family of proteins binds self and foreign glycolipids for presentation to CD1-restricted T cells. To identify previously uncharacterized active CD1 ligands, especially those of microbial origin,...Full Text Available

2005-02-01

319

Alterations in the steroid hormone receptor co-chaperone FKBPL are associated with male infertility: a case-control study

Familial defective apolipoprotein (apo) B-100 is a genetic disease that leads to hypercholesterolemia and to an increased serum concentration of low density lipoproteins that bind defectively to the...Full Text Available

1989-01-01

320

Allosteric Drug Discrimination Is Coupled to Mechanochemical Changes in the Kinesin-5 Motor Core*

BackgroundMale infertility is a common cause of reproductive failure in humans. In mice, targeted deletions of the genes coding for FKBP6 or FKBP52, members of the FK506 binding...Full Text Available

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25

321

Acute Drug-Induced Hepatitis Caused by Albendazole

Essential in mitosis, the human Kinesin-5 protein is a target for >80 classes of allosteric compounds that bind to a surface-exposed site formed by the L5 loop. Not established is why there...Full Text Available

2010-06-11

322

Absence of Ataxin-3 Leads to Enhanced Stress Response in C. elegans

Albendazole binds to parasite's tubulin inhibiting its glucose absorption. Its common adverse effects are nausea, vomiting, constipation, thirst, dizziness, headache, hair loss and pruritus. Although...Full Text Available

2008-10-01

323

Ability of complement to release systemic lupus erythematosus immune complexes from cell receptors.

Ataxin-3, the protein involved in Machado-Joseph disease, is able to bind ubiquitylated substrates and act as a deubiquitylating enzyme in vitro, and it has been involved in the modulation of protein...Full Text Available

324

Ab binding alters gene expression in Cryptococcus neoformans and directly modulates fungal metabolism

Endogenous immune complexes present in sera from 10 different patients with systemic lupus erythematosus (SLE) in an active phase were allowed to bind to Raji cells; the ability of intact complement...Full Text Available

1981-05-01

325

A small RNA promotes siderophore production through transcriptional and metabolic remodeling

Abs facilitate humoral immunity via the classical mechanisms of opsonization, complement activation, Ab-dependent cellular cytotoxicity, and toxin/viral neutralization. There is also evidence that some...Full Text Available

2010-04-01

326

A membrane-associated progesterone-binding protein, 25-Dx, is regulated by progesterone in brain regions involved in female reproductive behaviors

Siderophores are essential factors for iron (Fe) acquisition in bacteria during colonization and infection of eukaryotic hosts, which restrain iron access through iron-binding protein, such as lactoferrin...Full Text Available

2010-08-24

327

A genome-wide study of PDZ-domain interactions in C. elegans reveals a high frequency of non-canonical binding

The ventromedial hypothalamus (VMH) plays a central role in the regulation of the female reproductive behavior lordosis, a behavior dependent upon the sequential activation of receptors for the ovarian...Full Text Available

2000-11-07

328

A functional peptide encoded in the Escherichia coli 23S rRNA.

BackgroundProteins may evolve through the recruitment and modification of discrete domains, and in many cases, protein action can be dissected at the domain level. PDZ domains are...Full Text Available

329

A double antibody solid phase assay for DNA autoantibodies for clinical use.

A pentapeptide open reading frame equipped with a canonical ribosome-binding site is present in the Escherichia coli 23S rRNA. Overexpression of 23S rRNA fragments containing the mini-gene renders cells...Full Text Available

1996-05-28

330

A convenient and sensitive allergy test: IgE crosslinking-induced luciferase expression in cultured mast cells

DNA antoantibodies in serum will bind to antigen-coated polystyrene tubes and can be detected by radiolabelled anti-immunoglobulin. The method is quantitative, gives information on the antibody class...Full Text Available

1976-08-01

331

A Systematic Assessment of MHC Class II Peptide Binding Predictions and Evaluation of a Consensus Approach

BackgroundFor the detection of allergen-specific IgE in sera, solid-phase IgE-binding assays like the CAP test are commonly used. Although such immunochemical methods are very sensitive,...Full Text Available

2010-10-01

332

A Point Mutation in a Domain of Gamma Interferon Receptor 1 Provokes Severe Immunodeficiency

The identification of MHC class II restricted peptide epitopes is an important goal in immunological research. A number of computational tools have been developed for this purpose, but there is a lack...Full Text Available

2008-04-01

333

Synthesis and crystal structure of a new open-framework iron phosphate (NH4)4Fe3(OH)2F2[H3(PO4)4]: Novel linear trimer of corner-sharing Fe(III) octahedra

Gamma interferon (IFN-γ) and the cellular responses induced by it are essential for controlling mycobacterial infections. Most patients bearing an IFN-γ receptor ligand-binding chain...Full Text Available

2001-01-01

334

Spin-orbit splittings in the relativistic mean-field theory

A new iron phosphate (NH4)4Fe3(OH)2F2[H3(PO4)4] has been synthesized hydrothermally at HF concentrations from 0.5 to 1.2 mL. Single-crystal X-ray diffraction analysis reveals its three-dimensional open-framework structure (monoclinic, space group P21/n (No. 14), a=6.2614(13) A, b=9.844(2) A, c=14.271(3) A, ?=92.11(1)o, V=879.0(3) A3). This structure is built from isolated linear trimers of corner-sharing Fe(III) octahedra, which are linked by (PO4) groups to form ten-membered-ring channels along [1 0 0]. This isolated, linear trimer of corner-sharing Fe(III) octahedra, [(FeO4)3(OH)2F2], is new and adds to the diverse linkages of Fe polyhedra as secondary building units in iron phosphates. The trivalent iron at octahedral sites for the title compound has been confirmed by synchrotron Fe K-edge XANES spectra and magnetic measurements. Magnetic measurements also show that this compound exhibit a strong antiferromagnetic exchange below TN=17 K, ...

2010-12-01

335

New coumarin-based sensor molecule for magnesium and calcium ions

We have investigated the effect of the rho tensor coupling on binding energies, matter root-mean-square radii and spin orbit splittings of Ca isotopes in the relativistic mean-field theory with sigma, omega, and rho mesons. It is shown that binding energies and matter root-mean-square radii are insensitive to an alteration in the strength of the rho tensor coupling and an explanation of this is given. We have further shown that inclusion of the rho tensor coupling will give isospin-dependent spin-orbit splittings and this will greatly affect spin-orbit splittings of nuclei near the neutron drip line. (author). Letter-to-the-editor.

1995-11-01

336

British Library Electronic Table of Contents (United Kingdom)

A new coumarin-based sensor molecule (L1) has been synthesized and this was found to bind calcium and magnesium ions more effectively as compared to other alkali/alkaline earth/lanthanide and certain transition metal ions. A significant enhancement in fluorescence intensity was observed on binding to Ca2+ and Mg2+ ions; while a minor quenching was observed for weakly bound Hg2+, Ni2+, Fe3+, and Co2+ ions. PET process, coupled with the ICT process, is proposed to explain the observed spectral response.

2009-01-01

337

Interaction between flavonoid, quercetin and surfactant aggregates with different charges

British Library Electronic Table of Contents (United Kingdom)

The interactions of flavonoid, quercetin with sodium dodecyl sulfate (anionic surfactant) and cetyltrimethyl ammonium bromide (cationic surfactant) micelles were investigated. The average location site of quercetin in different micelles was determined by the cyclic voltammetry method with the aid of molecular optimization. The interaction parameters of quercetin with micelles of different charges such as binding constant K and normal binding energy DG were calculated. Furthermore, the morphologic change of the SDS and CTAB spherical micelles and rod-like micelles upon their interaction with quercetin was also observed.

2006-01-01

338

Structural determinants of alpha-bungarotoxin binding to the sequence segment 181-200 of the muscle nicotinic acetylcholine receptor #alpha# subunit: Effects of cysteine/cystine modification and species-specific amino acid substitution

Mapping of the nucleotide-binding sites in the ADP/ATP carrier of beef heart mitochondria by photolabeling with 2-azido[#alpha#-"3"2P]adenosine diphosphate

The sequence segment 181-200 of the Torpedo nicotinic acetylcholine receptor (nAChR) #alpha#subunit forms a binding site for #alpha#-bungarotoxin (#alpha#-BTX). Synthetic peptides corresponding to the homologous sequences of human, calf, mouse, chicken, frog, and cobra muscle nAChR #alpha#1 subunits were tested for their ability to bind "1"2"5I-#alpha#-BTX, and differences in #alpha#-BTX affinity were determined by using solution (IC_5_0s) and solid-phase (K_ds) assays. Panels of overlapping peptides corresponding to the complete #alpha#1 subunit of mouse and human were also tested for #alpha#-BTX binding, but other sequence segments forming the #alpha#-BTX site were not consistently detectable. The role of a putative vicinal disulfide bound between Cys-192 and -193, relative to the Torpedo sequence, was determined by modifying the peptides with sulfhydryl reagents. Reduction and alkylation of the peptides decreased ...

339

Growth hormone-like factor produced by the tapeworm, Spirometra mansonoides, displaces human growth hormone (hGH) from its receptors on cultured human lymphocytes

2-Azido[#alpha#-"3"2P]adenosine diphosphate (2-azido[#alpha#-"3"2P]ADP) has been used to photolabel the ADP/ATP carrier in beef heart mitochondria. In reversible binding assays carried out in the dark, this photoprobe was found to inhibit ADP/ATP transport in beef heart mitochondria and to bind to two types of specific sites of the ADP/ATP carrier characterized by high-affinity binding (K/sub d/ = 20 #mu#M) and low-affinity binding (K/sub d/ = 400 #mu#M). In contrast, it was unable to bind to specific carrier sites in inverted submitochondrial particles. Upon photoirradiation of beef heart mitochondria in the presence of 2-azido[#alpha#-"3"2P]ADP, the ADP/ATP carrier was covalently labeled. After purification, the photolabeled carrier protein was cleaved chemically by acidolysis or cyanogen bromide and enzymatically with the Staphylococcus aureus V8 protease. In the ADP/ATP carrier ...

340

Dopamine transporter density of the basal ganglia in children with attention deficit hyperactivity disorder assessed with I-123 IPT SPECT

An analogue of hGH isolated from plerocercoids of the tapeworm Spirometra mansonoides displaces ["1"2"5I]hGH from its receptors in rabbit, rat, and hamster liver membranes. Biologically, plerocercoid growth factor (PGF) is more similar to hGH than to other mammalian GH's but has not been shown to bond human cells. Receptors specific for hGH have been described on cultured human lymphocytes (IM-9). In this study, the authors compared the binding of PGF and hGH in IM-9 cells and in rabbit hepatic membranes. IM-9 lymphocytes (12 x 10"6 cells/tube) were incubated with ["1"2"5I]hGH and increasing concentrations of hGH (ng/ml) or PGF (serial dilutions) for 90 min at 30"0 C. Specific binding (B_0 - NSB) was determined for each dose of hGH or PGF and the binding curves were analyzed by logit-log regression. The results show that PGF displaced ["1"2"5I]hGH from human cells in a dose dependent manner (r = 0.98). Based on the IM-9 ...

1986-04-13

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25

341

Copper removal by algal biomass: Biosorbents characterization and equilibrium modelling

Attention deficit hyperactivity disorder (ADHD) has been known as psychiatric disorder in childhood associated with dopamine dysregulation. In present study, we investigated changes in dopamine transporter (DAT) density of the basal ganglias using I-123 N-(3-iodopropen-2-yl) -2-carbomethoxy-3beta-(4-chlorphenyl) tropane (I-123 IPT) SPECT in children with ADHD before and after methylphenidate treatment. Nine drug-naive children with ADHD and seven normal children were included in the study. We performed brain SPECT two hours after the intravenous administration of I-123 IPT and made both quantitative and qualitative analyses using the obtained SPECT data, which were reconstructed for the assessment of specific/nonspecific DAT binding ratios in the basal ganglia. All children with ADHD reperformed (123I)IPT SPECT after treatment with methylphenidate (0.7mg/kg/d) during about 8 weeks. SPECT data reconstructed for the assessment of specific/nonspecific DAT ...

2003-08-01

342

Attention deficit hyperactivity disorder: binding of [{sup 99m}Tc]TRODAT-1 to the dopamine transporter before and after methylphenidate treatment

The general principles of Cu(II) binding to algal waste from agar extraction, composite material and algae Gelidium, and different modelling approaches, are discussed. FTIR analyses provided a detailed description of the possible binding groups present in the biosorbents, as carboxylic groups (D-glucuronic and pyruvic acids), hydroxyl groups (cellulose, agar and floridean starch) and sulfonate groups (sulphated galactans). Potentiometric acid-base titrations showed a heterogeneous distribution of two major binding groups, carboxyl and hydroxyl, following the quasi-Gaussian affinity constant distribution suggested by Sips, which permitted to estimate the maximum amount of acid functional groups (0.36, 0.25 and 0.1 mmol g{sup -1}) and proton binding parameters (pK{sup '}{sub H}=5.0,5.3and4.4;m{sub H} = 0.43, 0.37, 0.33), respectively for algae Gelidium, algal waste and composite material. A ...

2009-04-30

343

Selective metabolic stimulation of the subfornical organ and pituitary neural lobe by peripheral angiotensin II

Involvement of the dopaminergic system has been suggested in patients suffering from attention deficit hyperactivity disorder (ADHD) since the symptoms can be successfully treated with methylphenidate, a potent blocker of the dopamine transporter (DAT). This study reports the findings on the status of the DAT in adults with ADHD before and after commencement of treatment with methylphenidate, as measured using [{sup 99m}Tc]TRODAT-1. Seventeen patients (seven males, ten females, aged 21-64 years, mean 38 years) were examined before and after the initiation of methylphenidate treatment (3 x 5 mg/day). All subjects were injected with 800 MBq [{sup 99m}Tc]TRODAT-1 and imaged 3 h p.i. Single-photon emission tomography (SPET) scans were acquired using a triple-headed gamma camera. For semi-quantitative evaluation of the DAT, transverse slices corrected for attenuation were used to calculate specific binding in the striatum, with the cerebellum used as background ...

2000-10-01

344

Protracted ethanol withdrawal in rats: Tolerance to the anxiolytic effects of diazepam and pentobarbital but not phenobarbital

The subfornical organ is a major receptor area for one of the principal stimuli of thirst, the octapeptide, angiotensin II. In conscious water-sated rats, the authors examined the effects of intravenous infusion of angiotensin II on the rate of glucose utilization in the subfornical organ and in structures anatomically and functionally connected with it. Angiotensin II produced pressor and drinking responses and increased glucose utilization selectively in the subfornical organ and pituitary neural lobe and in no other brain structure. Treatment with the angiotensin II antagonist, sar1-leu8-angiotensin II, before intravenous administration of angiotensin II prevented metabolic stimulation of the subfornical organ and neural lobe. Captopril, an inhibitor of angiotensin-converting enzyme, reduced subfornical organ glucose metabolism to a level similar to that found in control animals. These results demonstrate that peripheral angiotensin II stimulates glucose ...

1985-01-01

345

Polymorphism in HTR3D shows different risks for acute chemotherapy-induced vomiting after anthracycline chemotherapy

Anxiety is a common symptom during ethanol withdrawal contributing to its continuous abuse and alcoholism. Ethanol withdrawal in rats produces an interoceptive discriminative stimulus (IDS) similar to that produced by the anxiogenic drug pentylenetetrazol (PTZ). This stimulus peaks at 12 hours after last dose of ethanol and thereafter the IDS is detected for several days (protracted withdrawal) by sensitization to a probe drug. previously, the authors have shown that during the protracted withdrawal, the IDS is enhanced by GABA receptor antagonists suggesting alteration of brain GABA systems. This report provides further evidence that chronic ethanol alters GABAergic systems. Rats were trained to discriminate PTZ (20 mg/kg, ip) from saline. Diazepam, pentobarbital and phenobarbital blocked the PTZ-IDS dose dependently. Ethanol, 4.5% w/v, was then given in a nutritionally complete diet for a week. On termination of the ethanol diet, rats exhibited signs and symptoms ...

1990-02-26

346

British Library Electronic Table of Contents (United Kingdom)

Aims: Serotonin (5-hydroxytryptamine 3; 5-HT3) receptors are involved in chemotherapy-induced nausea and vomiting (CINV), and 5-HT3 antagonists are part of the `gold standard' antiemetic treatment during chemotherapy. We investigated the correlation of common variants in 5-HT3 receptor subunit genes with the occurrence of CINV. Materials & methods: A total of 110 previously characterized chemotherapy-naive women with primary breast cancer treated with anthracycline-containing chemotherapy served as a study group for mutational analysis by direct sequencing. Eight common SNPs in the 5-HT3 receptor genes, HTR3A, HTR3B, HTR3D and HTR3E, were selected for association analysis. Results: A nonsynonymous variant in HTR3D, p.G36A (rs6443930), was found to be over-represented in nonresponders, assu...

2010-01-01

347

CHRNA5 as negative regulator of nicotine signaling in normal and cancer bronchial cells: effects on motility, migration and p63 expression

British Library Electronic Table of Contents (United Kingdom)

Genome-wide association studies have linked lung cancer risk with a region of chromosome 15q25.1 containing CHRNA3, CHRNA5 and CHRNB4 encoding a3, a5 and b4 subunits of nicotinic acetylcholine receptors (nAChR), respectively. One of the strongest associations was observed for a non-silent single-nucleotide polymorphism at codon 398 in CHRNA5. Here, we have used pharmacological (antagonists) or genetic (RNA interference) interventions to modulate the activity of CHRNA5 in non-transformed bronchial cells and in lung cancer cell lines. In both cell types, silencing CHRNA5 or inhibiting receptors containing nAChR a5 with a-conotoxin MII exerted a nicotine-like effect, with increased motility and invasiveness in vitro and increasing calcium influx. The effects on motility were enhanced by addit...

2011-01-01

348

A Phase III Extension Trial With a 1-Arm Crossover From Leuprolide to Degarelix: Comparison of Gonadotropin-Releasing Hormone Agonist and Antagonist Effect on Prostate Cancer

British Library Electronic Table of Contents (United Kingdom)

PurposeWe investigated the efficacy and safety of degarelix treatment and the effects of switching from leuprolide to degarelix in an ongoing extension study with a median 27.5-month followup of a pivotal 1-year prostate cancer trial. Materials and MethodsPatients who completed a 1-year pivotal phase III trial continued on the same monthly degarelix maintenance dose (160 or 80 mg in 125 each), or were re-randomized from leuprolide 7.5 mg to degarelix 240/80 mg (69) or 240/160 mg (65). Data are shown on the approved degarelix 240/80 mg dose. The primary end point was safety/tolerability and the secondary end points were testosterone, prostate specific antigen, luteinizing hormone and follicle-stimulating hormone responses, and prostate specific antigen failure and progression-free survival....

2011-01-01

349

Inflammatory spine disease as a cause of back pain; Entzuendliche Wirbelsaeulenerkrankungen als Ursache fuer Rueckenschmerzen

Disruption of contact inhibition in rat liver epithelial cells by various types of AhR ligands

The aim of this review is to evaluate the role of inflammatory spine disease in patients with chronic back pain. The contribution of imaging modalities for the diagnostic evaluation of back pain is discussed. A systematic literature search based on the classification of seronegative spondyloarthropathies and rheumatoid arthritis was performed. The results of this search and the experiences in a large collective of rheumatological patients are analyzed. The prevalence of rheumatoid arthritis (1-2%) is comparable to that of spondyloarthropathies (1.9%). The etiology of these entities is not fully elucidated. Magnetic resonance imaging is increasingly used for early detection and surveillance of therapy with TNF-{alpha} antagonists. Bone marrow edema, which is only detectable with MRI, represents an early sign of inflammation. Therapy with TNF-{alpha} antagonists is based on clinical and laboratory criteria, and signs of inflammation in MRI. MRI ...

2006-06-15

350

Epitope mapping and functional analysis of sigma A and sigma NS proteins of avian reovirus

The maintenance of a balance between cell gain and cell loss is essential for proper liver function. The exact role of aryl hydrocarbon receptor (AhR) in regulating cell proliferation and apoptosis of liver cells remains unclear, since ligand-dependent activation of AhR has been shown to induce cell cycle arrest, proliferation, differentiation or apoptosis, depending on the cellular model used. AhR can directly interact with retinoblastoma protein in hepatic cells, forming protein complexes that can efficiently block cell cycle progression by inducing G1 arrest, or to induce the expression of inhibitors of cyclin-dependent kinases, such as p271. On the other hand, it has been suggested that AhR could play a stimulatory role in cell proliferation, either directly or by mediating a release from contact inhibition. It is now generally accepted that progenitor cells exist in the liver, are activated in various liver diseases and can form a potential target cell population for both tumor ...

2004-09-15

351

Two Functional S100A4 Monomers Are Necessary for Regulating Nonmuscle Myosin-IIA and HCT116 Cell Invasion.

We have previously shown that avian reovirus (ARV) #sigma#A and #sigma#NS proteins possess dsRNA and ssRNA binding activity and suggested that there are two epitopes on #sigma#A (I and II) and three epitopes (A, B, and C) on #sigma#NS. To further define the location of epitopes on #sigma#A and #sigma#NS proteins and to further elucidate the biological functions of these epitopes by using monoclonal antibodies (MAbs) 62, 1F9, H1E1, and 4A123 against the ARV S1133 strain, the full-length and deletion fragments of S2 and S4 genes of ARV generated by polymerase chain reaction (PCR) were cloned into pET32 expression vectors and the fusion proteins were overexpressed in Escherichia coli BL21 strain. Epitope mapping using MAbs and E. coli-expressed deletion fragments of #sigma#A and #sigma#NS of the ARV S1133 strain, synthetic peptides, and the cross reactivity of MAbs to heterologous ARV strains demonstrated that epitope II on #sigma#A was located at amino acid residues ...

2005-02-20

352

Synthesis and characterization of ["1"2"5I]-N-(N-benzylpiperidin-4-YL)-4-iodobenz amide, a potential high affinity sigma ligand for imaging breast cancer

S100A4, a member of the Ca(2+)-activated S100 protein family, regulates the motility and invasiveness of cancer cells. Moreover, high S100A4 expression levels correlate with poor patient survival in several cancers. Although biochemical, biophysical, and structural data indicate that S100A4 is a noncovalent dimer, it is unknown if two functional S100A4 monomers are required for the productive recognition of protein targets and the promotion of cell invasion. To address this question, we created covalently linked S100A4 dimers using a glycine rich flexible linker. The single-chain S100A4 (sc-S100A4) proteins exhibited wild-type affinities for calcium and nonmuscle myosin-IIA, retained the ability to regulate nonmuscle myosin-IIA assembly, and promoted tumor cell invasion when expressed in S100A4-deficient colon carcinoma cells. Mutation of the two calcium-binding EF-hands in one monomer, while leaving the other monomer intact, caused a 30-60-fold reduction in ...

2011-07-13

353

Propanil-induced methemoglobinemia and hemoglobin binding in the rat

Three regio-isomers of N-(N-benzylpiperidin-4-yl)-4-iodobenzamide, IBP, were prepared and evaluated for their sigma affinities. All three isomers (2, 3, and 4-substituted) showed high affinities for sigma-1 receptors in guinea pig brain membranes (Ki - 1.64 nM, 3.02 nM, 1.70 nM respectively) against ["3H]-(+)-pentazocine, a sigma-1 selective ligand. 2-IBP and 4-IBP showed modest affinities for sigma-2 sites in rat liver (Ki = 29.6 nM. 25.2 nM respectively) against ["3H]DTG in the presence of dextrallorphan to mask sigma-1 sites. The homologous competition binding studies of 4-["1"2"5I]BP in MCF-7 human breast tumor cells showed high affinity dose-dependent binding. Competition binding studies with haloperidol and DTG also showed a high affinity binding (Ki = 4.6 nM, 60 nM respectively), demonstrating the sigma specificity. The saturation binding (Scatchard analysis) of ["3H]DTG with ...

1994-08-21

354

Platelet fibrinogen binding in Basset Hound Hereditary Thrombopathy

Administration of [ring-U-14C]propanil (3,4-dichloropropionanilide) to male Sprague-Dawley rats (30, 100, and 300 mg/kg, ip) increased the formation of methemoglobin at the two highest doses. Following a propanil dose of 100 mg/kg, methemoglobin formation attained a maximum level of 5% by 1.5 hr and declined to normal levels (approximately 2.5%) by 12 hr. Hemoglobin binding attained a maximum level of 50 pmol/mg protein by 12 hr, and remained constant for 24 hr. Following a propanil dose of 300 mg/kg, methemoglobin formation attained a maximum level of 24% by 4.5 hr, and declined to a level of 5% by 24 hr. Hemoglobin binding attained a maximum level of 425 pmol/mg protein by 12 hr, and remained constant for 24 hr. Hemoglobin binding was also detected at the lowest propanil dose (10 pmol/mg protein) even though methemoglobin formation was not observed. HPLC analysis of alkaline-treated hemoglobin from propanil-treated rats ...

355

Crystal and solution structures of an odorant-binding protein from the southern house mosquito complexed with an oviposition pheromone

Platelets from dogs with Basset Hound Hereditary Thrombopathy (BHT) display a thrombasthenia-like aggregation defect but have been shown to have normal amounts of platelet membrane glycoproteins IIb and IIIa (GP IIb-IIIa). In order to investigate the possibility of a functionally abnormal GPIIb-IIIa complex, which might be unable to bind fibrinogen after stimulation, fibrinogen binding in BHT was evaluated. Two canine fibrinogen preparations were used, one from BHT dogs and one from normal control dogs, as well as a human fibrinogen preparation. Platelets from BHT and normal dogs were activated with 1 x 10/sup -5/M ADP in the presence of /sup 125/I-labeled fibrinogen and the surface bound radioactivity quantitated. For all fibrinogen preparations, the amount of fibrinogen bound by BHT platelets was not significantly different than that bound by normal dog platelets. BHT platelets bound 23,972 +/- 3612 and normal dog platelets bound 23,033 +/- ...

1986-03-01

356

Characterization of chicken octamer-binding proteins demonstrates that POU domain-containing homeobox transcription factors have been highly conserved during vertebrate evolution

Culex mosquitoes introduce the pathogens responsible for filariasis, West Nile virus, St. Louis encephalitis, and other diseases into humans. Currently, traps baited with oviposition semiochemicals play an important role in detection efforts and could provide an environmentally friendly approach to controlling their populations. The odorant binding proteins (OBPs) in the female's antenna play a crucial, if yet imperfectly understood, role in sensing oviposition cues. Here, we report the X-ray crystallography and NMR 3D structures of OBP1 for Culex quinquefasciatus (CquiOBP1) bound to an oviposition pheromone (5R,6S)-6-acetoxy-5-hexadecanolide (MOP). In both studies, CquiOBP1 had the same overall six-helix structure seen in other insect OBPs, but a detailed analysis revealed an important previously undescribed feature. There are two models for OBP-mediated signal transduction: (i) direct release of the pheromone from an internal binding ...

2010-11-15

357

A single amino acid substitution (R441A) in the receptor-binding domain of SARS coronavirus spike protein disrupts the antigenic structure and binding activity

The DNA sequence motif ATTTGCAT (octamer) or its inverse complement has been identified as an evolutionarily conserved element in the promoter region of immunoglobulin genes. Two major DNA-binding proteins that bind in a sequence-specific manner to the octamer DNA sequence have been identified in mammalian species--a ubiquitously expressed protein (Oct-1) and a lymphoid-specific protein (Oct-2). During characterization of the promoter region of the chicken immunoglobulin light chain gene, the authors identified two homologous octamer-binding proteins in chicken B cells. when the cloning of the human gene for Oct-2 revealed it to be a member of a distinct family of homeobox genes, they sought to determine if the human Oct-2 cDNA could be used to identify homologous chicken homeobox genes. Using a human Oct-2 homeobox-specific DNA probe, they were able to identify 6-10 homeobox-containing genes in the chicken genome, ...

1990-02-01

358

The cluster structure of the inner crust of neutron stars in the Hartree-Fock-Bogoliubov approach

The spike (S) protein of severe acute respiratory syndrome coronavirus (SARS-CoV) has two major functions: interacting with the receptor to mediate virus entry and inducing protective immunity. Coincidently, the receptor-binding domain (RBD, residues 318-510) of SAR-CoV S protein is a major antigenic site to induce neutralizing antibodies. Here, we used RBD-Fc, a fusion protein containing the RBD and human IgG1 Fc, as a model in the studies and found that a single amino acid substitution in the RBD (R441A) could abolish the immunogenicity of RBD to induce neutralizing antibodies in immunized mice and rabbits. With a panel of anti-RBD mAbs as probes, we observed that R441A substitution was able to disrupt the majority of neutralizing epitopes in the RBD, suggesting that this residue is critical for the antigenic structure responsible for inducing protective immune responses. We also demonstrated that the RBD-Fc bearing R441A mutation could not ...

2006-05-26

359

Suppression of receptors for prolactin and estrogen in rat liver due to treatment with the growth hormone analogue produced by the tapeworm Spirometra mansonoides.

We analyse how the structure of the inner curst is influenced by the pairing correlations. The inner-crust matter, formed by nuclear clusters immersed in a superfluid neutron gas and ultra-relativistic electrons, is treated in the Wigner-Seitz approximation. The properties of the Wigner-Seitz cells, i.e., their neutron to proton ratio and their radius at a given baryonic density, are obtained from the energy minimization at beta equilibrium. To obtain the binding energy of baryonic matter we perform Skyrme-HFB calculations with zero-range density-dependent pairing forces of various intensities. We find that the Wigner-Seitz cells have much smaller numbers of protons compared to previous calculations. For the dense cells the binding energy of the configurations with small proton numbers do not converge to a well-defined minimum value which precludes the determination of their structure. We show that for these cells there is a significant ...

2011-01-01

360

Single-molecular analysis of the binding state of myosin V and actin

Somatogenic hormones play an important role in regulation of receptors for prolactin (PRL) and estrogen. Plerocercoids of the tapeworm, S. mansonoides produce a factor which mimics some, but not all of the actions reported for GH. Intact female rats were subjected to a constant infusion of plerocercoid growth factor (PGF) via a subcutaneous infection for two weeks to determine if PGF influences receptors for PRL, GH or estradiol. The rate of weight gain in the PGF-treated rats was accelerated in spite of a marked reduction in serum GH. Partially-purified PGF specifically displaced [125I]hGH from rat liver receptors but microsomes prepared from rats treated with PGF specifically bound significantly less [125I]hGH than microsomes from control rats. The reduction in [125I]hGH binding was not due to occupancy or to a change in affinity but to a suppression in receptor concentration. Scatchard analysis of [3H]estradiol binding in rat liver cytosols ...

1986-01-01

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25

361

Radioiodinated peanut lecitin: A potential radiopharmaceutical for immunodetection of carcinoma expressing the T antigen

A class-V myosin, myosin V, one of 18 known classes of actin-based motor proteins, plays a role in transporting organelles within a cell. Unlike myosin-II, which functions as an assembly in the thick filaments of muscle, myosin V is a two-headed processive motor protein, which functions as a single molecule: myosin V performs many consecutive steps before it detaches from an actin filament accompanied by catalytic cycles of ATP (adenosine 5'-triphosphate) ase. The mechanism of such chemomechanical steps is explained by a 'Hand-over-hand model' in which two heads of myosin V alternately repeat single-headed and double-headed bindings with an actin filament. To investigate the binding state of myosin V at several key nucleotide states during ATP hydrolysis, we measured the mechanical properties of a single myosin V - actin complex by applying an external load with optical trap.

2006-03-21

362

Purification and analysis of RNA polymerase II transcription factors by using wheat germ agglutinin affinity chromatography.

The Thomsen-Friedenreich (T) antigen, #betta#-D-Gal-(1->3)-#alpha#-D-GalNAc, is exposed in reactive form on many human adenocarcinomata, but not on corresponding benign tissues. Peanut lectin (PNA) has a strong binding affinity for the T antigen and reportedly binds preferentially to certain malignant tissues. We investigated the potential of radio-labelled PNA as a tumour localising agent in an animal model system using a mouse lymphoma (RI) shown to bind fluorescein-labelled PNA in vitro. The radio-iodinated lectin showed good tumour localisation and rapid blood clearance. Clear images of tumours were obtained, in serial scintigraphic imaging, by 24 and 48 h. No blood background subtraction was necessary. Biodistribution studies revealed tumour to blood ratios in mice were 6:1 (at 24 h) and 17:1 (at 48 h), and tumour to muscle ratios were 34:1 (at 24 h) and 40:1 (at 48 h). Rapid in vivo breakdown of _1_2_5I-PNA led to ...

1983-01-01

363

NADP Regulates the Yeast GAL Induction System

We recently found that many RNA polymerase II transcription factors are modified with N-acetylglucosamine residues. These sugar moieties confer upon transcription factors an ability to bind the lectin wheat germ agglutinin. We have taken advantage of this interaction to devise a purification procedure for the "GC-box" binding transcription factor Sp1. Crude nuclear extracts are first subjected to wheat germ agglutinin affinity chromatography and then subjected to sequence-specific DNA affinity chromatography. The Sp1 protein purified by this procedure is at least 95% pure, and the overall recovery is greater than 80%. In addition to yielding larger quantities of Sp1 than conventional schemes, the new purification procedure is also simpler and more rapid. We show that wheat germ agglutinin affinity chromatography can also be used to purify the glycosylated forms of the CCAAT-binding transcription factor. Thus, wheat germ ...

1989-03-01

364

Motor Proteins Have Highly Correlated Brownian Engines

Transcriptional regulation of the galactose-metabolizing genes in Saccharomyces cerevisiae depends on three core proteins: Gal4p, the transcriptional activator that binds to upstream activating DNA sequences (UASGAL); Gal80p, a repressor that binds to the carboxyl terminus of Gal4p and inhibits transcription; and Gal3p, a cytoplasmic transducer that, upon binding galactose and adenosine 5'-triphosphate, relieves Gal80p repression. The current model of induction relies on Gal3p sequestering Gal80p in the cytoplasm. However, the rapid induction of this system implies that there is a missing factor. Our structure of Gal80p in complex with a peptide from the carboxyl-terminal activation domain of Gal4p reveals the existence of a dinucleotide that mediates the interaction between the two. Biochemical and in vivo experiments suggests that nicotinamide adenine dinucleotide phosphate (NADP) plays a key role in the initial ...

2008-01-01

365

Evolution of a molecular switch: universal bacterial GTPases regulate ribosome function.

Two headed motor proteins, such as kinesin and dynein, hidrolyze environmental ATP in order to propel unidirectionally along cytoskeletal filaments such as microtubules. In the case of kinesin, protein heads bind primarily on the alpha tubulin site of asymmetric alpha-beta 8nm-long tubulin dimers that constitute the microtubular protofilaments. Kinesin dimers overcome local binding forces up to 5pN and are known to move on protofilaments with ATP concentration-dependent speeds while hydrolizing on average one ATP molecule per 8nm step. The salient features of protein trajectories are the distinct abrupt usually 8nm-long steps from one tubulin dimer to the next interlaced with long quiescent binding periods at a tubulin site. Discrete walks of this type are characterized by substantially reduced variances compared to pure biased random walks, and as a result rule out flashing-type ratchet models as possible mechanisms for ...

1998-01-01

366

Biophysical analysis of DNA modified by 1,2-diaminocyclohexane platinum(II) complexes

The GTPases comprise a protein superfamily of highly conserved molecular switches adapted to many diverse functions. These proteins are found in all domains of life and often perform essential roles in fundamental cellular processes. Analysis of data from genome sequencing projects demonstrates that bacteria possess a core of 11 universally conserved GTPases (elongation factor G and Tu, initiation factor 2, LepA, Era, Obg, ThdF/TrmE, Ffh, FtsY, EngA and YchF). Investigations aimed at understanding the function of GTPases indicate that a second conserved feature of these proteins is that they elicit their function through interaction with RNA and/or ribosomes. An emerging concept suggests that the 11 universal GTPases are either necessary for ribosome function or transmitting information from the ribosome to downstream targets for the purpose of generating specific cellular responses. Furthermore, it is suggested that progenitor GTPases were early regulators of RNA function and may have ...

2001-07-01

367

Artificial receptor for peptide recognition in protic media: The role of metal ion coordination

Modification of DNA and double-stranded deoxyoligonucleotides with antitumor 1,2-diamino-cyclohexanedinitroplatinum(II) (Pt-dach) complexes was investigated with the aid of physico-chemical methods and chemical probes of nucleic acid conformation. The three Pt-dach complexes were used which differed in isomeric forms of the dach non-leaving ligand-Pt(1R,2R-dach), Pt(1S,2S-dach) and Pt(1R,2S-dach) complexes. The latter complex has lower antitumor activity than the other two Pt-dach complexes. Pt(1R,2S-dach) complex exhibits the slowest kinetics of its binding to DNA and of the conversion of monofunctional binding to bifunctional lesions. The anomalously slow electrophoretic mobility of multimers of the platinated and ligated oligomers suggests that bifunctional binding of Pt-dach complexes to a d(GG) site within double-stranded oligonucleotides induces bending of the oligomer. It is proposed that different effects of the ...

1992-01-25

368

Performance following a 500-675 rad neutron pulse. Report for June 1981-January 1984

The production of molecularly imprinted polymers (MIPs) for the recognition of C-terminal cholecystokinin pentapeptide (CCK-5) in the presence of metal ion is reported. The MIPs were produced under the same molar ratio of template to monomers (acrylamide, N,N'-methylene bisacrylamide) in the presence or absence of nitrilotriacetic acid-nickel (Ni-NTA) complex. Scanning electron microscopy images of MIPs were obtained in an attempt to correlate the adsorption characteristics with polymer's morphology. Subsequently Ni2+ was removed and substituted by other divalent ions such as Mg2+, Fe2+, Zn2+, Co2+ and Cu2+. It was found that polymers containing the metal ion complex with the order Fe-NTA, Ni-NTA and Cu-NTA presented lower dissociation constant values than the rest thus exhibiting stronger guest binding activity. The percentage of theoretical maximum binding sites Bmax was almost the same for these ions, indicating that the ion-template ...

2008-08-25

369

Extraction of rare earths by carbonic acids melts

A three-light, three-lever discrete avoidance behavioral task was initiated to study the effects of a 500-675 rad neutron pulse upon performance. Eight primates performed the task for 4 h(3.5 h postexposure) on exposure day and for 4 h on each of 3 d postexposure. For the exposure day, five subjects had a decrease in correct responses, seven had increased reaction times, and six experienced productive emesis within 3.5 hours postexposure. Although the performance degradations were not severe, these data suggest that the performance of time critical tasks could be significantly impaired.

1985-06-01

370

Extraction of americium of different oxidation states in two-phase aqueous system based on polyethylene glycol

Extraction of rare earths (La, Ce, Pr, Eu, Gd, Er, Yb) from nitrate solutions by melts of carboxylic acids of the C/sub 17/-C/sub 20/ fraction and stearic acid with paraffin, depending on the temperature (60-90 deg), phase contact time and their volume ratio (O:B from 1:5 up to 1:100), pH of the aqueous phase (2-6), rare earth concentration (10/sup -6/-10/sup -3/ m) is studied. It is shown that in the whole concentration range investigated rare earths are extracted quantitatively into the carboxylic acid melt of C/sub 17/-C/sub 20/ fraction at the equilibrium value of pH>=3.8, while into the melt of 0.1 M stearic acid in paraffin at pH>=4.5.

1980-10-01

371

Enzymatic solubilization of a pectinaceous dietary fiber fraction from potato pulp: Optimization of the fiber extraction process

Americium extraction in different oxidation states in two-phase aqueous system based on polyethylene glycol is investigated. Conditions for quantitative extraction of americium (3) and americium (5) from ammonium sulfate solutions within pH=3-5 interval in the presence of arsenazo 3 are found. Composition of the produced americium complexes with reagent is determined; americium (3) interacts with arsenazo 3 in ammonium sulfate solutions with the formation of MeR and Me_2R composition complexes. Absorption spectrum characteristics of americium (3) and- (5) complexes with arsenazo 3 in ammonium sulfate solutions and extracts based polyethylene glycol aqueous solutions are given. Molar extinction coefficients of americium complexes with arsenazo (3) in these solutions are determined.

1987-01-01

372

British Library Electronic Table of Contents (United Kingdom)

Upgrading of potato pulp, a byproduct stream from industrial manufacture of potato starch, is important for the continued economic competitiveness of the potato starch industry. The major part of potato pulp consists of the tuber plant cell wall material which is particularly rich in galactan branched rhamnogalacturonan I type pectin. In the work reported here, the release of high-molecular weight pectinaceous dietary fiber polysaccharides from starch free potato pulp was accomplished by use of a multicomponent pectinase preparation from Aspergillus aculeatus (Viscozyme L). The enzyme reaction conditions for the solubilization were optimized via a surface response design to be addition of 0.27% Viscozyme L by weight of potato pulp substrate dry matter, 1h treatment at pH 3.5, 62.5degreeC. ...

2009-01-01

373

Crystal structure of the human centromeric nucleosome containing CENP-A

British Library Electronic Table of Contents (United Kingdom)

In eukaryotes, accurate chromosome segregation during mitosis and meiosis is coordinated by kinetochores, which are unique chromosomal sites for microtubule attachment. Centromeres specify the kinetochore formation sites on individual chromosomes, and are epigenetically marked by the assembly of nucleosomes containing the centromere-specific histone H3 variant, CENP-A. Although the underlying mechanism is unclear, centromere inheritance is probably dictated by the architecture of the centromeric nucleosome. Here we report the crystal structure of the human centromeric nucleosome containing CENP-A and its cognate ?-satellite DNA derivative (147 base pairs). In the human CENP-A nucleosome, the DNA is wrapped around the histone octamer, consisting of two each of histones H2A, H2B, H4 and CENP...

2011-01-01

374

A comparison of thermal maturity parameters between freely extracted hydrocarbons (Bitumen I) and a second extract (Bitumen II) from within the kerogen matrix of Permian and Triassic sedimentary rocks

British Library Electronic Table of Contents (United Kingdom)

In this study we compared various maturity dependent aromatic, steroid and triterpenoid hydrocarbon ratios in bitumens that are freely extractable from sedimentary rocks (Bitumen I) with those in second extracts that comprised hydrocarbons closely associated with the kerogen/mineral matrix (Bitumen II). Bitumen II was released through kerogen isolation and demineralisation using HCl and HF/H3BO3. The samples studied, although of similar age, come from different localities. They represent a range of facies and two kerogen types (II and III), and all were deposited under marine conditions. The results show that the more stable b isomers of methylnaphthalene (MN) and methylphenanthrene (MP) are relatively more abundant in Bitumen II. The difference between the methylnaphthalene ratio (MNR) of...

2010-01-01

375

The expression profile of TLR9 mRNA and CpG ODNs immunostimulatory actions in the teleost gilthead seabream points to a major role of lymphocytes

British Library Electronic Table of Contents (United Kingdom)

Abstract. The potential effects of synthetic unmethylated oligodeoxynucleotides (ODN) containing CpG motifs, mimicking bacterial DNA, has never been evaluated on the immune response in the teleost fish gilthead seabream (Sparus aurata), the most important fish species in Mediterranean aquaculture. First, binding and competition studies have demonstrated that binding is saturated and promiscuous, suggesting the participation of several receptors. Moreover, leucocyte cytotoxic (NCC) activity, production of ROIs (reactive oxygen intermediates), and expression of immune-relevant genes was greatly primed by ODNs. Focusing on the mechanism, the TLR9 gene is widely distributed in seabream tissues and differently regulated in vitro by several stimuli. Moreover, and for the first time in fish, TLR9...

2008-01-01

376

Sorbent extraction and high performance liquid chromatography (HPLC) of homidium bromide and isometamidium chloride in bovine plasma

Some sulfonamide drugs inhibit ATPase activity of heat shock protein 90: investigation by docking simulation and experimental validation

Homidium bromide and isometamidium chloride are used extensively in the treatment of bovine trypanosomiasis in Africa, but no specific and sensitive method to detect the drug in plasma has been published yet. Comparing the methods of other investigators it was found that they could not overcome the protein binding of these drugs which reduced the available and determined drug to 10% of the real concentrations. These techniques overcome the protein binding by enzyme digestion and an alteration of the pH before adding the sample directly on clean-up columns. Drug recover rates above 80% were obtained. For the detection, the HPLC was employed using a C18 reversed phase analytical column and UV detection, determining both drugs as intact molecules. (author).

1992-01-01

377

British Library Electronic Table of Contents (United Kingdom)

Eight selected sulfonamide drugs were investigated as inhibitors of heat shock protein 90 (Hsp90). The investigation included simulated docking experiments to fit the selected compounds within the binding pocket of Hsp90. The selected molecules were found to readily fit within the ATP-binding pocket of Hsp90 in low-energy poses. The sulfonamides torsemide, sulfathiazole, and sulfadiazine were found to inhibit the ATPase activity of Hsp90 with IC50 values of 1.0, 2.6, and 1.5 mM, respectively. Our results suggest that these well-established sulfonamides can be good leads for subsequent optimization into potent Hsp90 inhibitors.

2011-01-01

378

On the binding effect of air pollution concentration values of the Technical Code Clean Air (TA Luft) in favor of the plant operator. Zur Bindungswirkung der Emissionswerte der TA Luft zugunsten des Anlagenbetreibers

Metallointercalators and Metalloinsertors

The dogmatic and constitutional basis as well as points of definition concerning the Technical Code Clean Air (TA Luft) are explained at first, followed by an assessment of the air pollution concentrations within the overall complex of the air pollution abatement measures, and an analyses of air pollution concentrations as a concretization of the state-of-the-art. In connection with the differentiation of the various applicability levels of TA Luft, the inhouse validy for authorities, the importance for law courts and, finally, the external binding effect for plant operators and possible third parties are discussed. At the center of attention are questions concerning validity claims and validity possibilities. (HSCH).

1991-01-01

379

Metallo-intercalators and metallo-insertors.

Since the elucidation of the structure of double helical DNA, the construction of small molecules that recognize and react at specific DNA sites has been an area of considerable interest. In particular, the study of transition metal complexes that bind DNA with specificity has been a burgeoning field. This growth has been due in large part to the useful properties of metal complexes, which possess a wide array of photophysical properties and allow for the modular assembly of an ensemble of recognition elements. Here we review recent experiments in our laboratory aimed at the design and study of octahedral metal complexes that bind DNA non-covalently and target reactions to specific sites. Emphasis is placed both on the variety of methods employed to confer site-specificity and upon the many applications for these complexes. Particular attention is given to the family of complexes recently designed that target single base mismatches in duplex ...

2007-09-20

380

Mannose-binding lectin codon 54 gene polymorphism in relation to risk of nosocomial invasive fungal infection in preterm neonates in the neonatal intensive care unit

Since the elucidation of the structure of double helical DNA, the construction of small molecules that recognize and react at specific DNA sites has been an area of considerable interest. In particular, the study of transition metal complexes that bind DNA with specificity has been a burgeoning field. This growth has been due in large part to the useful properties of metal complexes, which possess a wide array of photophysical attributes and allow for the modular assembly of an ensemble of recognition elements. Here we review recent experiments in our laboratory aimed at the design and study of octahedral metal complexes that bind DNA non-covalently and target reactions to specific sites. Emphasis is placed both on the variety of methods employed to confer site-specificity and upon the many applications for these complexes. Particular attention is given to the family of complexes recently designed that target single base mismatches in duplex ...

2007-09-20

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25

381

British Library Electronic Table of Contents (United Kingdom)

Objective. Preterm neonates are susceptible to infection due to a combination of sub-optimal immunity and increased exposure to invasive organisms. Invasive fungal infections are associated with significant morbidity and mortality among preterm infants cared for in the neonatal intensive care unit (NICU). Mannose-binding lectin (MBL) is a component of the innate immune system, which may be especially important in the neonatal setting. The objective of this study was to investigate the presence of any association between MBL gene polymorphism and nosocomial invasive fungal infection in preterm neonates. Methods. Codon 54 (B allele) polymorphism in exon 1 of the MBL gene was investigated in 31 patients diagnosed as nosocomial invasive fungal infection and 30 control preterm neonates. Results...

2011-01-01

382

Exploring the binding of the strong organic acceptor F{sub 4}TCNQ to coinage metals

Evidence for involvement of the astrocytic benzodiazepine receptor in the mechanism of action of convulsant and anticonvulsant drugs

Organic/metal interface properties are of high interest for the application of molecular (sub)monolayers to modify surface properties. They are applied for, e.g., molecular electronics, chemical sensing, or the tuning of injection barriers in organic electronic devices. We present a joint theoretical and experimental study of F{sub 4}TCNQ adsorbed on Cu(111). The electronic and structural properties were determined by ultraviolet photoelectron spectroscopy (UPS) and X-ray standing wave (XSW) measurements. To better understand the complex process of binding, we modelled the system using density-functional theory. We find forward-donation from the lone pairs of the molecule into metallic states and back-donation from the metal into the LUMO of the molecule. The data on Cu(111) are compared to F4TCNQ on Au(111) and Ag(111) as well as to investigations of pyrenetetraone on various coinage metals.

2008-07-01

383

Electron binding to isolated polar molecules and molecular dipole assemblies

The anticonvulsant drugs carbamazepine, phenobarbital, trimethadione, valproic acid and ethosuximide at pharmacologically relevant concentrations inhibit (/sup 3/H)diazepam binding to astrocytes in primary cultures but have much less effect on a corresponding preparation of neurons. Phenytoin as well as pentobarbital (which is not used chronically as an anticonvulsant) are equipotent in the two cell types. The convulsants picrotoxinin and pentylenetetrazol, the convulsant benzodiazepine RO 5-3663 and the two convulsant barbiturates DMBB and CHEB similarly inhibit diazepam binding to astrocytes but have little effect on neurons. On the basis of these findings it is suggested that these convulsants and anticonvulsants owe at least part of their effect to an interaction with the astrocytic benzodiazepine receptor, perhaps by interference with a calcium channel.

1988-01-01

384

ECRbase: Database of Evolutionary Conserved Regions, Promoters, and Transcription Factor Binding Sites in Vertebrate Genomes

In a sufficiently large cluster of several polar molecules, collective interactions lead to localization or 'solvation' of electrons. The existence of the solvated electron is known since 1863 in liquid ammonia and since 1962 for liquid water. In 1984, electron localization in clusters was experimentally demonstrated in (H_2O)_N_#>=#_1_1 and (NH_3)_N_#>=#_3_4 clusters. In cooperation with K. Bowen, we recently initiated a test of the theory of electron binding by a dipole and a new ground state dipole bound dimer anion, (H_2O..NH_3), was predicted and observed. We here describe results of a search for new dipole-bound and solvated electron systems. (author).

1994-03-20

385

Constrained NBMPR analogue synthesis, pharmacophore mapping and 3D-QSAR modeling of equilibrative nucleoside transporter 1 (ENT1) inhibitory activity

Evolutionary conservation of DNA sequences provides a tool for the identification of functional elements in genomes. We have created a database of evolutionary conserved regions (ECRs) in vertebrate genomes entitled ECRbase that is constructed from a collection of pairwise vertebrate genome alignments produced by the ECR Browser database. ECRbase features a database of syntenic blocks that recapitulate the evolution of rearrangements in vertebrates and a collection of promoters in all vertebrate genomes presented in the database. The database also contains a collection of annotated transcription factor binding sites (TFBS) in all ECRs and promoter elements. ECRbase currently includes human, rhesus macaque, dog, opossum, rat, mouse, chicken, frog, zebrafish, and two pufferfish genomes. It is freely accessible at http://ECRbase.dcode.org.

2006-08-08

386

British Library Electronic Table of Contents (United Kingdom)

Conformationally constrained analogue synthesis was undertaken to aid in pharmacophore mapping and 3D-QSAR analysis of nitrobenzylmercaptopurine riboside (NBMPR) congeners as equilibriative nucleoside transporter 1 (ENT1) inhibitors. In our previous study [J. Med. Chem. 2003, 46, 831-837], novel regioisomeric nitro-1,2,3,4-tetrahydroisoquinoline conformationally constrained analogues of NBMPR were synthesized and evaluated as ENT1 ligands. 7-NO2-1,2,3,4-Tetrahydroisoquino-2-yl purine riboside was identified as the analogue with the nitro group in the best orientation at the NBMPR binding site of ENT1. In the present study, further conformational constraining was introduced by synthesizing 5prime-O,8-cyclo derivatives. The flow cytometrically determined binding affinities indicated that the...

2008-01-01

387

Characterization of acid sites in pentasil zeolites by x-ray photolectron spectroscopy

Methionine kinetics in adult men: effects of dietary betaine on L-[2H3-methyl-1-13C]methionine

The N{sub 1s} XPS band of pyridine chemisorbed on Al-ZSM-5 zeolite was found to be properly deconvoluted into three component peaks. In a previous contribution these three components were assigned to pyridine chemisorbed on two kinds of Bronsted acid sites and one Lewis acid site. This analysis is extended here to Fe-ZSM-5 and B-ZSM-5. Isomorphous substitution of Fe for Si or Al in the zeolite framework leads to a slight decrease in the binding energy of the N{sub 1s} Lewis component. In the case of B substitution a decrease in the binding energy of all three N{sub 1s} components is observed.

1990-11-01

388

Methionine kinetics and balance at the 1985 FAO/WHO/UNU intake requirement in adult men studied with L-[2H3-methyl-1-13C]methionine as a tracer

The effects of a daily 3-g supplement of betaine on kinetic aspects of L-[2H3-methyl-1-13C]methionine (MET) metabolism in healthy young adult men were explored. Four groups of four subjects each were given a control diet, based on an L-amino acid mixture supplying 29.5 and 21.9 mg.kg-1.d-1 of L-methionine and L-cystine for 4 d before the tracer study, conducted on day 5 during the fed state. Two groups received the control diet and two groups received the betaine supplement. Tracer was given intravenously (iv) or orally. The transmethylation rate of MET (TM), homocysteine remethylation (RM), and oxidation of methionine were estimated from plasma methionine labeling and 13C enrichment of expired air. RM tended to increase (P = 0.14) but the TM and methionine oxidation were significantly (P less than 0.05) higher after betaine supplementation when estimated with the oral tracer. No differences were detected with the intravenous tracer. Methionine ...

389

Isotope effects on the metabolism and pulmonary toxicity of butylated hydroxytoluene in mice by deuteration of the 4-methyl group

The upper range of the requirement for methionine plus cystine in healthy adults was proposed in 1985 by FAO/WHO/UNU to be 13 mg.kg body wt-1.d-1. To explore the validity of this estimate, five healthy, young adult men were given for 7 d a diet based on an L-amino acid mixture supplying 13 mg methionine.kg-1.d-1 (87 mumol.kg-1.d-1) without cystine. Constant intravenous infusions of L-[2H3-methyl-1-13C]methionine were given on days 5 and 7 while subjects were in the fed and postabsorptive states, respectively. Estimates were made of methionine oxidation, and daily methionine balance was derived from the intake-oxidation data. For the five subjects, methionine balances were -0.9, +0.7, +3.5, -3.1, and -3.8 mg kg-1.d-1, or -6, +5, +23, -21, and -26 mumol.kg-1.d-1. These findings lead to the conclusion that the upper range of the requirement for methionine plus cystine probably exceeds 13 mg.kg-1.d-1 in healthy young adults. The implications of ...

390

Yeast ribosomal protein L1 is required for the stability of newly synthesized 5S rRNA and the assembly of 60S ribosomal subunits.

A comparative test in mice for pulmonary toxicity between butylated hydroxytoluene (2,6-di-tert.-butyl-4-methylphenol, BHT) and 2,6-di-tert.-butyl-4-(alpha, alpha, alpha-2H3)methylphenol (BHT-d3) showed a significantly lower toxic potency of the latter. The rate of in vitro BHT metabolism to 2,6-di-tert.-butyl-4-methylene-2,5-cyclohexadienone (BHT-QM) was slowed by deuterating BHT in the 4-methyl group. On the other hand, the rate of in vitro metabolism to 2,6-di-tert.-butyl-4-hydroxy-4-methyl-2,5-cyclohexadienone (BHT-OH) was increased with the deuteration. A similar isotope effect of the deuterium substitution on the in vivo metabolic rates of BHT was observed. These observations support the concept that the lung damage caused by BHT is mediated by BHT-QM. The pulmonary toxicity of 2-tert.-butyl-4-ethylphenol (4-EP) and their deuterated analogs was also compared. 2-tert.-Butyl-4-(1,1-2H2)ethylphenol (4-EP-d2) showed a significantly lower ...

1983-06-30

391

Two and 8-azido photoaffinity probes. 2. Studies on the binding process of 2-5A synthetase by photosensitive ATP analogues

Ribosomal protein L1 from Saccharomyces cerevisiae binds 5S rRNA and can be released from intact 60S ribosomal subunits as an L1-5S ribonucleoprotein (RNP) particle. To understand the nature of the...Full Text Available

1993-05-01

392

Treatment of uteral cancer by the brake irradiation (25 MeV)

The photoaffinity probes [#gamma#-"3"2P]2-azidoATP (2-N_3ATP) and [#alpha#-"3"2P]8-azido-ATP (8-N_3ATP) were used to investigate the binding of ATP to highly purified 2-5A synthetase. 2-N_3APT and 8-N_3ATP are substrates for 2-5A synthetase. In this study the authors show that 2- and 8-N_3ATP are competitive inhibitors of the enzymatic conversion of ATP to 2-5A. Ultraviolet irradiation results in the photoinsertion of 2-N_3ATP and 8-N_3ATP into the enzyme. The covalent photoinsertion of [#alpha#-"3"2P]8-N_3ATP into the 2-5A synthetase is proportional to the inactivation of the enzyme as UV irradiation is increased. Photolabeling of 2-5A synthetase is saturated at 1.5 mM 2-N_3ATP and 2.0 mM 8-N_3ATP. Computer analysis of the curvilinear Scatchard plots of the 2-5A synthetase suggest the presence of high-affinity and low-affinity binding sites that may correspond to the acceptor and the 2'-adenylation sites of the enzyme. The competition of ...

393

Transcription of the E2F-1 gene is rendered cell cycle dependent by E2F DNA-binding sites within its promoter.

The method of treatment of uteral cancer by the brake irradiation of 25 MeV betatrone using original devices which promote forming therapeutic figured bunches is presented. The binding of the protective blocks with a special adjusting frame within the aperture of the diaphragm provided for low relative entering dose which is the advantage of high energy irradiation bunch. The use of the forming devices makes it possible to practice individual treatment and decrease the levels of irradiation doses for intact organs and tissues.

394

The metabolism of L-tryptophan by isolated rat liver cells. Effect of albumin binding and amino acid competition on oxidatin of tryptophan by tryptophan 2,3-dioxygenase.

The cell cycle-regulatory transcription factor E2F-1 is regulated by interactions with proteins such as the retinoblastoma gene product and by cell cycle-dependent alterations in E2F-1 mRNA abundance....Full Text Available

1994-10-01

395

The human U1-70K snRNP protein: cDNA cloning, chromosomal localization, expression, alternative splicing and RNA-binding.

1. Novel methods, using L-[ring-2-14C]tryptophan, are described for the measurement of tryptophan 2,3-dioxygenase activity and tryptophan accumulation in isolated rat liver cells. 2. The effects of...Full Text Available

1980-03-15

396

The effects of diphenyleneiodonium on mitochondrial reactions. Relation of binding of diphenylene[125I]iodonium to mitochondria to the extent of inhibition of oxygen uptake.

We have isolated and sequenced cDNA clones encoding the human U1-70K snRNP protein, and have mapped this locus (U1AP1) to human chromosome 19. The gene produces two size classes of RNA, a major 1.7-kb...Full Text Available

1987-12-23

397

The YTH Domain Is a Novel RNA Binding Domain*

1. Several ring-substituted derivatives of diphenyleneiodonium catalyse the exchange of Cl- and OH- ions across the inner membrane of rat liver mitochondria. They also inhibit state 3 and state 3u oxidations...Full Text Available

1976-08-15

398

The Structure of the Amyloid-[beta] Peptide High-Affinity Copper II Binding Site in Alzheimer Disease

The YTH (YT521-B homology) domain was identified by sequence comparison and is found in 174 different proteins expressed in eukaryotes. It is characterized by 14 invariant residues within an α-helix/β-sheet...Full Text Available

2010-05-07

399

The DNA and RNA specificity of eilatin Ru(II) complexes as compared to eilatin and ethidium bromide

Neurodegeneration observed in Alzheimer disease (AD) is believed to be related to the toxicity from reactive oxygen species (ROS) produced in the brain by the amyloid-{beta} (A{beta}) protein bound primarily to copper ions. The evidence for an oxidative stress role of A{beta}-Cu redox chemistry is still incomplete. Details of the copper binding site in A{beta} may be critical to the etiology of AD. Here we present the structure determined by combining x-ray absorption spectroscopy (XAS) and density functional theory analysis of A{beta} peptides complexed with Cu{sup 2+} in solution under a range of buffer conditions. Phosphate-buffered saline buffer salt (NaCl) concentration does not affect the high-affinity copper binding mode but alters the second coordination sphere. The XAS spectra for truncated and full-length A{beta}-Cu{sup 2+} peptides are similar. The novel distorted six-coordinated (3N3O) geometry around copper in the A{beta}-Cu{sup ...

2008-11-03

400

Synthesis of non-steroidal anti-inflammatory drug analogues for selective studies on the COX-II enzyme

Eilatin-containing ruthenium complexes bind to a broad range of different nucleic acids including: calf thymus (CT) DNA, tRNA^Phe, polymeric RNAs and DNAs, and viral RNAs including the HIV-1...Full Text Available

2003-10-01

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401

Synthesis of 25-hydroxyvitamin D sub 3 3. beta. -3 prime -(N-(4-azido-2-nitrophenyl)amino)propyl ether, a second-generation photoaffinity analogue of 25-hydroxyvitamin D sub 3 : Photoaffinity labeling of rat serum vitamin D binding protein

Synthesis of the azido substituted non-steroidal anti-inflammatory drug 2-(2,6-dichloroanilino)phenylacetic acid and isotope labeling of this compound have been performed and are described. Initial evaluation of the binding ability and photoreactivity indicates that this compound has potential for photoaffinity labeling as well as enzyme selectivity studies. (author).

402

Synthesis and cloning of the genes of antisense peptides of human calcitonin and miniproinsulin

Vulnerability of 25-hydroxy-(26,27-{sup 3}H)vitamin D{sub 3} 3{beta}-N-(4-azido-2-nitrophenyl)glycinate, a photoaffinity analogue of 25-hydroxyvitamin D{sub 3} (25-OH-D{sub 3}) toward standard conditions of carboxymethylationin promoted the authors to synthesize 25-hydroxyvitamin D{sub 3} 3{beta}-3{prime}-(N-(4-azido-2-nitrophenyl)amino)propyl ether (25-ANE), a hydrolytically stable photoaffinity analogue of 25-OH-D{sub 3}, and 25-hydroxyvitamin D{sub 3} 3{beta}-3{prime}-(N-(4-azido-2-nitro-(3,5-{sup 3}H)phenyl)amino)propyl ether ({sup 3}H-25-ANE), the radiolabeled counterpart of 25-ANE competes for the 25-OH-D{sub 3} binding site in rat serum vitamin D binding protein (rDBP). On the other hand, UV exposure of a sample of purified rat DBP (rDBP), preincubated in the dark with {sup 3}H-25-ANE, covalently labeled the protein. However, very little covalent labeling was observed in the absence of UV light or in the presence of a large excess of ...

1991-05-14

403

Structural and Biochemical Basis for the Binding Selectivity of Peroxisome Proliferator-activated Receptor [gamma] to PGC-1[alpha

With the aim of an experimental check on the validity of the theory of molecular recognition, the authors have carried out the chemical-enzymatic synthesis and cloning of the gene of human calcitonin and also of the genes of antisense polypeptides to human calcitonin and miniproinsulin. It has been shown that recombinant plasmids obtained on the basis of these synthetic genes are capable of ensuring the biosynthesis of the given polypeptides in E. coli cells as hybrid proteins with the IgG-binding domain of staphylococcal protein A.

1994-07-20

404

Specific in vitro initiation of transcription on the adenovirus type 2 early and late EII transcription units.

The functional interaction between the peroxisome proliferator-activated receptor {gamma} (PPAR{gamma}) and its coactivator PGC-1{alpha} is crucial for the normal physiology of PPAR{gamma} and its pharmacological response to antidiabetic treatment with rosiglitazone. Here we report the crystal structure of the PPAR{gamma} ligand-binding domain bound to rosiglitazone and to a large PGC-1{alpha} fragment that contains two LXXLL-related motifs. The structure reveals critical contacts mediated through the first LXXLL motif of PGC-1{alpha} and the PPAR{gamma} coactivator binding site. Through a combination of biochemical and structural studies, we demonstrate that the first LXXLL motif is the most potent among all nuclear receptor coactivator motifs tested, and only this motif of the two LXXLL-related motifs in PGC-1{alpha} is capable of binding to PPAR{gamma}. Our studies reveal that the strong interaction of PGC-1{alpha} and ...

2008-07-23

405

Salmonella enterica Serovar Typhimurium Expressing a Chromosomally Integrated Copy of the Bacillus anthracis Protective Antigen Gene Protects Mice against an Anthrax Spore Challenge

Three transcription units are present in the adenovirus type 2 region EII. Transcription units EIIaE and EIIaL encode the mRNA for the 72,000-dalton DNA binding protein, early and late in the lytic...Full Text Available

1981-12-01

406

SAS1 and SAS2, GTP-binding protein genes in Dictyostelium discoideum with sequence similarities to essential genes in Saccharomyces cerevisiae.

Protective immunity against infection with Bacillus anthracis is almost entirely based on a response to the protective antigen (PA), the binding moiety for the two other toxin components....Full Text Available

2003-07-01

407

Ryanodine produces a low frequency stimulation-induced NMDA receptor-independent long-term potentiation in the rat dentate gyrus in vitro.

We have identified two novel, very closely related genes, SAS1 and SAS2, from Dictyostelium discoideum. These encode small, approximately 20-kilodaton proteins with amino acid sequences thought to be...Full Text Available

1990-05-01

408

Roles of the TNF receptor-associated factor (TRAF)2/3 binding site in differential B cell signaling by CD40 and its viral oncogenic mimic, latent membrane protein 1 (LMP1)

1. The induction of long-term potentiation (LTP) was investigated in the rat dentate gyrus in the presence of ryanodine, an agent which is known to selectively bind to the ryanodine receptor (RyR) Ca2+...Full Text Available

1996-09-15

409

Role of Intimin-Tir Interactions and the Tir-Cytoskeleton Coupling Protein in the Colonization of Calves and Lambs by Escherichia coli O157:H7

The Epstein-Barr virus protein, LMP1, is a functional mimic of the cellular receptor CD40, but signals to B lymphocytes in an amplified and sustained manner compared to CD40. LMP1 contributes...Full Text Available

2009-09-01

410

Release of oxidized plastocyanin from photosystem I limits electron transfer between photosystem I and cytochrome b₆f complex in vivo

Intimin facilitates intestinal colonization by enterohemorrhagic Escherichia coli O157:H7; however, the importance of intimin binding to its translocated receptor (Tir) as opposed to...Full Text Available

2006-01-01

411

Relative Rates of Transcapillary Movement of Free Thyroxine, Protein-Bound Thyroxine, Thyroxine-Binding Proteins, and Albumin

We used fast absorbance spectroscopy to investigate in vivo binding dynamics and electron transfer between plastocyanin (pc) and photosystem I (PSI), and cytochrome (cyt) f...Full Text Available

2005-05-10

412

Purification and characterization of (-)(/sup 125/I)hydroxyphenylisopropyladenosine, an adenosine R-site agonist radioligand and theoretical analysis of mixed stereoisomer radioligand binding

The rate of appearance of labeled thyroxine (T4) and albumin in lymph from various areas after simultaneous i.v. injection of the labeled substances in conscious ambulatory sheep has been used to estimate...Full Text Available

1974-07-01

413

Protective Effects of a Human 18-Kilodalton Cationic Antimicrobial Protein (CAP18)-Derived Peptide against Murine Endotoxemia

(-)-N6-(R-4-Hydroxyphenylisopropyl)adenosine (HPIA) was iodinated with NaI and trace /sup 125/I. Mono- and diiodinated reaction products and the starting material were separated by high pressure liquid chromatography and the structures of the reaction products were verified by NMR. (-)-N6-(R-Phenylisopropyl)adenosine (PIA), IHPIA, and I2HPIA decreased rat atrial contractility with ED50 values of 24, 28, and 33 nM, respectively. The contractile effects of these compounds were competitively blocked by theophylline (KI . 7.9 microM), but were not affected by adenosine deaminase. IHPIA also inhibited (-)isoproterenol-stimulated cyclic AMP accumulation in adipocytes with an ED50 (10 nM) and to an extent (83%) nearly identical to PIA. (/sup 125/I)HPIA prepared using carrier-free /sup 125/I bound to adenosine receptors on membranes from rat cerebral cortex, adipocyte ghosts, and heart ventricles. Binding was inhibited stereospecifically by PIA and by other adenosine ...

1984-11-01

414

Polybutylene terephthalate on metals: a density functional theory and cluster models investigation

CAP18 (an 18-kDa cationic antimicrobial protein) is a granulocyte-derived protein that can bind lipopolysaccharide (LPS) and inhibit various activities of LPS in vitro. The present study examined the...Full Text Available

1998-05-01

415

Pair formation in two-electron correlated chains

The strength of adhesion of polybutylene terephthalate (PBT) on aluminium is investigated using density functional theory-based energy calculations. The aluminium atom is connected to a PBT monomer at different orientations, and total energies are calculated and compared to determine the most stable orientation. The binding is strongest when the Al is oriented at 180{sup 0} to the ester group of the monomer. Using this orientation as a basis, PBT adhesion on Ti, Ag, and Au is also investigated.

2006-02-01

416

P130Cas Src-Binding and Substrate Domains Have Distinct Roles in Sustaining Focal Adhesion Disassembly and Promoting Cell Migration

We study two correlated electrons in a nearest-neighbour tight-binding chain, with both on-site and nearest-neighbour interaction. Both the cases of parallel and antiparallel spin are considered. In addition to the free electron band for two electrons, there are correlated bands with positive or negative energy, depending on whether the interaction parameters are repulsive or attractive. Electrons form bound states, with amplitudes that decay exponentially with separation. Conditions for such states to be filled at low temperatures are discussed.

2003-05-21

417

Novel snake venom ligand dendroaspis natriuretic peptide is selective for natriuretic peptide receptor-A in human heart: downregulation of natriuretic peptide receptor-A in heart failure.

The docking protein p130Cas is a prominent Src substrate found in focal adhesions (FAs) and is implicated in regulating critical aspects of cell motility including FA disassembly and protrusion of the...Full Text Available

418

Neuroprotectin D1/Protectin D1 Stereoselective and Specific Binding With Human Retinal Pigment Epithelial Cells and Neutrophils

The natriuretic peptides are considered to be cardioprotective; however, their receptors have not been identified in human myocardium using radiolabeled analogs. Dendroaspis natriuretic peptide (DNP) has been recently identified as a new member of this peptide family and is thought to be less susceptible to enzymatic degradation. Therefore, we have developed the novel radiolabeled analog [125I]-DNP and used this to localize high-affinity (K(D)=0.2 nmol/L), saturable, specific binding sites in adult human heart (n=6) and coronary artery (n=8). In competition binding experiments, atrial natriuretic peptide and brain type natriuretic peptide had greater affinity for [125I]-DNP binding sites than C-type natriuretic peptide and the natriuretic peptide receptor (NPR)-C ligand, cANF. This rank order of potency suggested binding of [125I]-DNP was specific to NPR-A. Messenger RNA encoding NPR-A was identified in ...

2006-06-15

419

Mutations at the accommodation gate of the ribosome impair RF2-dependent translation termination

Retinal pigment epithelial (RPE) cells, derived from the neuroectoderm, biosynthesize the novel lipid mediator neuroprotectin D1 (NPD1) from docosahexaenoic acid (DHA) in response to oxidative...Full Text Available

2010-01-01

420

Mutations Affecting Motifs of Unknown Function in the Central Domain of Nitrogen Regulatory Protein C

During protein synthesis, aminoacyl-tRNA (aa-tRNA) and release factors 1 and 2 (RF1 and RF2) have to bind at the catalytic center of the ribosome on the 50S subunit where they take part in peptide bond...Full Text Available

2010-09-01

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421

Monoclonal antibodies to ovine SBU-T8 and SBU-T6 bind analogous molecules on bovine lymphocytes.

The positive control function of the bacterial enhancer-binding protein NtrC resides in its central domain, which is highly conserved among activators of ς⁵⁴ holoenzyme. Previous...Full Text Available

1999-09-01

422

Molecular recognition of nitrated fatty acids by PPAR[gamma

Monoclonal antibodies (mAb) to ovine T-lymphocyte molecules SBU-T8 (Maddox, Mackay & Brandon, 1985), the cytotoxic T lymphocyte, human CD8 equivalent, and SBU-T6 (Mackay et al., 1985), the immature...Full Text Available

1989-06-01

423

Molecular basis of factor VIII inhibition by human antibodies. Antibodies that bind to the factor VIII light chain prevent the interaction of factor VIII with phospholipid.

Peroxisome proliferator activated receptor-{gamma} (PPAR{gamma}) regulates metabolic homeostasis and adipocyte differentiation, and it is activated by oxidized and nitrated fatty acids. Here we report the crystal structure of the PPAR{gamma} ligand binding domain bound to nitrated linoleic acid, a potent endogenous ligand of PPAR{gamma}. Structural and functional studies of receptor-ligand interactions reveal the molecular basis of PPAR{gamma} discrimination of various naturally occurring fatty acid derivatives.

2010-03-08

424

Metabolism and Binding of ¹⁴C-Maleic Hydrazide ¹

Most antibodies to factor VIII have recently been shown to react with discrete regions of the factor VIII light chain (within the C2 domain) and/or the factor VIII heavy chain (within the amino-terminal...Full Text Available

1989-06-01

425

Medium-chain fatty acid binding to albumin and transfer to phospholipid bilayers.

Maleic hydrazide (MH) is taken up by corn and pea seedling roots and bound to some material which is insoluble in 80% ethanol or 5% trichloroacetic acid. ¹⁴C-MH is stable metabolically; chromatography...Full Text Available

1970-01-01

426

Meat factor peptides as a good iron source for vegetarians

Temperature-dependent (5-42 degrees C) 13C NMR spectra of albumin complexes with 90% isotopically substituted [1-13C]decanoic acids (3 mol of fatty acid per mol of albumin) showed a single peak at greater...Full Text Available

1989-04-01

427

Environmental Research Database

DescriptionIron deficiency anaemia is a common problem and may be particularly important to certain groups of vegetarians. This project investigates isolating and identifying iron-binding constituents of meat digests using human Caco-2 cell lines. Stable isotope techniques used to test whether one or more of these compounds enhance iron absorpion in vivo and could therefore be added to vegetarian products to imporve iron nutrition.

2005-01-31

428

Mapping of TH1 helper T-cell epitopes on major secreted mycobacterial antigen 85A in mice infected with live Mycobacterium bovis BCG.

Mapping a nucleolar targeting sequence of an RNA binding nucleolar protein, Nop25

TH1 cytokine secretion was examined in response to synthetic peptides of the 85A component of the major secreted, fibronectin-binding antigen 85 complex from Mycobacterium tuberculosis in seven different...Full Text Available

1994-02-01

429

Magnetoresistance of Two-Dimensional Tight-Binding Electrons in a Weak Magnetic Field

Nop25 is a putative RNA binding nucleolar protein associated with rRNA transcription. The present study was undertaken to determine the mechanism of Nop25 localization in the nucleolus. Deletion experiments of Nop25 amino acid sequence showed Nop25 to contain a nuclear targeting sequence in the N-terminal and a nucleolar targeting sequence in the C-terminal. By expressing derivative peptides from the C-terminal as GFP-fusion proteins in the cells, a lysine and arginine residue-enriched peptide (KRKHPRRAQDSTKKPPSATRTSKTQRRRR) allowed a GFP-fusion protein to be transported and fully retained in the nucleolus. When the peptide was fused with cMyc epitope and expressed in the cells, a cMyc epitope was then detected in the nucleolus. Nop25 did not localize in the nucleolus by deletion of the peptide from Nop25. Furthermore, deletion of a subdomain (KRKHPRRAQ) in the peptide or amino acid substitution of lysine and arginine residues in the subdomain resulted in the loss ...

2006-06-10

430

Lack of the Long Pentraxin PTX3 Promotes Autoimmune Lung Disease but not Glomerulonephritis in Murine Systemic Lupus Erythematosus

We study the Anderson model on a two-dimensional square lattice with an applied weak magnetic field B which causes the hopping matrix elements to have Peierls phase factors. The recursion method is applied and B dependent conductivity ?(B) is calculated from the Kubo formula for different system sizes and degree of disorder W . For large W there is no systematic change of ?(B) with B, it shows a fluctuating behavior.

2008-08-25

431

Kidney-specific allo- and autoantibodies in the alloantibody response to rat kidney: the use of kidney homogenate as a target for serological analysis.

The long pentraxin PTX3 has multiple roles in innate immunity. For example, PTX3 regulates C1q binding to pathogens and dead cells and regulates their uptake by phagocytes. It also inhibits P-selectin-mediated...Full Text Available

432

Kes1p shares homology with human oxysterol binding protein and participates in a novel regulatory pathway for yeast Golgi-derived transport vesicle biogenesis.

LEW anti-DA kidney and DA anti-LEW kidney sera were assayed using an indirect 125I anti-immunoglobulin-binding assay with kidney homogenate as target. This allowed the full spectrum of antibodies to...Full Text Available

1980-04-01

433

Interactions between tRNA identity nucleotides and their recognition sites in glutaminyl-tRNA synthetase determine the cognate amino acid affinity of the enzyme.

The yeast phosphatidylinositol transfer protein (Sec14p) is required for biogenesis of Golgi-derived transport vesicles and cell viability, and this essential Sec14p requirement is abrogated by inactivation...Full Text Available

1996-12-02

434

Identification of a nucleoside triphosphate binding site on calf thymus RNA polymerase II

Sequence-specific interactions between aminoacyl-tRNA synthetases and their cognate tRNAs both ensure accurate RNA recognition and prevent the binding of noncognate substrates. Here we show for Escherichia...Full Text Available

1996-07-09

435

Identification of a Drosophila G protein alpha subunit (dGq alpha-3) expressed in chemosensory cells and central neurons.

A nucleoside triphosphate binding site on calf thymus RNA polymerase II was identified by using photoaffinity analogues of adenosine 5'-triphosphate and guanosine 5'-triphosphate. Both radiolabeled 8-azidoadenosine 5'-triphosphate (8-N3ATP) and radiolabeled 8-azidoguanosine 5'-triphosphate (8-N3GTP) bound to a single polypeptide of this enzyme. This polypeptide has a molecular mass of 37 kilodaltons and an isoelectric point of 5.4. Ultraviolet (UV) irradiation was necessary for photolabeling to occur. In addition, no labeling occurred when the probe was prephotolyzed or when the enzyme was inactivated. Furthermore, photolabeling of the enzyme could be decreased by preincubation with natural substrates. To provide evidence that the radiolabeled polypeptide forms a part of the domain of the nucleoside triphosphate binding site, experiments were performed using unlabeled 8-N3ATP. Although this unlabeled analogue ...

1986-01-14

436

Hypoxia down-regulates sFlt-1 (sVEGFR-1) expression in human microvascular endothelial cells by a mechanism involving mRNA alternative processing

We have identified another Drosophila GTP-binding protein (G protein) alpha subunit, dGq alpha-3. Transcripts encoding dGq alpha-3 are derived from alternative splicing of the dGq alpha locus previously...Full Text Available

1995-12-05

437

HupUV proteins of Rhodobacter capsulatus can bind H2: evidence from the H-D exchange reaction.

sFlt-1 (soluble Flt-1) potently inhibits angiogenesis by binding extracellularly to VEGF (vascular endothelial growth factor). In the present paper, we report that hypoxia down-regulates sFlt-1 expression...Full Text Available

2011-06-01

438

Heparin blocks /sup 125/I-calmodulin internalization by isolated rat renal brush border membrane vesicles

The H-D exchange reaction has been measured with the D2-H2O system, for Rhodobacter capsulatus JP91, which lacks the hupSL-encoded hydrogenase, and R. capsulatus BSE16, which lacks the HupUV proteins....Full Text Available

1997-01-01

439

Green tea increases anti-inflammatory tristetraprolin and decreases pro-inflammatory tumor necrosis factor mRNA levels in rats

/sup 125/I-Calmodulin is internalized by isolated rat renal brush border membrane vesicles (BBV) in a time, temperature and calcium dependent manner. Internalization of /sup 125/I-calmodulin into the osmotically sensitive space of BBV was distinguished from binding of the ligand to the outer BBV surface by examining the interaction of ligand and BBV at different medium osmolarities (300-1100 mosm), uptake was inversely proportional to medium osmolarity. Internalized /sup 125/I-calmodulin was intact and Western blots of solubilized BBV with /sup 125/I-calmodulin demonstrated the presence of several calmodulin-binding proteins of 143, 118, 50, 47.5, 46.5 and 35 kilodaltons which could represent potential intravesicular binding sites for the ligand. Heparin and the related glycosaminoglycan heparin sulfate both showed a dose-dependent inhibition (0.5-50 ..mu..g/ml) of /sup 125/I-calmodulin uptake by BBV, but other sulfated and ...

1986-03-05

440

Global analysis of estrogen receptor beta binding to breast cancer cell genome reveals an extensive interplay with estrogen receptor alpha for target gene regulation

BackgroundTristetraprolin (TTP/ZFP36) family proteins have anti-inflammatory activity by binding to and destabilizing pro-inflammatory mRNAs such as Tnf mRNA, and represent a potential...Full Text Available

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25

441

Friction between different wire-bracket configurations and materials.

BackgroundEstrogen receptors alpha (ERα) and beta (ERβ) are transcription factors (TFs) that mediate estrogen signaling and define the hormone-responsive phenotype...Full Text Available

442

Formation of an intramolecular cystine disulfide during the reaction of 8-azidoguanosine 5'-triphosphate with cytosolic phosphoenolpyruvate carboxykinase (GTP) causes inactivation without photolabeling

Friction opposes tooth motion whenever sliding mechanics is employed. Understanding what friction is and how to manage it is of paramount importance to the successful practitioner. In this article, the coefficients of friction are summarized between different arch wire-bracket couples as a function of material, geometric, and external parameters. From this vantage point, friction can then be evaluated within the context of other factors that affect sliding-binding and notching. PMID:9573878

1997-09-01

443

Formation of an intramolecular cystine disulfide during the reaction of 8-azidoguanosine 5 prime -triphosphate with cytosolic phosphoenolpyruvate carboxykinase (GTP) causes inactivation without photolabeling

Phosphoenolpyruvate carboxykinase (GTP) (PEPCK) specifically utilizes a guanosine or inosine nucleotide as a substrate, yet it does not share extended sequence homology with other GTP-binding proteins, and the molecular basis for its nucleotide specificity is not understood. In an effort to locate the enzyme's nucleotide-binding site, the authors have studied the interaction of cytosolic PEPCK from rat liver with the photoprobe 8-azidoGTP, which fulfills the criteria of a specific photoaffinity label for PEPCK. The photoprobe binds reversibly to the enzyme prior to modification and at low concentrations causes greater than 60% inactivation-GTP provides nearly complete protection against inactivation by 8-azidoGTP, whereas phosphoenolpyruvate and metal ions provide partial protection. In addition, the photoprobe is a substrate for the enzyme and has a K_m similar to that for GTP. However, the extent of covalent modification ...

444

Fatty acid distribution in systems modeling the normal and diabetic human circulation. A 13C nuclear magnetic resonance study.

Phosphoenolpyruvate carboxykinase (GTP) (PEPCK) specifically utilizes a guanosine or inosine nucleotide as a substrate, yet it does not share extended sequence homology with other GTP-binding proteins, and the molecular basis for its nucleotide specificity is not understood. In an effort to locate the enzyme's nucleotide-binding site, the authors have studied the interaction of cytosolic PEPCK from rat liver with the photoprobe 8-azidoGTP, which fulfills the criteria of a specific photoaffinity label for PEPCK. The photoprobe binds reversibly to the enzyme prior to modification and at low concentrations causes greater than 60% inactivation-GTP provides nearly complete protection against inactivation by 8-azidoGTP, whereas phosphoenolpyruvate and metal ions provide partial protection. In addition, the photoprobe is a substrate for the enzyme and has a K{sub m} similar to that for GTP. However, the extent of covalent ...

1989-11-28

445

Extracellular Protein Disulfide Isomerase Regulates Feedback Activation of Platelet Thrombin Generation Via Modulation of Coagulation Factor Binding.

A nonperturbing 13C nuclear magnetic resonance (NMR) method was used to monitor the equilibrium distribution of carboxyl 13C-enriched fatty acids (FA) between distinct binding sites on human serum albumin,...Full Text Available

1991-04-01

446

Dopamine transporter density in the basal ganglia assessed with [{sup 123}I]IPT SPET in children with attention deficit hyperactivity disorder

Background: Protein disulfide isomerase (PDI) controls platelet integrin function, tissue-factor (TF) activation, and concentrates at fibrin and thrombus formation sites of vascular injury. Objective: We investigated involvement of surface thiol isomerases and especially PDI, in thrombin-mediated thrombin amplification on human platelets. Methods/Results: Using a new developed thrombin-dependent platelet thrombin generation assay we observed that the feedback activation of thrombin generation on the platelet surface does not depend on TF, as anti-TF antibodies inhibiting TF-induced thrombin formation in platelet-depleted plasma had no effect compared to vehicle-treated controls. Feedback activation of thrombin generation in the presence of platelets was significantly diminished by membrane impermeant thiol blockers or by the thiol isomerase-inhibitors bacitracin and anti-PDI antibody RL90, respectively. Platelet thrombin formation depends on binding of coagulation ...

2011-09-19

447

Disruption of the ATP-binding Cassette B7 (ABTM-1/ABCB7) Induces Oxidative Stress and Premature Cell Death in Caenorhabditis elegans*

Attention deficit hyperactivity disorder (ADHD) is a psychiatric disorder in childhood that is known to be associated with dopamine dysregulation. In this study, we investigated dopamine transporter (DAT) density in children with ADHD using iodine-123 labelled N-(3-iodopropen-2-yl)-2β-carbomethoxy-3β-(4-chlorophenyl) tropane ([{sup 123}I]IPT) single-photon emission tomography (SPET) and postulated that an alteration in DAT density in the basal ganglia is responsible for dopaminergic dysfunction in children with ADHD. Nine drug-naive children with ADHD and six normal children were included in the study. We performed brain SPET 2 h after the intravenous administration of [{sup 123}I]IPT and carried out both quantitative and qualitative analyses using the obtained SPET data, which were reconstructed for the assessment of the specific/non-specific DAT binding ratio in the basal ganglia. We then investigated the correlation between the severity ...

2003-02-01

448

Density of states of ordered and disordered A-15 phase

X-linked sideroblastic anemia with ataxia (XLSA/A) is a rare inherited disorder characterized by mild anemia and ataxia. XLSA/A is caused by mutations in the ABCB7 gene, which encodes...Full Text Available

2011-06-17

449

Cyclopeptide alkaloids. Synthesis of the ring system and its ion affinity

Within the tight binding framework, a study is made of how the disorder affects the electronic properties of A-15 compounds. In particular it is shown that for compounds of two transition metals in the A-15 structure, the vacancy formation affects the density of states only in the low energy region or in the high energy region, in opposition with the isolated chain model of Labbe and Friedel. It is concluded that interchain interactions are important. (U.K.).

450

Covalent Modification of Thr302 in Cytochrome P450 2B1 by the Mechanism-Based Inactivator 4-tert-Butylphenylacetylene

Several examples of the 14-membered, para-bridged ring system of the cyclopeptide alkaloids have been synthesized via an active ester cyclization. The yield of monomeric cyclopeptide varied from 1 to 33% and was affected by the amino acid substitution pattern and amide conformation of the linear peptide precursors. Both the synthetic models and a naturally occurring cyclopeptide alkaloid, ceanothine B, bind monovalent (Li"+) and divalent (Ca"2"+, Mg"2"+) cations. 4 figures, 1 table.

451

Changes in cardiac glycoside receptor sites, 86rubidium uptake and intracellular sodium concentrations in the erythrocytes of patients receiving digoxin during the early phases of treatment of cardiac failure in regular rhythm and of atrial fibrillation.

The mechanism of inactivation of cytochrome P450 2B1 (CYP2B1) by 4-tert-butylphenylacetylene (BPA) has been characterized previously to be caused by the covalent binding of a reactive...Full Text Available

2010-06-01

452

Cadmium down-regulation of kidney Sp1 binding to mouse SGLT1 and SGLT2 gene promoters: Possible reaction of cadmium with the zinc finger domain of Sp1

1 Measurements of the binding of 12-alpha-[3H]-digoxin to the membranes of intact erythrocytes, erythrocytic 86rubidium uptake and intraerythrocytic sodium concentrations have been made in the red cells...Full Text Available

1979-08-01

453

BosR (BB0647) Controls the RpoN-RpoS Regulatory Pathway and Virulence Expression in Borrelia burgdorferi by a Novel DNA-Binding Mechanism

Cadmium (Cd) exposure causes glucosuria (glucose in the urine). Previously, it was shown that Cd exposure of primary cultures of mouse kidney cells (PMKC) decreased mRNA levels of the glucose...Full Text Available

2010-05-01

454

Bax Activation by Engagement with, Then Release from, the BH3 Binding Site of Bcl-x_L?

In Borrelia burgdorferi (Bb), the Lyme disease spirochete, the alternative σ factor σ⁵⁴ (RpoN) directly activates transcription of another alternative σ...Full Text Available

2011-02-01

455

ATP Hydrolysis in Eg5 Kinesin Involves a Catalytic Two-water Mechanism*^?

Bcl-2 homologues (such as Bcl-x_L) promote survival in part through sequestration of “activator” BH3-only proteins (such as Puma), preventing them from directly activating...Full Text Available

2011-02-01

456

A study of the interactions of some polypyridylruthenium (II) complexes with DNA using fluorescence spectroscopy, topoisomerisation and thermal denaturation.

Motor proteins couple steps in ATP binding and hydrolysis to conformational switching both in and remote from the active site. In our kinesin·AMPPPNP crystal structure, closure of the active...Full Text Available

2010-02-19

457

A precise structure redetermination of nickel ammonium sulfate hexahydrate, Ni(H_2O)_6.2NH_4.2SO_4

The nature of binding of Ru(phen) 2+ (I), Ru(bipy) 2+ (II), Ru(terpy) 2+ (III) (phen = 1,10-phenanthroline, bipy 3 = 2,2'-bipyridyl, 3 terpy = 2,2'2," - 2 terpyridyl) to DNA, poly[d(G-C)] and poly[d(A-T)]...Full Text Available

1985-09-11

458

A microscopic description of neutron-rich lithium isotopes

The Ni(H_2O)_6 ion is located at an inversion center. Six octahedral water molecules surround the Ni"I"I ion and form hydrogen bonds with the sulfate groups. Each ammonium group binds to the sulfate groups through hydrogen bonds. (orig.).

1994-05-01

459

1,1-Dichloroethylene hepatotoxicity: Proposed mechanism of action and distribution and binding of ¹⁴C radioactivity following inhalation exposure in rats

A unified calculation of neutron-rich isotopes in lithium is performed using the hyperspherical basis in which the underlying symmetry of each isotope exhibits a simple structure. The variation of the binding energy as a function of mass number is qualitatively reproduced, and the asymptotic of radial distribution of each isotope decreases exponentially. The form factors of the lithium isotopes are calculated and display diffraction minima. 27 refs., 3 figs., 3 tabs.

460

Characterization of [[sup 123]I]IDAM as a novel single-photon emission tomography tracer for serotonin transporters

1,1-Dichloroethylene is reported to produce renal tumors in male mice. It is an hepatotoxin in fasted rats after inhalation. We found that trichloropropane epoxide, an inhibitor of epoxide hydrase,...Full Text Available

1977-12-01

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25

461

beta. -Endorphin and related peptides suppress phorbol myristate acetate-induced respiratory burst in human polymorphonuclear leukocytes

Development of selective serotonin transporter (SERT) tracers for single-photon emission tomography (SPET) is important for studying the underlying pharmacology and interaction of specific serotonin reuptake site inhibitors, commonly used antidepressants, at the SERT sites in the human brain. In search of a new tracer for imaging SERT, IDAM (5-iodo-2-[[2-2-[(dimethylamino)methyl]phenyl]thio]benzyl alcohol) was developed. In vitro characterization of IDAM was carried out with binding studies in cell lines and rat tissue homogenates. In vivo binding of [[sup 125]I]IDAM was evaluated in rats by comparing the uptakes in different brain regions through tissue dissections and ex vivo autoradiography. In vitro binding study showed that IDAM displayed an excellent affinity to SERT sites (K[sub i]=0.097 nM, using membrane preparations of LLC-PK[sub 1] cells expressing the specific transporter) and showed more than 1000-fold of ...

1999-08-01

462

Studies on the mechanism of action of enterotoxin-induced fluid secretion in the gut

In the present study, the immunomodulatory effect of {beta}-endorphin ({beta}-E) and shorter pro-opiomelancortin (POMC) fragments was evaluated by assessing their influence on respiratory burst in human polymorphonuclear leukocytes (PMN). The effect of the peptides on phorbol myristate acetate (PMA)-stimulated production of reactive oxygen metabolites was measured in a lucigenin-enhanced chemiluminescence (CL) assay. Both POMC peptides with opiate-like activity and their non-opioid derivatives were tested. With the exception of {alpha}-E, PMA-stimulated respiratory burst was suppressed by all POMC fragments tested. A U-shaped dose-response relation was observed. Doses lower than 10{sup {minus}17}M and higher than 10{sup {minus}8}M were without effect. {beta}-E and dT{beta}E both suppressed PMA-induced oxidative burst in human PMN at physiological concentrations. {gamma}-E and dT{gamma}E proved to be less potent inhibitors, reaching maximal effect at higher concentrations. DE{gamma}E ...

1989-01-01

463

Involvement of a glutamergic mechanism in gamma-dendrotoxin-induced hippocampal neuronal cell loss in the rat.

The mechanism of action of Clostridium difficile enterotoxin A (CA), of Escherichia coli enterotoxin (STa) and of cholera toxin (CT), which are known to cause severe diarrhea, were studied in a preparation of ligated jejunal loops of anesthetized rats in vivo. The toxins were administered intraluminally. Pharmacological agents, which were tested for their potency to influence toxin-related effects, were administered subcutaneously. Net fluid transport was determined gravimetrically, prostaglandin (PG) E_2-output into the lumen, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) contents in the mucosa were measured by radioimmunoassay, serotonin-(5-HT)-output into the lumen was determined by high performance liquid chromatography. The histopathological effects of CA and CT were examined by light- and scanning electron microscopy. All three toxins caused net fluid secretion (FS). 5-HT_2-(ketanserin) and 5-HT_3-receptor antagonists ...

1992-01-01

464

Effects of opioid peptides on thermoregulation

The epileptogenic and neurodegenerative effects of gamma-dendrotoxin, from Dendroaspis angusticeps, a specific blocker of a non-inactivating, voltage-sensitive K+ channel, were studied after focal injection into one dorsal hippocampus in rats pretreated with CGP040116, a N-methyl-D-aspartate (NMDA) receptor antagonist, and in rats bearing a monolateral surgical lesion of the Schaffer collaterals whose terminals originate from CA3 pyramids and release glutamate in the CA1 hippocampal area. Administration of 35 pmol gamma-dendrotoxin elicited in all of the treated animals (n=8) bilateral EEG discharges and damage to the hippocampal formation. Quantitation of the damage revealed significant bilateral neuronal cell loss in the CA1, CA3 and CA4 pyramidal cell layers. The lowest dose (0.35 pmol; n=4) of the toxin used did not affect EEG activity and failed to cause significant hippocampal cell loss whereas the 3.5 pmol (n=6) dose caused EEG seizures and hippocampal cell ...

2004-03-01

465

Contribution of calcium ions and hydrogen ions to the signal transduction chain in phytochrome-mediated spore germination. [Onoclea sensibilis L

In a given species, injected opioid peptides usually cause changes in temperature similar to those caused by nonpeptide opioids. The main effect in those species most studied, the cat, rat, and mouse, is an increase in the level about which body temperature is regulated; there is a coordinated change in the activity of thermoregulatory effectors such that hyperthermia is produced in both hot and cold environments. Larger doses may depress thermoregulation, thereby causing body temperature to decrease in the cold. Elicitation of different patterns of response over a range of environmental temperatures and studies with naloxone and naltrexone indicate that stimulation of a number of different receptors by both peptide and nonpeptide opioids can evoke thermoregulatory responses. ..beta..-Endorphin is readily antagonized by naloxone whereas methionine-enkephalin can act on naloxone-insensitive receptors. Moreover, synthetic peptide analogs do not necessarily evoke the same response as does ...

1981-11-01

466

Assessing radiologic risk for population due to human activities

Red light stimulates germination in the spores of Onoclea sensibilis L. Phytochrome is confirmed to be the photoreceptor pigment in the germination response by demonstrating red-far-red photoreversibility. External Ca/sup 2 +/ is required for this response with a threshold at a submicromolar concentration. Red light stimulates an increase in the total concentration of intracellular calcium in the spores as determined by atomic absorption spectroscopy. Subsequent exposure to far-red light inhibits the red light-induced increase in intracellular calcium. The majority of the increase occurs 5 minutes after the onset of irradiation. The calcium-antagonist, La/sup 3 +/ inhibits both germination and the red light-induced increase in intracellular calcium. Using /sup 31/P-nuclear magnetic resonance spectroscopy, the author tested the hypothesis that a sustained increase in intracellular pH contributes to the signal transduction chain. He never detected a red light-induced ...

1985-01-01

467

Thermal stress imposed by prototype bilayer and current ground crew chemical defense ensembles: a limited laboratory comparison. Final report, 30 June 1986-1 January 1987

The most important factor in assessing radiologic risk is ensuring scientific means for evaluation of the radioactive release impact upon humans and organisms. To evaluate quantitatively this impact not only knowledge of radioactivity distribution in these dynamical systems is necessary but also understanding the transfer mechanisms between ecosystem components is needed. Thus a complete radioecologic study appear to be very complex and needs defining the source term, dynamic description of radionuclides behavior in the ecosystem, estimation of radiation doses in the major components of the ecosystem and finally the effects of radiation doses upon different parts of the systems. A diagram of the steps implied in evaluation of the effects due to radioactive effluent release in the environment is presented and discussed. The following steps are described: - identification of radioactive sources, as well as their input rate. Presence of noxious materials such as heavy metals or some ...

2002-09-06

468

Theoretical and scaling factors methods to calculate the radioactivity in operational waste streams from Unit 1 at Cernavoda NPP

An open bilayer ground-crew chemical defense ensemble (CDE) was proposed to reduce the thermal burden during vapor-only exposure periods. This study compared the thermal-stress profile of the proposed ensemble to that produced by the currently employed closed CDE. Four subjects, alternating ensembles on separate days, walked on a treadmill in an environmental chamber at 5.3 km/h (3.3 mph) and 2% grade (an energy expenditure of 350 kcal/h) for alternating work/rest to achieve significant recovery. Mean total sweat production was lower (1.38 vs. 2.50 liters) and percent sweat evaporation greater (65.7% vs. 30.0%) in the prototype ensemble than in the CDE. The prototype ensemble provided greater heat dissipation and allowed more-efficient sweat evaporation which had the double benefit of reducing heat storage and limiting dehydration.

1988-07-01

469

The Redshift Evolution of Wet, Dry, and Mixed Galaxy Mergers from Close Galaxy Pairs in the DEEP2 Galaxy Redshift Survey

The main goal of this paper is to present a methodology for calculating the radioactivity in the moderator and heat transport systems of Cernavoda NPP Unit 1, with the intention to improve the knowledge on the radionuclides inventories in the operational waste streams, and to aid the licensing process of new near surface repository. In the present paper we describe our methodology for estimating H-3 and C-14 production rates in the heavy-water moderator and heat transport systems using the capacity factors from 1997 to 2007 years. The radioactivity of the difficult-to-measure nuclides is predicted by scaling method using measured concentration in reference CANDU 6 reactor Gentilly-2. The difficult-to-measure radionuclides of primary interest in this study were those with long half-lives which have a significant role for post-closure safety assessment. The equation used to scale fission products (parents and daughters) is based on the ...

2009-05-27

470

Structure of human insulin monomer in water/acetonitrile solution

We study the redshift evolution of galaxy pair fractions and merger rates for different types of galaxies using kinematic pairs selected from the DEEP2 Redshift Survey. Parameterizing the evolution of the pair fraction as (1+z)^{m}, we find that the companion rate increases mildly with redshift with m = 0.41+-0.20 for all galaxies with -21 < M_B^{e} < -19. Blue galaxies show slightly faster evolution in the blue companion rate with m = 1.27+-0.35 while red galaxies have had fewer red companions in the past as evidenced by the negative slope m = -0.92+-0.59. We find that at low redshift the pair fraction within the red sequence exceeds that of the blue cloud, indicating a higher merger probability among red galaxies compared to that among the blue galaxies. With further assumptions on the merger time scale and the fraction of pairs that will merge, the galaxy major merger rates for 0.1 < z <1.2 are estimated to be ...

2008-01-01

471

Structure and kinematics of edge-on galaxy discs - I. Observations of the stellar kinematics

Here we present evidence that in water/acetonitrile solvent detailed structural and dynamic information can be obtained for important proteins that are naturally present as oligomers under native conditions. An NMR-derived human insulin monomer structure in H{sub 2}O/CD{sub 3}CN, 65/35 vol%, pH 3.6 is presented and compared with the available X-ray structure of a monomer that forms part of a hexamer (Acta Crystallogr. 2003 Sec. D59, 474) and with NMR structures in water and organic cosolvent. Detailed analysis using PFGSE NMR, temperature-dependent NMR, dilution experiments and CSI proves that the structure is monomeric in the concentration and temperature ranges 0.1-3 mM and 10-30 deg. C, respectively. The presence of long-range interstrand NOEs, as found in the crystal structure of the monomer, provides the evidence for conservation of the tertiary structure. Starting from structures calculated by the program CYANA, two different molecular ...

2008-01-15

472

Separation of trace radionuclides by ion exchange in the presence of competing ions

We present deep optical long-slit spectra of 17 edge-on spiral galaxies of intermediate to late morphological type, mostly parallel to their major axes and in a few cases parallel to the minor axes.The line-of-sight stellar kinematics are obtained from the stellar absorption lines using the improvedc ross-correlation technique. In general, the stellar kinematics are regular and can be traced well into the disc-dominated region. The mean stellar velocity curves are far from solid-body, indicating that the effect of dust extinction is not large. The line-of-sight stellar disc velocity dispersion correlates with the galaxy maximum rotational velocity, but detailed modeling is necessary to establish whether this represents a physical relation. In four spirals with a boxy- or peanut-shaped bulge we are able to detect asymmetric velocity distributions, having a common signature with projected radius in the mean line-of-sight velocity and the $h_{3}$ ...

2004-01-01

473

Multilayered Nano-Microcomposite Ti-Al-N/TiN/Al_2O_3 Coatings. Their Structure and Properties

The performance of larger than bench scale ion exchange systems is evaluated by using solutions containing trace amounts of "1"3"7Cs, "8"5Kr, and "1"3"1I, and large amounts of either NaCl or Na_2HPO_4, H_3BO_3, and LiOH. The significant finding in this study is that the empirical rules of ionic selectivity of strong acid cation and strong base anion resins were followed by all ionic species, even though concentrations of some macrocomponents were nearly 10"6 times those of trace components. Other results of possible importance are the correlation between the instantaneous decontamination factor (DF) and the efficiency of column exchange capacity utilization, and the concept of time average decontamination factor (anti DF). The plot of anti DF vs. feed throughput will serve as a guide in determining when the feed should be discontinued in order to achieve a desired anti DF. Both of these correlations are derived from the breakthrough curves.

474

Molar extinction coefficients of some commonly used solvents

This paper presents the first results on formation and study of structure and properties of micro- and nanocomposite combined coatings. By means of modeling the deposition processes (deposition conditions, current density-discharge, plasma composition and density, voltage) we formed the three-layer nanocomposite coatings of Ti-Al-N/Ti-N/Al_2O_3. The coating composition, structure and properties were studied using physical and nuclear-physical methods. The Rutherford proton and helium ion backscattering, scanning electron microscopy with microanalysis, grazing incidence X-ray diffraction, as well as nanohardness tests (hardness) were used. Measurements of wear resistance and corrosion resistance in NaCl, HCl and H_2SO_4 solutions were also performed. For testing mechanical properties such characteristics of layered structures as hardness H, elastic modulus E: H"3/E"2 etc. were measured. It is demonstrated that the formed three-layer ...

2011-07-01

475

Measurement of unpolarized semi-inclusive pi+ electroproduction off the proton

Molar extinction coefficients of some commonly used solvents (ethanol (C_2H_5OH), methanol (CH_3OH), propanol (C_3H_7OH), butanol (C_4H_9OH), water (H_2O), toluene (C_7H_8), benzene (C_6H_6), carbontetrachloride (CCl_4), acetonitrile (C_4H_3N), chlorobenzene (C_6H_5Cl), diethylether (C_4H_1O) and dioxane (C_4H_8O_2)) have been determined by a well-collimated narrow beam transmission geometry at 279, 356, 662, 1173, 1252 and 1332 keV #gamma# rays. The total #gamma# ray interaction cross sections of these solvents have also been determined. A good agreement has been obtained between the experimental results with the theoretical values evaluated through XCOM calculations.

2006-07-01

476

Limits on Anomalous Trilinear Gauge Couplings in Zgamma Events from ppbar Collisions at sqrt{s} = 1.96 TeV

Semi-inclusive pi+ electroproduction on protons has been measured with the CLAS detector at Jefferson Lab. The measurement was performed on a liquid-hydrogen target using a 5.75 GeV electron beam. The complete five-fold differential cross sections were measured over a wide kinematic range in Q2, x, z, and pT and over the complete range of azimuthal angles, phi, enabling us to separate the different structure functions, H2+eps*H1, H3 and H4. Our measurements of H2 at low-x were found to be in fairly good agreement with pQCD calculations, suggesting a precocious factorization of the process. Indeed, the conventional f(x)*D(z) term can account for almost all of the observed cross section, even at small z. The measured xF-distributions are in qualitative agreement with high energy data, which suggests a surprising numerical similarity between the spectator diquark fragmentation in the present reaction and the anti-quark fragmentation measured in ...

2008-01-01

477

Inelastic Neutron Scattering on an Mn10 Supertetrahedron: Assessment of Exchange Coupling Constants, Ferromagnetic Spin Waves and an Analogy to the Hckel Method

Using Zgamma candidate events collected by the CDF detector at the Tevatron Collider, we search for potential anomalous (non-standard-model) couplings between the Z boson and the photon. At the hard scatter energies typical of the Tevatron, standard model Zgamma couplings are too weak to be detected by current experiments; hence any evidence of couplings indicates new physics. Measurements are performed using data corresponding to an integrated luminosity of 4.9 /fb in the Z -> nunubar decay channel and 5.1 /fb in the Z -> l^+l^- (l=mu, e) decay channels. The combination of these measurements provides the most stringent limits to date on Zgamma trilinear gauge couplings. Using an energy scale of Lambda = 1.5 TeV to allow for a direct comparison with previous measurements, we find limits on the CP-conserving parameters that describe Zgamma couplings to be |h_3^{\\gamma,Z}| < 0.017 and |h_4^{\\gamma,Z}| < 0.0006. These results are ...

2011-01-01

478

British Library Electronic Table of Contents (United Kingdom)

Abstract The synthesis, crystal structure and magnetic characterisation by magnetisation and inelastic neutron scattering (INS) of a mixed-valent Mn10 supertetrahedral aggregate [MnIII6MnII4(4-O)4(3-N3)3(3-Br)(Hmpt)6(Br)]Br0.7(N3)0.3-2-MeOH-3-MeCN (1) (H3mpt=3-methylpentan-1,3,5-triol) is reported. The magnetic core of the molecule can be described as an octahedron of six S=2 MnIII ions with four faces, each capped by a S=5/2 MnII ion such as to form the supertetrahedron. Unlike most related complexes, the molecular symmetry is slightly reduced from approximately Td to C3. The magnetic data reveal a total spin of S=22 in the ground state due to ferromagnetic exchange couplings within the molecule. The combined INS and magnetic data permits the accurate determination of the exchange couplin...

2011-01-01

479

Equilibrium, kinetics and thermodynamic studies on phosphate biosorption from aqueous solutions by Fe(III)-treated Staphylococus xylosus biomass: Common ion effect

British Library Electronic Table of Contents (United Kingdom)

The biosorption of phosphate from aqueous solutions using Fe(III)-treated Staphylococus xylosus cells was investigated. Langmuir and Freundlich isotherm models were applied to describe the adsorption equilibrium and found that Langmuir isotherm model fitted the equilibrium data better than Freundlich isotherm model. The biosorption capacity of Fe(III)-treated biomass for phosphate was found to be 70.92mg/g at optimum conditions of pH 3.0, biomass concentration 0.5g/L and equilibrium phosphate-biomass time 60min respectively. The sorption efficiency at initial phosphate concentration of 50mg/L was not influenced upon addition of SO4^2^-, Cl^-, CO3^2^-, NO3^-, Mg^2^+ and Ca^2^+ ions from 0 to 800mg/L, whereas under the same conditions, phosphate sorption was increased with increase in concen...

2011-01-01

480

Environmental impact assessment around TRIGA research reactor

Electrochemical corrosion behavior of alloy 400: Intergranular corrosion in acidic Na_2SO_4 solutions

Population distribution, atmospheric change, X/Q, characteristics of terrestrial ecosystem around Seoul site were surveyed. Environmental radiation and radioactivities such as gross#alpha#, gross#beta#, Cs-137, Sr-90 and H-3 of various environmental samples were analyzed. The values of environmental radiation dose tended to increase gradually in the light of the recent five years' results of environmental radiation monitoring around the nuclear power plants from 1980 to 1984, however, the changes were not significant. In addition, continuous assessment of environmental radiation monitoring on the roofs of main building and life science building at KAERI showed that the environmental radiation dose tended to increase a little during the night time. Judging from the above results, it is concluded that environmental contamination level by radioactive materials could be ignored in the case of radioisotope production or experiment using ...

1985-04-01

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25

481

Effect on heat-transfer augmentation by channel width in a sinusoidal wave channel

The influence of heat treatments on the anodic polarization behavior of alloy 400 in acidic Na_2SO_4 solutions with different pH values and chloride contents has been studied. Alloy 400 is susceptible to intergranular corrosion (IGC) in 0.5 N Na_2SO_4 solution (pH 3) containing 0.2% CuCl_2. For the same heat treatment (soaking for one hour at 900 C), the extent of IGC appears to be significantly affected by the cooling rate, which is greater for faster cooling (e.g., water quenching). Aging the water-quenched alloy at 500 C enhances IGC susceptibility, and aging at higher temperatures imparts resistance to IGC. Note that addition of small amounts of hafnium has a beneficial effect on the resistance to IGC of alloy 400 under similar exposure conditions. An attempt has been made to rationalize the observations in terms of segregation of sulfur and phosphorus to the grain boundaries.

482

Effect of external pH on the cytoplasmic and vacuolar pHs in Mung bean root-tip cells. A T P nuclear magnetic resonance study

In the development of high performance heat transfer surface on a compact heat exchanger, it was clarified that how reattachment point heat transfer and fluid flow are affected by channel width, at the same time, an evaluation of heat transfer performance and an investigation of optimum channel width were carried out. The channel system used in the experiment is as follows; (1) blow-off type with rectangular section channel, (2) span length of 200 mm, (3) wave length (pitch) of 80 mm, and (4) channel length of 12.5 wave length. The channel Reynolds number was set at about 10/sup 4/ which is relatively higher than the current studies. The results of the experiment were summarized as follows. (1) The channel width H has relevance to the phase difference between the fluid flow in cone portion of main stream and wave shape, the flow patterns are divided roughly into three types. These boundaries exist at P/H 3.0 and 1.5 (P: pitch, H: width). (2) ...

1988-06-25

483

Effect of external pH on the cytoplasmic and vacuolar pHs in Mung bean root-tip cells

The effect of the external pH on the intracellular pH in mung bean (Vigna mungo (L.) Hepper) root-tip cells was investigated with the T P nuclear magnetic resonance (NMR) method. The T P NMR spectra showed three peaks caused by cytoplasmic G-6-P, cytoplasmic Psub(i) and vacuolar Psub(i). The cytoplasmic and vacuolar pHs could be determined by comparing the Psub(i) chemical shifts with the titration curve. When the external pH was changed over a range from pH 3 to 10, the cytoplasmic pH showed smaller changes than the vacuolar pH, suggesting that the former is regulated more strictly than the latter. The H -ATPase inhibitor, DCCD, caused the breakdown of the mechanism that regulates the intracellular pH. H -ATPase appears to have an important part in the regulation of the intracellular pH.

1984-12-01

484

Development of value-added products from alumina industry mineral wastes using low-temperature-setting phosphate ceramics

The effect of the external pH on the intracellular pH in mung bean (Vigna mungo (L.) Hepper) root-tip cells was investigated with the "3"1P nuclear magnetic resonance (NMR) method. The "3"1P NMR spectra showed three peaks caused by cytoplasmic G-6-P, cytoplasmic Psub(i) and vacuolar Psub(i). The cytoplasmic and vacuolar pHs could be determined by comparing the Psub(i) chemical shifts with the titration curve. When the external pH was changed over a range from pH 3 to 10, the cytoplasmic pH showed smaller changes than the vacuolar pH, suggesting that the former is regulated more strictly than the latter. The H"+-ATPase inhibitor, DCCD, caused the breakdown of the mechanism that regulates the intracellular pH. H"+-ATPase appears to have an important part in the regulation of the intracellular pH. (author).

485

Determination of impurities in sialon by ICP-AES

A room-temperature process for stabilizing mineral waste streams has been developed, based on acid-base reaction between MgO and H3PO4 or acid phosphate solution. The resulting waste form sets into a hard ceramic in a few hours. In this way, various alumina industry wastes, such as red mud and treated potliner waste, can be solidified into ceramics which can be used as structural materials in waste management and construction industry. Red mud ceramics made by this process were low-porosity materials ({approx}2 vol%) with a compression strength equal to portland cement concrete (4944 psi). Bonding mechanism appears to be result of reactions of boehmite, goethite, and bayerite with the acid solution, and also encapsulation of red mud particles in Mg phosphate matrix. Possible applications include liners for ponds and thickned tailings disposal, dikes for waste ponds, and grouts. Compatability problems arising at the interface of the liner and ...

1996-01-01

486

Bar Diagnostics in Edge-On Spiral Galaxies. III. N-Body Simulations of Disks

Impurities (Ca, Cr, Cu, Fe, K, Mg, Mn, Na, Ni, Ti, Y, Zn and Zr) in sialon powder were determined by the following procedure: A sample (0.5 g) was heated with a mixture of hydrofluoric acid (3 ml) and nitric acid (1 ml) in a Teflon pressure vessel at 170degC for 16 h. The contents of the vessel were transferred into a platinum crucible containing phosphoric acid (4 ml) and heated on a hot plate until the opaque appearance of the content changed to a clear-syrupy fluid. The fluid was diluted to 100 ml with water and used for ICP-AES analysis of all impurity elements except K, which was determined by AAS. It was necessary to match closely the matrix concentrations (H_3PO_4, Al and/or Y) of the standard solutions with those of sialon sample solutions for the determination of impurities because of interferences of the matrix components. This method was successfully applied to the determination of impurities in commercial sialon samples. (author).

487

A comparison of the low cycle fatigue behavior of alloy 800 and alloy 800H

Present in over 45% of local spirals, boxy and peanut-shaped bulges are generally interpreted as edge-on bars and may represent a key phase in the evolution of bulges. Aiming to test such claims, the kinematic properties of self-consistent 3D N-body simulations of bar-unstable disks are studied. Using Gauss-Hermite polynomials to describe the stellar kinematics, a number of characteristic bar signatures are identified in edge-on disks: 1) a major-axis light profile with a quasi-exponential central peak and a plateau at moderate radii (Freeman Type II profile); 2) a ``double-hump'' rotation curve; 3) a sometime flat central velocity dispersion peak with a plateau at moderate radii and occasional local central minimum and secondary peak; 4) an h3-V correlation over the projected bar length. All those kinematic features are spatially correlated and can easily be understood from the orbital structure of barred disks. They thus provide a reliable ...

2004-01-01

488

Effect of D-amino acids at Asp"2"3 and Ser"2"6 residues on the conformational preference of A#beta#_2_0_-_2_9 peptides

The low cycle fatigue testing was carried out to provide a basis for comparison of the behavior of the two kinds of Alloy 800 (low carbon Alloy 800 and high carbon Alloy 800H). The testing was done at temperatures of 500"0C and 650"0C either with or without hold. The results obtained were as follows: (1) At 650"0C, the low-cycle fatigue life was essentially the same for the two alloys on the basis of strain amplitude, but Alloy 800H had a longer life on the basis of stress amplitude. (2) At 500"0C, the two alloys exhibited longer lives than at 650"0C, with Alloy 800 exhibiting 2-3 times longer life than Alloy 800H when compared on the basis of plastic strain range. At this temperature the stress range showed the maximum for Alloy 800H. (3) When a creep effect was introduced either by way of a hold time or a reduced frequency, Alloy 800 exhibited a greater reduction in life than in Alloy 800H. (4) At lower temperature the strain aging phenomena ...

1979-06-01

489

Studies on sugar recognizing and binding protein (lectin) in marine invertebrates (physiological control of lectin); Kaiyo musekitsui dobutsu no toninshiki ketsugo tanpakushitsu (lectin) ni kansuru kenkyu (lectin no seiriteki seigyo)

The effects of D-amino acids at Asp"2"3 and Ser"2"6 residues on the conformational preference of #beta#-amyloid (A#beta#) peptide fragment (A#beta#_2_0_-_2_9) have been studied using different spectroscopic techniques, namely vibrational circular dichroism (VCD), vibrational absorption, and electronic circular dichroism. To study the structure of the A#beta#_2_0_-_2_9, [D-Asp"2"3]A#beta#_2_0_-_2_9, and [D-Ser"2"6]A#beta#_2_0_-_2_9 peptides under different conditions, the spectra were measured in 10 mM acetate buffer (pH 3) and in 2,2,2-trifluoroethanol (TFE). The spectroscopic results indicated that at pH 3, A#beta#_2_0_-_2_9 peptide takes random coil with #beta#-turn structure, while [D-Ser"2"6]A#beta#_2_0_-_2_9 peptide adopts significant amount of polyproline II (PPII) type structure along with #beta#-turn contribution and D-Asp-substituted peptide ([D-Asp"2"3]A#beta#_2_0_-_2_9) adopts predominantly ...

2005-09-30

490

Spectroscopic studies on the interaction of the antibiotic lasalocid A (x-537a) with technetium (V) ions in methanol

Lectin is a generic name of sugar binding protein in living organisms. With an objective to clarify physiological functions of lectin in marine invertebrates and utilize it as a useful material in the bio-chemical industry, studies were carried out on the chemical structure, distribution in living organisms and structural changes of lectin. Lectin is involved with such physiological actions as immunity reactions, generation and differentiation, Ca fixation and symbiosis. Lectin is one of the main components of lymph fluid in shellfish and crustacean, and is a multi-functional polymer that is related with foreign substance recognition, Ca transport, and shell formation. Lectin of a certain kind shows strong actions to accelerate cell division. Organs and cells were cultivated for lectin producing organs and lectin producing cells to verify the production thereof. Elucidation was attempted in a molecular level on such physiological functions as foreign substance ...

1993-03-01

491

Radiation-induced changes in the cell membrane of cultured human endothelial cells

In the present study, the authors examine the interactions of pentavalent technetium ions (TcO/sup 3+/) with the basic form of the lasalocid A in pure methanol solvent and in methanol-water mixtures. There are a number of reasons for such a study. First, the interactions of technetium ions with biologically important compounds are of considerable importance owing to the widespread use of /sup 99m/Tc in diagnostic radio-imaging. Second, lasalocid A is known to transport metal ions across phospholipid bilayer membranes and between the aqueous cores of phospholipid inverse micelles. Third, lasalocid A is known to bind and solubilize metal ions in bulk organic liquid phases. Fourth, the conformation adopted by lasalocid A on interaction with TcO/sup 3+/ appears to be different than those found in most other cases and circumstances. Fifth, it may also be possible to use the competition of TcO/sup 3+/ with other, physiologically relevant cations (Na/sup +/, K/sup +/, ...

492

Poncirin promotes osteoblast differentiation but inhibits adipocyte differentiation in mesenchymal stem cells.

We investigated the effect of irradiation on the kinetic characteristics of amino acid and glucose transport, and the effect on the activity of the cell membrane-bound enzyme 5'-nucleotidase and on the receptor-mediated stimulation of cyclic adenosine monophosphate synthesis by prostaglandin E1. Irradiation inhibited the sodium-dependent amino acid transport by a reduced binding of the amino acid to the transport unit. The transport of glucose, which appeared to be a sodium-independent process, was temporarily stimulated by increased maximal velocity of the transport. No effect was found on the binding to the transport unit. Irradiation increased the 5'-nucleotidase activity and decreased the prostaglandin E1-stimulated cyclic adenosine monophosphate synthesis 48 h after exposure to 20 Gy. It is concluded that irradiation decreases sodium-dependent transport by impairment of the transport unit, does not impair a ...

1985-12-01

493

Phosphomimetic mutation of the mitotically phosphorylated serine 1880 compromises the interaction of the transmembrane nucleoporin gp210 with the nuclear pore complex

Poncirin, flavanone glycoside, isolated from the fruit of Poncirus trifoliata, has anti-bacterial and anti-inflammatory activities. In this study, the effects of poncirin on the differentiation of mesenchymal stem cells were investigated. The C3H10T1/2 mesenchymal stem cells and primary bone marrow mesenchymal stem cells were studied. In the C3H10T1/2 cells, poncirin prevented adipocyte differentiation, as demonstrated by inhibition of cytoplasm lipid droplet accumulation and peroxisome proliferator-activating receptor-? (PPAR-?) and CCAAT-enhancer-binding protein-? (C/EBP-?) mRNA expression. By contrast, poncirin enhanced the expression of the key osteogenic transcription factors, runt-related transcription factor 2 (Runx2) and transcriptional coactivator with PDZ-binding motif (TAZ). Poncirin also enhanced expression of the osteogenic marker genes including alkaline phosphatase (ALP) and osteocalcin (OC). Poncirin increased mineral nodule ...

2011-05-01

494

Influence of valency and labelling chemistry on in vivo targeting using radioiodinated HER2-binding Affibody molecules

The nuclear pore complexes (NPCs) reversibly disassemble and reassemble during mitosis. Disassembly of the NPC is accompanied by phosphorylation of many nucleoporins although the function of this is not clear. It was previously shown that in the transmembrane nucleoporin gp210 a single serine residue at position 1880 is specifically phosphorylated during mitosis. Using amino acid substitution combined with live cell imaging, time-lapse microscopy and FRAP, we investigated the role of serine 1880 in binding of gp210 to the NPC in vivo. An alanine substitution mutant (S1880A) was significantly more dynamic at the NPC compared to the wild-type protein, suggesting that serine 1880 is important for binding of gp210 to the NPC. Moreover a glutamate substitution (S1880E) closely mimicking phosphorylated serine specifically interfered with incorporation of gp210 into the NPC and compromised its post-mitotic recruitment to the nuclear envelope of ...

2007-07-15

495

British Library Electronic Table of Contents (United Kingdom)

Purpose HER2 is a transmembrane tyrosine kinase, which is overexpressed in a number of carcinomas. The Affibody molecule ZHER2:342 is a small (7?kDa) affinity protein binding to HER2 with an affinity of 22?pM. The goal of this study was to evaluate the use of ((4-hydroxyphenyl)ethyl)maleimide (HPEM) for radioiodination of ZHER2:342 and to compare the targeting properties of monomeric and dimeric forms of ZHER2:342. Methods The biodistribution of different radioiodinated derivatives of ZHER2:342 was studied in BALB/C nu/nu mice bearing HER2-expressing SKOV-3 xenografts. Biodistributions of 125I-PIB-ZHER2:342 and site-specifically labelled 125I-HPEM-ZHER2:342-C were compared. Biodistributions of monomeric 131I-HPEM-ZHER2:342-C and dimeric 125I-HPEM-(ZHER2:342)2-C were evaluated using a paire...

2009-01-01

496

Homology analyses of the protein sequences of fatty acid synthases from chicken liver, rat mammary gland, and yeast

Effect of butylated hydroxytoluene pretreatment on the excretion, tissue distribution and DNA binding of (/sup 14/C)aflatoxin B1 in the rat

Homology analyses of the protein sequences of chicken liver and rat mammary gland fatty acid synthases were carried out. The amino acid sequences of the chicken and rat enzymes are 67% identical. If conservative substitutions are allowed, 78% of the amino acids are matched. A region of low homologies exists between the functional domains, in particular around amino acid residues 1059-1264 of the chicken enzyme. Homologies between the active sites of chicken and rat and of chicken and yeast enzymes have been analyzed by an alignment method. A high degree of homology exists between the active sites of the chicken and rat enzymes. However, the chicken and yeast enzymes show a lower degree of homology. The DADPH-binding dinucleotide folds of the {beta}-ketoacyl reductase and the enoyl reductase sites were identified by comparison with a known consensus sequence for the DADP- and FAD-binding dinucleotide folds. The active sites of all of the enzymes ...

1989-11-01

497

Calmodulin Kinase II Interacts with the Dopamine Transporter C Terminus to Regulate Amphetamine-Induced Reverse Transport

The effect of butylated hydroxytoluene (BHT) pretreatment (0.5% in the diet for 10 days) on the excretion, tissue distribution and DNA binding of orally administered (/sup 14/C)aflatoxin B1 (AFB1) was determined in male Fischer F344 rats. The amount of radioactivity excreted in the urine and feces by 24 hr was higher in BHT-treated rats than in controls. Treatment with BHT enhanced the excretion of water-soluble metabolites in the urine and in the large intestines plus feces at the earlier sampling times. The amount of radioactivity bound to hepatic nuclear DNA was six times less in the BHT-pretreated rats than in controls 6 hr after administration of the isotope. The half-lives of (/sup 14/C)DNA in the rat liver were 30 and 46 hr for control and BHT-pretreated rats, respectively. These results indicate that BHT pretreatment may protect the animal from the carcinogenic effects of AFB1 by enhancing the detoxification and excretion of the mycotoxin.

1985-06-01

498

DEFF Research Database (Denmark)

Efflux of dopamine through the dopamine transporter (DAT) is critical for the psychostimulatory properties of amphetamines, but the underlying mechanism is unclear. Here we show that Ca(2+)/calmodulin-dependent protein kinase II (CaMKII) plays a key role in this efflux. CaMKIIalpha bound to the distal C terminus of DAT and colocalized with DAT in dopaminergic neurons. CaMKIIalpha stimulated dopamine efflux via DAT in response to amphetamine in heterologous cells and in dopaminergic neurons. CaMKIIalpha phosphorylated serines in the distal N terminus of DAT in vitro, and mutation of these serines eliminated the stimulatory effects of CaMKIIalpha. A mutation of the DAT C terminus impairing CaMKIIalpha binding also impaired amphetamine-induced dopamine efflux. An in vivo role for CaMKII was supported by chronoamperometry measurements showing reduced amphetamine-induced dopamine efflux in response to the CaMKII inhibitor KN93. Our data suggest that CaMKIIalpha ...

2006-01-01

499

A single amino acid substitution results in a retinoblastoma protein defective in phosphorylation and oncoprotein binding