WorldWideScience
1

Thymol, a constituent of thyme essential oil, is a positive allosteric modulator of human GABAA receptors and a homo-oligomeric GABA receptor from Drosophila melanogaster  

UK PubMed Central (United Kingdom)

The GABA-modulating and GABA-mimetic activities of the monoterpenoid thymol were explored on human GABAA and Drosophila melanogaster...Full Text Available

2003-12-01

2

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

International Nuclear Information System (INIS)

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 reduced by ethanol (#<=# 100 mM ethanol). Chronic ethanol ingestion in vivo, ...

3

Temporal development of GABA agonist induced alterations in ultrastructure and GABA receptor expression in cultured cerebellar granule cells  

DEFF Research Database (Denmark)

The temporal development of the effect of THIP (4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol) on the ultrastructure composition and GABA receptor expression in cerebellar granule cells was investigated by quantitative electron microscopy (morphometric analysis) and GABA binding assays. It was found that the cytoplasmic density of smooth endoplasmic reticulum was decreased, while the cytoplasmic density of rough endoplasmic reticulum, Golgi apparatus, vesicles and coated vesicles was greatly enhanced after exposure of the cells to THIP (150 microM) for only 1 hr. In cerebellar granule cells exposed to THIP (150 microM) for 3 hr low affinity GABA receptors were induced. These findings show that the effect of THIP on the ultrastructure composition and GABA receptor expression in cultured cerebellar granule cells may be interrelated and ...

1987-01-01

4

Neuroactive steroids have multiple actions to potentiate GABAA receptors  

UK PubMed Central (United Kingdom)

The effects of neuroactive steroids on the function of GABAA receptors were studied using cell-attached records of single channel activity recorded from HEK293 cells transfected with α1...Full Text Available

2004-07-01

5

New insights into purinergic receptor signaling in neuronal differentiation, neuroprotection, and brain disorders  

UK PubMed Central (United Kingdom)

Ionotropic P2X and metabotropic P2Y purinergic receptors are expressed in the central nervous system and participate in the synaptic process particularly associated with acetylcholine, GABA, and glutamate...Full Text Available

2007-09-01

6

Zero net flux estimates of septal extracellular glucose levels and the effects of glucose on septal extracellular GABA levels  

UK PubMed Central (United Kingdom)

Although hippocampal infusions of glucose enhance memory, we have found repeatedly that septal glucose infusions impair memory when γ-aminobutyric acid (GABA) receptors are activated....Full Text Available

2009-06-02

7

Beyond Acid Suppression: New Pharmacologic Approaches for Treatment of GERD  

British Library Electronic Table of Contents (United Kingdom)

Proton pump inhibitors are highly successful in treating gastroesophageal reflux disease, but a significant proportion of patients have persistent symptoms from weakly or nonacidic reflux. Transient lower esophageal sphincter relaxation (TLESR) represents the dominant mechanism of gastroesophageal reflux and has therefore become the most intensely investigated therapeutic target. The triggering of TLESR involve the vagal pathways and the ?-aminobutyric type B (GABA(B)) and metabotropic glutamate type 5 (mGluR5) receptors. Baclofen is a GABA(B) receptor agonist that is effective in inhibiting TLESR and reducing the number of reflux episodes, but is associated with significant central nervous system (CNS) side effects. The newer GABA(B) agonists, such as AZD9343 and AZD3355, and mGluR5 antag...

2010-01-01

8

Blockade of androgen receptors is sufficient to alter the sexual differentiation of the substantia nigra pars reticulata seizure-controlling network  

UK PubMed Central (United Kingdom)

The substantia nigra pars reticulata (SNR) controls seizures in a sex-specific manner. At postnatal day 15 (P15), SNR infusion of GABAA receptor agonist muscimol have proconvulsant...Full Text Available

2008-03-01

9

Altered GABAA receptor-mediated synaptic transmission disrupts the firing of gonadotropin-releasing hormone neurons in male mice under conditions that mimic steroid abuse  

UK PubMed Central (United Kingdom)

Gonadotropin–releasing hormone (GnRH) neurons are the central regulators of reproduction. GABAergic transmission plays a critical role in pubertal activation of pulsatile GnRH secretion....Full Text Available

2010-05-12

10

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

Science.gov (United States)

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 ...

1990-02-26

11

Nerve growth factor actions on the brain  

International Nuclear Information System (INIS)

We examined the effect of the trophic protein, nerve growth factor (NGF), on cultures of fetal rat neostriatum and basal forebrain-medial septal area (BF-MS) to define its role in brain development. Treatment of cultures with NGF resulted in an increase in the specific activity of the cholinergic enzyme choline acetyltransferase (CAT) in both brain areas. CAT was immunocytochemically localized to neurons. In the BF-MS, NGF treatment elicited a marked increase in staining intensity and an apparent increase in the number of CAT-positive neurons. Moreover, treatment of BF-MS cultures with NGF increased the activity of acetylcholinesterase, suggesting that the cholinergic neuron as a whole was affected. To begin defining mechanisms of action of NGF in the BF-MS, we detected NGF receptors by two independent methods. Receptors were localized to two different cellular populations: neuron-like cells, and non-neuron-like cells. Dissociation studies with ...

13

Factors affecting actions of ethanol on GABA-activated chloride channels  

International Nuclear Information System (INIS)

Effects of ethanol in vitro on membrane vesicles were evaluated by monitoring "3"6Cl"- influx. Different assay parameters were tested to determine increased or decreased action of ethanol on GABA-activated chloride channels. The ability of 30 mM ethanol to augment "3"6Cl"- flux was seen at 0 degree C, in the absence of GABA, and at 34 degree C in the presence of GABA, using two different assay procedures. Picrotoxin blocked the direct effects of ethanol suggesting GABA_a involvement. Endogenous GABA in the medium surrounding the microsacs was assayed at different temperatures both in the presence and absence of GABA and ethanol. The direct effect of ethanol did not appear to involve the action of endogenous GABA. In addition to temperature effects on the assay, time of membrane storage also influenced ethanol action. Microsacs stored on ice ...

14

Kinetic Complexity of the Global Response to Glucocorticoid Receptor Action  

UK PubMed Central (United Kingdom)

We have characterized the kinetic response of gene targets throughout the murine genome to transcriptional modulation by the glucocorticoid receptor (GR). In contrast to a model in which multiple genes...Full Text Available

2009-04-01

15

Effects of cultivar and culture conditions on g-aminobutyric acid accumulation in germinated fava beans (Vicia faba L.)  

British Library Electronic Table of Contents (United Kingdom)

BACKGROUND: High levels of g-aminobutyric acid (GABA) accumulate in plant tissues under various stresses. GABA accumulation is also influenced by cultivar. This aim of this study was to select the most promising cultivar of fava bean for GABA accumulation and to optimise the culture conditions for GABA production in germinated fava beans by response surface methodology based on central composite design (CCD). RESULTS: GABA content and glutamate decarboxylase activity in germinated seeds of cultivar S2 were significantly higher than those in other cultivars (P < 0.05). A significant negative correlation (r = -0.765, P < 0.05) between germination percentage and 1000-kernel weight was observed. There was a linear relationship between GABA content and sprout length (R2 = 0.816). The regression...

2010-01-01

16

Kinetic manifestation of cooperative interaction between quinuclidinyl benzilate and rat brain muscarine cholinoreceptors  

Energy Technology Data Exchange (ETDEWEB)

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 antagonists and muscarine ...

1985-01-01

17

Genetic Modulation of GABA Levels in the Anterior Cingulate Cortex by GAD1 and COMT  

UK PubMed Central (United Kingdom)

γ-Aminobutyric acid (GABA)-ergic transmission is critical for normal cortical function and is likely abnormal in a variety of neuropsychiatric disorders. We tested the in...Full Text Available

2010-07-01

18

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

UK PubMed Central (United Kingdom)

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

19

Internalized insulin-receptor complexes are unidirectionally translocated to chloroquine-sensitive degradative sites. Dependence on metabolic energy  

Energy Technology Data Exchange (ETDEWEB)

Insulin receptors on the surface of isolated rat adipocytes were photoaffinity labeled at 12 degrees C with the iodinated photoreactive insulin analogue, 125I-B2 (2-nitro-4-azidophenylacetyl)-des-PheB1-insulin, and the pathways in the intracellular processing of the labeled receptors were studied at 37 degrees C. During 37 degrees C incubations, the labeled 440-kDa insulin receptors were continuously internalized (as assessed by trypsin inaccessibility) and degraded such that up to 50% of the initially labeled receptors were lost by 120 min. Metabolic poisons (0.125-0.75 mM 2,4-dinitrophenol (DNP) and 1-10 mM NaF), which led to dose-dependent depletion of adipocyte ATP pools, inhibited receptor loss, and caused up to 3-fold increase in intracellular receptor accumulation. This effect was due to inhibition of intracellular receptor ...

1988-04-25

20

Cumulus expansion, nuclear maturation and connexin 43, cyclooxygenase-2 and FSH receptor mRNA expression in equine cumulus-oocyte complexes cultured in vitro in the presence of FSH and precursors for hyaluronic acid synthesis  

UK PubMed Central (United Kingdom)

The aim of this study was to investigate cumulus expansion, nuclear maturation and expression of connexin 43, cyclooxygenase-2 and FSH receptor transcripts in equine cumuli oophori during in vivo and...Full Text Available

21

Synapse-Associated Protein 102/dlgh3 Couples the NMDA Receptor to Specific Plasticity Pathways and Learning Strategies  

UK PubMed Central (United Kingdom)

Understanding the mechanisms whereby information encoded within patterns of action potentials is deciphered by neurons is central to cognitive psychology. The multiprotein complexes formed by...Full Text Available

2007-03-07

22

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

International Nuclear Information System (INIS)

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) ...

1987-01-01

23

Insight into Thyroid-Stimulating Autoantibody Interaction with the Thyrotropin Receptor N-Terminus Based on Mutagenesis and Re-Evaluation of Ambiguity in This Region of the Receptor Crystal Structure  

British Library Electronic Table of Contents (United Kingdom)

Background: Thyroid-stimulating autoantibodies (TSAb) bind to the thyrotropin receptor (TSHR) extracellular domain, or ectodomain (ECD), comprising a leucine-rich repeat domain (LRD) linked by a hinge region to the transmembrane domain (TMD). The LRD (residues 22???260; signal peptide 1???21) contains two disulfide-bonded loops at its N-terminus. In the crystal structure of the isolated LRD complexed with human TSAb monoclonal antibody (mAb) M22, N-terminal disulfide loop 1 (residues 22???30) could not be determined because of crystal disorder. Nevertheless, present crystal structure data are interpreted to exclude a role for the LRD N-terminal disulfide loops in the TSAb epitope(s), contradicting prior functional evidence of a role for these loops in TSAb function. Materials and Methods: ...

2011-01-01

24

T cell receptor beta chain from sea bream (Sparus aurata): Molecular cloning, expression and modelling of the complexes with MHC class I  

British Library Electronic Table of Contents (United Kingdom)

The T cell receptor is a fundamental mediator of the adaptive immune responses, since TR ab on T cells recognize foreign structures (peptides derived from processed antigens) bound to the major histocompatibility complex (MHC) on APC cells. In the present study, we report the cloning of six TRB chains cDNA sequences from gilthead sea bream (Sparus aurata), a fish of high economical impact in South Mediterranean aquaculture. The V-BETA domains have the canonical features of known teleost and mammalian TR V-BETA domains and have been divided in four different subgroups. A multiple alignment of the six sea bream TRB chains with other known TRB sequences was assembled and showed the conservation of the four cysteine residues involved in disulphide bonds and of some amino acids with an importan...

2008-01-01

25

Selective Excitatory Actions of DNQX and CNQX in Rat Thalamic Neurons  

UK PubMed Central (United Kingdom)

The thalamic reticular nucleus (TRN) consists of GABA-containing neurons that form reciprocal synaptic connections with thalamic relay nuclei. Excitatory synaptic innervation of TRN neurons arises from...Full Text Available

2010-04-01

26

Long-term synaptic transformation of hippocampal CA1 gamma-aminobutyric acid synapses and the effect of anandamide.  

UK PubMed Central (United Kingdom)

Evidence is presented for a distinctive type of hippocampal synaptic modification [previously described for a molluscan gamma-aminobutyric acid (GABA) synapse after paired pre- and postsynaptic excitation]:...Full Text Available

1995-10-24

27

Cerebrospinal fluid zinc concentrations in febrile convulsions.  

UK PubMed Central (United Kingdom)

Zinc modulates the activity of glutamic acid decarboxylase, the rate limiting enzyme in the synthesis of gamma-aminobutyric acid (GABA), which is a major inhibitory neurotransmitter. Low cerebrospinal...Full Text Available

1995-10-01

28

Small and neutral Tc"vO BAT, bisaminoethanethiol (N_2S_2) complexes for developing new brain imaging agents  

International Nuclear Information System (INIS)

Bisaminoethanethiol (BAT) ligands with various gem-dimethyl and amide groups were prepared, and the corresponding neutral Tc-99m complexes were prepared and evaluated for their relative stabilities by ligand-exchange reactions. It was demonstrated that technetium complexes containing gem-dimethyl substituents have higher lipophilicities, whereas those with an amide group possess greater stability, which enhances ligand-exchange reaction. The most interesting observation was that the brain uptake in rats is not determined only by lipophilicity. Apparently, Tc-99m complexes with an amide functional group display lower brain uptakes in rats compared to those without an amide group. The brain uptake was strongly influenced by substituents on the BAT ligand. These factors are critically important and should be taken into consideration when designing Tc-99m-labeled agents for CNS receptor imaging.

1998-02-01

29

Regulation of NMDA and AMPA receptors during the maturation phase of chicken brain development  

International Nuclear Information System (INIS)

Full text: The maturation of chicken forebrain is protracted and occurs well after synapse formation providing a good model for studying mechanisms of brain maturation. Using microslices from immature (10 day) and adult chicken forebrain prepared after decapitation, we have examined functional properties of NMDA and AMPA receptors by measuring agonist-induced uptake of "4"5Ca"2"+ . The rate and extent of NMDA induced "4"5Ca"2"+ accumulation decreased during maturation with no change in EC_5_0. The rate and extent of the AMPA induced response also decreased with a 60-fold increase in EC_5_0. However, the total NMDA receptor content did not change as indicated by 3 H-MK801 binding and NR1 immunoreactivity in P2 fractions. Similarly, there was no change in the B_m_a_x of "3H-AMPA, though there was a two-fold increase in K_D, and little or no change in the immunoreactivity in GluR1, 2, 2/3 or 4. These results suggest that it is the regulation of ...

2002-02-04

30

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

International Nuclear Information System (INIS)

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 ...

31

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

International Nuclear Information System (INIS)

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

32

Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor  

Energy Technology Data Exchange (ETDEWEB)

Crystallography and computer modeling have been used to exploit a previously unexplored channel in the glucocorticoid receptor (GR). Highly potent, nonsteroidal indazole amides showing excellent complementarity to the channel were designed with the assistance of the computational technique AlleGrow. The accuracy of the design process was demonstrated through crystallographic structural determination of the GR ligand-binding domain-agonist complex of the D-prolinamide derivative 11. The utility of the channel was further exemplified through the design of a potent phenylindazole in which structural motifs, seen to interact with the traditional GR ligand pocket, were abandoned and replaced by interactions within the new channel. Occupation of the channel was confirmed with a second GR crystal structure of this truncated D-alaninamide derivative 13. Compound 11 displays properties compatible with development as an intranasal solution formulation, ...

2010-09-17

33

Small and neutral Tc{sup v}O BAT, bisaminoethanethiol (N{sub 2}S{sub 2}) complexes for developing new brain imaging agents  

Energy Technology Data Exchange (ETDEWEB)

Bisaminoethanethiol (BAT) ligands with various gem-dimethyl and amide groups were prepared, and the corresponding neutral Tc-99m complexes were prepared and evaluated for their relative stabilities by ligand-exchange reactions. It was demonstrated that technetium complexes containing gem-dimethyl substituents have higher lipophilicities, whereas those with an amide group possess greater stability, which enhances ligand-exchange reaction. The most interesting observation was that the brain uptake in rats is not determined only by lipophilicity. Apparently, Tc-99m complexes with an amide functional group display lower brain uptakes in rats compared to those without an amide group. The brain uptake was strongly influenced by substituents on the BAT ligand. These factors are critically important and should be taken into consideration when designing Tc-99m-labeled agents for CNS receptor imaging.

1998-02-01

34

Allosteric Tuning of the Intra-Cavity Binding Properties of a Calix[6]arene through External Binding to a ZnII Center Coordinated to Amino Side Chains  

British Library Electronic Table of Contents (United Kingdom)

Molecular recognition by calix[6]arene-based receptors bearing three primary alkylamino side chain arms (1) is described. Complexation of ZnII ion provides the dinuclear m-hydroxo complex ${{\\bf 2}{{{\\rm OH}\\hfill \\atop {\\rm G}\\hfill}}}$, XRD characterization of which, together with solution studies, provided evidence of its hosting of neutral polar organic guests G. Treatment of this complex with a carboxylic acid or a sulfonamide (XH) results in the formation of mononuclear species ${{\\bf 3}{{{\\rm X}\\hfill \\atop {\\rm G}\\hfill}}}$, one of which (X = Cl) has been characterized by XRD. A dicationic complex ${{\\bf 3}{{{\\rm RNH}{_{2}}\\hfill \\atop {\\rm G}\\hfill}}}$ is obtained upon treatment of ${{\\bf 2}{{{\\rm OH}\\hfill \\atop {\\rm G}\\hfill}}}$ with a mixture of an alkylamine and a strong acid....

2007-01-01

35

The structure of receptor-associated protein (RAP)  

UK PubMed Central (United Kingdom)

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

36

Structure and function of an acetylcholine receptor.  

UK PubMed Central (United Kingdom)

Structural analysis of an acetylcholine receptor from Torpedo californica leads to a three-dimensional model in which a "monomeric" receptor is shown to contain subunits arranged around a central ionophoretic...Full Text Available

1982-01-01

37

Orphan GPCR research  

UK PubMed Central (United Kingdom)

Orphan G protein-coupled receptors (GPCRs) are receptors lacking endogenous ligands. Found by molecular biological analyses, they became the roots of reverse pharmacology, in which receptors are attempted...Full Text Available

2008-03-01

38

Bioengineered bugs expressing oligosaccharide receptor mimics  

UK PubMed Central (United Kingdom)

Many microbial pathogens recognize oligosaccharides displayed on the surface of host cells as receptors for toxins and adhesins. These ligand-receptor interactions are critical for disease pathogenesis,...Full Text Available

2010-05-01

39

AMPA-receptor trafficking and injury-induced cell death  

UK PubMed Central (United Kingdom)

AMPA receptors (AMPARs) are critical for synaptic plasticity, and are subject to alterations based on subunit composition and receptor trafficking to and from the plasma membrane. One of the...Full Text Available

2010-07-01

40

Synthesis, solid and solution studies of paraquat dichloride calixarene complexes. Molecular modelling  

International Nuclear Information System (INIS)

The interaction of the herbicide paraquat dichloride (P Q, substrate) with p-tert-butylcalix arenas (L, receptor) was investigated in both the solution and solid states. The isolated paraquat calixarene complexes were characterised by UV-visible, 1H NMR, ESI-Ms, Luminescence and IR spectroscopies and elemental analysis. The stoichiometry of complexes 1 and 2 was 1:1 (1 herbicide: 1 calixarene) and both revealed a biexponential luminescence decay with lifetimes depending on the size and the conformational particularity of the calixarenes. Molecular modelling suggested that both calixarenes interact with the herbicide through cation-? interaction. P Q in included in the p-tert butylcalix a rene cavity, a situation favoured by its pinched conformation in polar solvent while it is partially included in the p-tert butylcalix a rene cavity because of its in-out cone conformation. The theoretical results, in particular using Mopac ...

41

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

UK PubMed Central (United Kingdom)

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

42

Leptin receptor gene expression and number in the brain are regulated by leptin level and nutritional status  

UK PubMed Central (United Kingdom)

Hormone potency depends on receptor availability, regulated via gene expression and receptor trafficking. To ascertain how central leptin receptors are regulated, the effects of leptin challenge, high-fat...Full Text Available

2009-07-15

43

Intracellular delivery of an antisense?oligonucleotide via endocytosis of a G protein-coupled receptor  

UK PubMed Central (United Kingdom)

Gastrin-releasing peptide receptor (GRPR), a member of the G protein-coupled receptor superfamily, has been utilized for receptor-mediated targeting of imaging and therapeutic agents; here we extend...Full Text Available

2010-10-01

45

Agonist-dependent up-regulation of thyrotrophin-releasing hormone receptor protein.  

UK PubMed Central (United Kingdom)

To study the effect of agonist on the TRH (thyrotrophin-releasing hormone) receptor protein, an epitope-tagged receptor was stably expressed in HEK-293 cells (human embryonic kidney 293 cells) and receptor...Full Text Available

2004-06-15

47

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

Science.gov (United States)

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 Fst288 or Fst315. Overall, we have identified ...

2009-09-29

48

Presentation of Type B Peptide-MHC Complexes from Hen Egg White Lysozyme by TLR Ligands and Type I IFNs Independent of H2-DM Regulation.  

Science.gov (United States)

In APCs, presentation by MHC II molecules of the chemically dominant peptide from the protein hen egg white lysozyme (HEL) generates different conformational isomers of the peptide-MHC II complexes (pMHC). Type B pMHCs are formed in early endosomes from exogenous peptides in the absence of H2-DM, whereas in contrast, type A pMHC complexes are formed from HEL protein in late vesicles after editing by H2-DM. Thus, H2-DM edits off the more unstable pMHC complexes, which are not presented from HEL. In this study, we show that type B pMHC complexes were presented from HEL protein only after stimulation of dendritic cells (DC) with TLR ligands or type I IFN. Type I IFN contributed to most TLR ligand-induced type B pMHC generation, as presentation decreased in DC lacking the receptor for type I IFNs (IFNAR1(-/-)). In contrast, presentation of type A pMHC from HEL and from peptide was ...

2011-07-25

49

Biokinetic and dosimetric studies of {sup 188}Re-hyaluronic acid: a new radiopharmaceutical for treatment of hepatocellular carcinoma  

Energy Technology Data Exchange (ETDEWEB)

Hepatocellular carcinoma (HCC) is the most common primary liver cancer and has very limited therapeutic options. Recently, it has been found that hyaluronic acid (HA) shows selective binding to CD44 receptors expressed in most cancer histotypes. Since the trend in cancer treatment is the use of targeted radionuclide therapy, the aim of this research was to label HA with rhenium-188 and to evaluate its potential use as a hepatocarcinoma therapeutic radiopharmaceutical. Methods: {sup 188}Re-HA was prepared by a direct labelling method to produce a ReO(O-COO){sub 2}-type coordination complex. {sup 188}Re-HA protein binding and its stability in saline, phosphate buffer, human serum and cysteine solutions were determined. Biokinetic and dosimetric data were estimated in healthy mice (n=60) using the Medical Internal Radiation Dose methodology and mouse model beta-absorbed fractions. To evaluate liver toxicity, alanine aminotranferase (AST) and ...

2009-08-15

50

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

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

51

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

International Nuclear Information System (INIS)

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 ...

2006-03-24

52

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  

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

53

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

International Nuclear Information System (INIS)

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

54

In vivo and in vitro evaluation of dota-lanreotide radiolabelled with gallium-67  

International Nuclear Information System (INIS)

One of the refinements of modern Nuclear Medicine is the capacity of providing dynamic and kinetics images of the administered radiopharmaceutical, reproducing its transport mechanism, action sites, receptor binding and excretion route. With the continues technological advances new radiopharmaceuticals have been developed in order to express higher specificity and with higher characters of affinity between receptor/complex. One radiopharmaceutical is formed by a reagent or bio molecule that has in its structure a radioisotope, that has the objectives of carrying it to the organs of affinity or to benign or malign tumoral process. Somatostatin inhibits the growing and proliferation of several tumoral cells. Somatostatin analogs bind to somatostatic receptors that are expressed in different kind of neoplasia DOTA-LANREOTIDE (DOTALAN) is an octapeptide analog to somatostatin. The interest of labeling the bio conjugate with ...

55

Modulation of Retinoic Acid Receptor-related Orphan Receptor ? and ? Activity by 7-Oxygenated Sterol Ligands*  

UK PubMed Central (United Kingdom)

The retinoic acid receptor-related orphan receptors α and γ (RORα (NR1F1) and RORγ (NR1F3)) are orphan nuclear receptors and perform critical roles in regulation of development,...Full Text Available

2010-02-12

56

Gastrin releasing peptide (GRP) receptor targeted radiopharmaceuticals: A concise update  

Energy Technology Data Exchange (ETDEWEB)

The gastrin releasing peptide (GRP) receptor is becoming an increasingly attractive target for development of new radiolabeled peptides with diagnostic and therapeutic potential. The attractiveness of the GRP receptor as a target is based upon the functional expression of GRP receptors in several tumors of neuroendocrine origin including prostate, breast, and small cell lung cancer. This concise review outlines some of the efforts currently underway to develop new GRP receptor specific radiopharmaceuticals by employing a variety of radiometal chelation systems.

2003-11-01

57

Structural Insights into the Interaction of the Evolutionarily Conserved ZPR1 Domain Tandem with Eukaryotic EF1A, Receptors, and SMN Complexes  

Energy Technology Data Exchange (ETDEWEB)

Eukaryotic genomes encode a zinc finger protein (ZPR1) with tandem ZPR1 domains. In response to growth stimuli, ZPR1 assembles into complexes with eukaryotic translation elongation factor 1A (eEF1A) and the survival motor neurons protein. To gain insight into the structural mechanisms underlying the essential function of ZPR1 in diverse organisms, we determined the crystal structure of a ZPR1 domain tandem and characterized the interaction with eEF1A. The ZPR1 domain consists of an elongation initiation factor 2-like zinc finger and a double-stranded {beta} helix with a helical hairpin insertion. ZPR1 binds preferentially to GDP-bound eEF1A but does not directly influence the kinetics of nucleotide exchange or GTP hydrolysis. However, ZPR1 efficiently displaces the exchange factor eEF1B from preformed nucleotide-free complexes, suggesting that it may function as a negative regulator of eEF1A activation. Structure-based mutational and ...

2007-01-01

58

The Pregnane X Receptor: From Bench to Bedside  

UK PubMed Central (United Kingdom)

BackgroundThe pregnane X receptor (PXR; NR1I2), a member of the nuclear receptor superfamily, regulates the expression of metabolic enzymes and transporters involved...Full Text Available

2008-07-01

59

Surface structure recognized for covalent modification of the aspartate receptor in chemotaxis.  

UK PubMed Central (United Kingdom)

The aspartate receptor involved in chemotaxis is modified by methyl esterification at four distinct glutamate residues during the adaptive response of this receptor. To explain the high degree of specificity...Full Text Available

1986-09-01

60

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

UK PubMed Central (United Kingdom)

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

61

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

UK PubMed Central (United Kingdom)

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

62

Lineage-specific co-evolution of the Egf receptor/ligand signaling system  

UK PubMed Central (United Kingdom)

BackgroundThe epidermal growth factor receptor (Egfr) with its numerous ligands has fundamental roles in development, cell differentiation and physiology. Dysfunction of the receptor-ligand...Full Text Available

63

Involvement of the chemokine-like receptor GPR33 in innate immunity?  

UK PubMed Central (United Kingdom)

Chemokine receptors control leukocyte chemotaxis and cell-cell communication but have also been associated with pathogen entry. GPR33, an orphan member of the chemokine-like receptor family,...Full Text Available

2010-05-28

64

Influence of atrial stretch receptors on hypothalamic neurosecretory neurones.  

UK PubMed Central (United Kingdom)

1. The effects of stimulation of atrial receptors on hypothalamic neurosecretory cells were investigated in anaesthetized dogs and cats. Atrial receptors were activated by stretching the left and the...Full Text Available

1978-12-01

65

In vitro selection of RNA molecules that displace cocaine from the membrane-bound nicotinic acetylcholine receptor  

UK PubMed Central (United Kingdom)

The nicotinic acetylcholine receptor (AChR) controls signal transmission between cells in the nervous system. Abused drugs such as cocaine inhibit this receptor. Transient kinetic investigations indicate...Full Text Available

1998-11-24

66

Immunoglobulins in myasthenia gravis. Kinetic properties of the acetylcholine-receptor antibody studied during lymph drainage.  

UK PubMed Central (United Kingdom)

A specific immunoglobulin, the receptor antibody, can be found in most patients with myasthenia gravis. In order to study the kinetic properties of this antibody, serial determinations of receptor antibody,...Full Text Available

1978-10-01

67

Hormone Receptor Status in Breast Cancer and its Relation to Age and Other Prognostic Factors  

UK PubMed Central (United Kingdom)

Background:Increasing evidence shows the importance of young age, estrogen receptor (ER), progesterone receptor (PR) status, and HER-2 expression in patients with breast cancers.Patients...Full Text Available

68

Continuous monitoring of receptor-mediated changes in the metabolic rates of living cells.  

UK PubMed Central (United Kingdom)

Activation of beta-adrenergic or muscarinic acetylcholine receptors expressed in transfected cells or epidermal growth factor receptors in human keratinocytes produces 15% to 200% changes in cellular...Full Text Available

1990-05-01

69

Construction of a novel bifunctional biogenic amine receptor by two point mutations of the H2-histamine receptor.  

UK PubMed Central (United Kingdom)

BACKGROUND: H2-histamine receptors mediate a wide range of physiological functions extending from stimulation of gastric acid secretion to induction of human promyelocyte differentiation. We have previously...Full Text Available

1995-03-01

70

Changes in Androgen Receptor, Estrogen Receptor alpha, and Sexual Behavior with Aging and Testosterone in Male Rats1  

UK PubMed Central (United Kingdom)

Reproductive aging in males is characterized by a diminution in sexual behavior beginning in middle age. We investigated the relationships among testosterone, androgen receptor (AR) and estrogen...Full Text Available

2010-07-01

71

A Hot New Twist to Hair Biology  

UK PubMed Central (United Kingdom)

The vanilloid receptor-1 (VR1, or transient receptor potential vanilloid-1 receptor, TRPV1) is activated by capsaicin, the key ingredient of hot peppers. TRPV1 was originally described on sensory neurons...Full Text Available

2005-04-01

72

Rapidly adapting receptors in a rabbit model of mitral regurgitation  

UK PubMed Central (United Kingdom)

Unlike in normal rabbits, pulmonary rapidly adapting receptors (RARs) in rabbits with chronic mitral regurgitation (MR) do not respond to small changes in extravascular...Full Text Available

1999-12-15

73

New Developments in the Use of Histamine and Histamine Receptors  

UK PubMed Central (United Kingdom)

Histamine and the histamine receptors are important regulators of a plethora of biological processes, including immediate hypersensitivity reactions and acid secretion in the stomach. In these...Full Text Available

2011-04-01

74

Anesthetic stimulation of insect water receptors.  

UK PubMed Central (United Kingdom)

Halothane, chloroform, and carbon tetrachloride, in the vapor and liquid phases, stimulate the water receptor of the blowfly Phormia regina. There are three successive phases of response to long-lasting...Full Text Available

1976-09-01

75

Tissue structure, nuclear organization and gene expression in normal and malignant breast  

Energy Technology Data Exchange (ETDEWEB)

Because every cell within the body has the same genetic information, a significant problem in biology is to understand how cells within a tissue express genes selectively. A sophisticated network of physical and biochemical signals converge in a highly orchestrated manner to bring about the exquisite regulation that governs gene expression in diverse tissues. Thus, the ultimate decision of a cell to proliferate, express tissue-specific genes, or apoptose must be a coordinated response to its adhesive, growth factor, and hormonal milieu. The unifying hypothesis examined in this overview is that the unit of function in higher organisms is neither the genome nor the cell alone but the complex, three-dimensional tissue. This is because there are bidirectional connections between the components of the cellular microenvironment (growth factors, hormones, and extracellular matrix) and the nucl2048 These connections are made via membrane-bound ...

2000-01-27

79

Role of B2 Adrenergic Receptors in Labor Pain  

Science.gov (United States)

Pain; Pain Threshold; Labour Pain

2010-10-01

83

Effects of single or combined histamine H1-receptor and leukotriene CysLT1-receptor antagonism on nasal adenosine monophosphate challenge in persistent allergic rhinitis  

UK PubMed Central (United Kingdom)

BackgroundThe effects of single or combined histamine H1-receptor and leukotriene CysLT1-receptor antagonism on nasal adenosine monophosphate (AMP) challenge...Full Text Available

2004-06-01

84

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

UK PubMed Central (United Kingdom)

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

85

Magnetic resonance imaging of cerebral anomalies in subjects with resistance to thyroid hormone  

Energy Technology Data Exchange (ETDEWEB)

Resistance to thyroid hormone (RTH) is an autosomal dominant disease caused by mutations in the human thyroid receptor beta gene on chromosome 3. Individuals with RTH have an increased incidence of attention deficit hyperactivity disorder (ADHD). The purpose of this study was to search for developmental brain malformations associated with RTH. Forty-three subjects (20 affected males [AM], 23 affected females [AF]) with resistance to thyroid hormone and 32 unaffected first degree relatives (18 unaffected males [UM], 14 unaffected females [UF]) underwent MRI brain scans with a volumetric acquisition that provided 90 contiguous 2 mm thick sagittal images. Films of six contiguous images beginning at a standard sagittal position lateral to the insula were analyzed by an investigator who was blind with respect to subject characteristics. The presence of extra or missing gyri in the parietal bank of the Sylvian fissure (multimodal association cortex) and multiple Heschl`s ...

1995-06-19

86

Gene Repressive Activity of RIP140 Through Direct Interaction with CDK8.  

Science.gov (United States)

Receptor interacting protein 140 (RIP140) is a coregulator for numerous nuclear receptors and transcription factors and primarily exerts gene-repressive activities on various target genes. We previously identified a spectrum of posttranslational modifications on RIP140 that augment its property and biological activity. In T(3)-triggered biphasic regulation of cellular retinoic acid binding protein 1 (Crabp1) gene along the course of fibroblast-adipocyte differentiation, we found TRAP220(MED1) critical for T(3)-activated chromatin remodeling whereas RIP140 essential for T(3)-repressive chromatin remodeling of this gene promoter. In this current study, we aim to examine whether and how RIP140 replaces TRAP220(MED1) on the CrabpI promoter in differentiating adipocyte cultures. We find increasing recruitment of RIP140 to this promoter, with corresponding reduction in TRAP220(MED1) recruitment during the T(3)-repressive phase. We also uncover direct ...

2011-08-25

87

Limitation of immunohistochemical localization of estrogen receptor  

Energy Technology Data Exchange (ETDEWEB)

Although the radioreceptor method is widely used for estrogen receptor assay in human tissue, it has several limitations and a number of alternative methods are being explored. An immunohistochemical method of estrogen receptor assay using a specific antibody to estradiol has been proposed as a suitable alternative. The present study was designed to evaluate the validity of this method in detecting true estrogen receptors in human tumor tissue. Using radioiodinated antibody to estrogen, we have demonstrated that the estrogen antibody can detect the estrogen when it is bound to 4S type receptor but is unable to bind to estrogen when the hormone is bound to 8S type receptor. Our observations suggest that the immunohistochemical method of detection of intracellular cytosolic receptor for estrogen is not a suitable alternative to the currently used radioreceptor ...

1986-10-01

88

Study of epileptiform activity in cerebral ganglion of mud crab Scylla serrata  

British Library Electronic Table of Contents (United Kingdom)

An attempt is made to induce in mud crab (Scylla serrata) epileptiform activities that resemble the generalized epileptic seizures. Cerebral ganglion of crab was exposed in situ, to a convulsant drug pentylenetetrazole (PTZ) 100?mM, for induction of seizures. Also, crabs were pretreated with antiepileptic drug viz sodium valproate (120??mol/l) to inhibit epileptiform activities. The surface electrical discharges of cerebral ganglion were recorded using Unkelscope (MIT, USA) in control as well as experimental animals. The cerebral ganglion of crab showed a pattern of high cerebral electrical discharges after PTZ treatment compared to control. The sodium valproate promoted sedative action in control and prevented PTZ-mediated epileptiform discharges. Glutamate and GABA contents in cerebral g...

2011-01-01

89

Cloning and expression of a human kidney cDNA for an /alpha//sub 2/-adrenergic receptor subtype  

Energy Technology Data Exchange (ETDEWEB)

An /alpha//sub 2/-adrenergic receptor subtype has been cloned from a human kidney cDNA library using the gene for the human platelet /alpha//sub 2/-adrenergic receptor as a probe. The deduced amino acid sequence resembles the human platelet /alpha//sub 2/-adrenergic receptor and is consistent with the structure of other members of he family of guanine nucleotide-binding protein-coupled receptors. The cDNA was expressed in a mammalian cell line (COS-7), and the /alpha//sub 2/-adrenergic ligand (/sup 3/H)rauwolscine was bound. Competition curve analysis with a variety of adrenergic ligands suggests that this cDNA clone represents the /alpha//sub 2/B-adrenergic receptor. The gene for this receptor is on human chromosome 4, whereas the gene for the human platelet /alpha//sub 2/-adrenergic receptor (/alpha//sub 2/A) lies on chromosome 10. This ...

1988-09-01

90

GABAB Receptors Modulate NMDA Receptor Calcium Signals in Dendritic Spines  

British Library Electronic Table of Contents (United Kingdom)

Summary Metabotropic GABAB receptors play a fundamental role in modulating the excitability of neurons and circuits throughout the brain. These receptors influence synaptic transmission by inhibiting presynaptic release or activating postsynaptic potassium channels. However, their ability to directly influence different types of postsynaptic glutamate receptors remains unresolved. Here we examine GABAB receptor modulation in layer 2/3 pyramidal neurons from the mouse prefrontal cortex. We use two-photon laser-scanning microscopy to study synaptic modulation at individual dendritic spines. Using two-photon optical quantal analysis, we first demonstrate robust presynaptic modulation of multivesicular release at single synapses. Using two-photon glutamate uncaging, we then reveal that GABAB r...

2010-01-01

91

Cloning of the cDNA and gene for a human D sub 2 dopamine receptor  

Energy Technology Data Exchange (ETDEWEB)

A clone encoding a human D{sub 2} dopamine receptor was isolated from a pituitary cDNA library and sequenced. The deduced protein sequence is 96% identical with that of the cloned rat receptor with one major difference: the human receptor contains an additional 29 amino acids in its putative third cytoplasmic loop. Southern blotting demonstrated the presence of only one human D{sub 2} receptor gene. Two overlapping phage containing the gene were isolated and characterized. DNA sequence analysis of these clones showed that the coding sequence is interrupted by six introns and that the additional amino acids present in the human pituitary receptor are encoded by a single exon of 87 base pairs. The involvement of this sequence in alternative splicing and its biological significance are discussed.

1989-12-01

92

Platelet fibrinogen binding in Basset Hound Hereditary Thrombopathy  

Energy Technology Data Exchange (ETDEWEB)

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 +/- 3971 molecules of ...

1986-03-01

93

Azathia crown ethers carrying pyrene pendant as receptor molecules for metal sensor systems  

International Nuclear Information System (INIS)

A series of crown ethers carrying a pyrene group with nitrogen-sulfur donor atoms, that differ in having three, four and five sulfur atoms in the macrocycle was designed and synthesized by the reaction of the corresponding macrocyclic compound and 1-bromomethylpyrene. The influence of metal cations such as Mn2+, Fe2+, Fe3+, Co2+, Ni2+, Cu2+, Zn2+, Cd2+, Hg2+, Pb2+ and Al3+ on the spectroscopic properties of the ligands was investigated in acetonitrile-dichloromethane (1:1) by means of absorption and emission spectrometry. Absorption spectra show isosbestic points in the spectrophotometric titration of Fe2+, Zn2+, Cu2+, Pb2+ and Hg2+. The results of spectrophotometric titration experiments disclosed the complexation compositions and complex stability constants of the novel ligands with Fe2+, Zn2+, Cu2+, Pb2+ and Hg2+ cations. The monoazatetrathia crown ether showed good sensitivity for Cu2+ with linearity in the range 5.0x10-7-2.5x10-6 M and ...

2011-04-01

94

p53 mutation in breast cancer. Correlation with cell kinetics and cell of origin  

UK PubMed Central (United Kingdom)

Aim: Several studies have investigated the expression of the cytokeratins (CKs), vimentin, the epithelial growth factor receptor (EGFR), the oestrogen receptor (ER), and the progesterone...Full Text Available

2002-06-01

95

The Melanocortin 3 Receptor: A Novel Mediator of Exercise-Induced Inflammation Reduction in Postmenopausal Women?  

UK PubMed Central (United Kingdom)

The purpose of this study was to determine whether resistance exercise training-induced reductions in inflammation are mediated via melanocortin 3 receptor expression in obese (BMI 32.7 ± 3.7)...Full Text Available

96

The Cytokinin Receptors of Arabidopsis Are Located Mainly to the Endoplasmic Reticulum1[W][OA]  

UK PubMed Central (United Kingdom)

The plant hormone cytokinin is perceived by membrane-located sensor histidine kinases. Arabidopsis (Arabidopsis thaliana) possesses three cytokinin receptors: ARABIDOPSIS HISTIDINE...Full Text Available

2011-08-01

97

The Anti-Inflammatory Drug Leflunomide Is an Agonist of the Aryl Hydrocarbon Receptor  

UK PubMed Central (United Kingdom)

BackgroundThe aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor that mediates the toxicity and biological activity of dioxins and related chemicals. The...Full Text Available

98

T cell-engaging BiTE antibodies specific for EGFR potently eliminate KRAS- and BRAF-mutated colorectal cancer cells  

UK PubMed Central (United Kingdom)

Epidermal growth factor receptor (EGFR)-specific monoclonal antibodies predominantly inhibit colorectal cancer (CRC) growth by interfering with receptor signaling. Recent analyses have shown that patients...Full Text Available

2010-07-13

99

Structure of Natural Killer Cell Receptor KLRG1 Bound to E-Cadherin Reveals Basis for MHC-Independent Missing Self Recognition  

UK PubMed Central (United Kingdom)

SUMMARYThe cytolytic activity of natural killer (NK) cells is regulated by inhibitory receptors that detect the absence of self molecules on target cells. Structural studies of...Full Text Available

2009-07-17

100

Spontaneous expression of the interleukin 2 receptor gene and presence of functional interleukin 2 receptors on T lymphocytes in the blood of individuals with active pulmonary sarcoidosis.  

UK PubMed Central (United Kingdom)

Current concepts of the pathogenesis of sarcoidosis suggest that the expanded numbers of activated T-helper/inducer cells at sites of disease activity result, at least in part, from their proliferation...Full Text Available

1988-09-01

101

Sodium/Calcium Exchangers Selectively Regulate Calcium Signaling in Mouse Taste Receptor Cells  

UK PubMed Central (United Kingdom)

Taste cells use multiple signaling mechanisms to generate appropriate cellular responses to discrete taste stimuli. Some taste stimuli activate G protein coupled receptors (GPCRs) that cause calcium...Full Text Available

2010-07-01

102

Signal transduction underlying the control of urinary bladder smooth muscle tone by muscarinic receptors and ?-adrenoceptors  

UK PubMed Central (United Kingdom)

The normal physiological contraction of the urinary bladder, which is required for voiding, is predominantly mediated by muscarinic receptors, primarily the M3 subtype, with the M2...Full Text Available

2008-06-01

103

Sensitivity limits for voltage control of P2Y receptor-evoked Ca2+ mobilization in the rat megakaryocyte  

UK PubMed Central (United Kingdom)

G-protein-coupled receptor signalling has been suggested to be voltage dependent in a number of cell types; however, the limits of sensitivity of this potentially important phenomenon are unknown. Using...Full Text Available

2004-02-15

104

Retinoic acid X receptor in the diploblast, Tripedalia cystophora  

UK PubMed Central (United Kingdom)

Nuclear hormone receptors comprise a characteristic family of transcription factors found in vertebrates, insects and nematodes. Here we show by cDNA and gene cloning that a Cnidarian, Tripedalia...Full Text Available

1998-11-10

105

Replication of Extended Lifespan Phenotype in Mice with Deletion of Insulin Receptor Substrate 1  

UK PubMed Central (United Kingdom)

We previously reported that global deletion of insulin receptor substrate protein 1 (Irs1) extends lifespan and increases resistance to several age-related pathologies in female mice....Full Text Available

106

Relative potencies for barbiturate binding to the Torpedo acetylcholine receptor.  

UK PubMed Central (United Kingdom)

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

107

Regulation of rat hepatic low density lipoprotein receptors. In vivo stimulation by growth hormone is not mediated by insulin-like growth factor I.  

UK PubMed Central (United Kingdom)

Growth hormone (GH) has an important role in the regulation of hepatic LDL receptor expression and plasma lipoprotein levels. This investigation was undertaken to evaluate if these effects of GH on...Full Text Available

1996-01-15

108

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

UK PubMed Central (United Kingdom)

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

109

Receptor mechanisms and dose-response models for the effects of dioxins.  

UK PubMed Central (United Kingdom)

There is increasing evidence that receptor-mediated events impact one or more stages responsible for tumor development in experimental animals and humans. Although many chemicals and endogenous hormones...Full Text Available

1993-04-22

110

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

UK PubMed Central (United Kingdom)

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

111

Rapid detection of epidermal growth factor receptor mutations with multiplex PCR and primer extension in lung cancer  

UK PubMed Central (United Kingdom)

Epidermal growth factor receptor (EGFR) kinase domain mutations hyperactivate the kinase and confer kinase addiction of the non-small-cell lung cancer (NSCLC) tumor...Full Text Available

112

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

UK PubMed Central (United Kingdom)

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

113

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

UK PubMed Central (United Kingdom)

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

114

Predictive and prognostic markers for epidermal growth factor receptor inhibitor therapy in non-small cell lung cancer  

UK PubMed Central (United Kingdom)

Epidermal growth factor receptor (EGFR) related therapies – mainly tyrosine kinase inhibitors (TKIs) such as erlotinib and gefitinib, but also monoclonal antibodies targeting EGFR, for example,...Full Text Available

2009-11-01

115

Polymorphisms in the epidermal growth factor receptor gene and the risk of primary lung cancer: a case-control study  

UK PubMed Central (United Kingdom)

BackgroundPolymorphisms in Epidermal Growth Factor Receptor (EGFR) gene may influence EGFR production and/or activity, thereby modulating susceptibility to lung...Full Text Available

116

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

UK PubMed Central (United Kingdom)

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

117

Neurotensin Receptor 1 Is Expressed in Gastrointestinal Stromal Tumors but Not in Interstitial Cells of Cajal  

UK PubMed Central (United Kingdom)

Gastrointestinal stromal tumors (GIST) are thought to derive from the interstitial cells of Cajal (ICC) or an ICC precursor. Oncogenic mutations of the KIT or PDGFRA receptor tyrosine kinases are present...Full Text Available

118

Multiple Functions of the 37/67-kd Laminin Receptor Make It a Suitable Target for Novel Cancer Gene Therapy  

UK PubMed Central (United Kingdom)

The 37/67-kd laminin receptor, LAMR, is a multifunctional protein that associates with the 40S ribosomal subunit and also localizes to the cell membrane to interact with the extracellular matrix. LAMR...Full Text Available

2010-01-01

119

Lack of LDL Receptor Enhances Amyloid Deposition and Decreases Glial Response in an Alzheimer's Disease Mouse Model  

UK PubMed Central (United Kingdom)

BackgroundApolipoprotein E (ApoE), a cholesterol carrier associated with atherosclerosis, is a major risk factor for Alzheimer's disease (AD). The low-density lipoprotein receptor...Full Text Available

120

Isolation and partial characterization of a specific alpha-fetoprotein receptor on human monocytes.  

UK PubMed Central (United Kingdom)

Since a large body of data has suggested a significant role for alpha-fetoprotein (AFP) in the regulation of the immune response at a number of levels, we examined the possibility of a specific receptor...Full Text Available

1992-10-01

121

Insulin-Like Growth Factor I Receptor Signaling Is Required for Exercise-Induced Cardiac Hypertrophy  

UK PubMed Central (United Kingdom)

The receptors for IGF-I (IGF-IR) and insulin (IR) have been implicated in physiological cardiac growth, but it is unknown whether IGF-IR or IR signaling are critically required. We generated mice with...Full Text Available

2008-11-01

122

Induction of Oxidative Stress Responses by Dioxin and other Ligands of the Aryl Hydrocarbon Receptor  

UK PubMed Central (United Kingdom)

TCDD and other polyhalogenated aromatic hydrocarbon ligands of the aryl hydrocarbon receptor (AHR) have been classically considered as non-genotoxic compounds because they fail to be directly mutagenic...Full Text Available

123

Identification of LRRc17 as a Negative Regulator of Receptor Activator of NF-?B Ligand (RANKL)-induced Osteoclast Differentiation*S?  

UK PubMed Central (United Kingdom)

Osteoblasts are the primary cells responsible for bone formation. They also support osteoclast formation from bone marrow precursors in response to osteotropic factors by inducing receptor activator...Full Text Available

2009-05-29

124

Functional Analysis of the Murine Cytomegalovirus Chemokine Receptor Homologue M33: Ablation of Constitutive Signaling Is Associated with an Attenuated Phenotype In Vivo?  

UK PubMed Central (United Kingdom)

The murine cytomegalovirus (MCMV) M33 gene is conserved among all betaherpesviruses and encodes a homologue of seven-transmembrane receptors (7TMR) with the capacity for constitutive signaling. Previous...Full Text Available

2008-02-01

125

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

UK PubMed Central (United Kingdom)

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

126

Evidence for an association between TSH and IGF-1 receptors  

UK PubMed Central (United Kingdom)

TSH receptor (TSHR) plays a central role in regulating thyroid function and is targeted by IgGs in Graves’ disease (GD-IgG). Whether TSHR is involved in the pathogenesis of thyroid associated...Full Text Available

2008-09-15

127

Effects of metabotropic glutamate receptor 2/3 agonism and antagonism on schizophrenia-like cognitive deficits induced by phencyclidine in rats  

UK PubMed Central (United Kingdom)

Dysregulation of glutamate neurotransmission may play a role in cognitive deficits in schizophrenia. Manipulation of glutamate signaling using drugs acting at metabotropic glutamate receptors...Full Text Available

2010-08-10

128

Development of a Selective Modulator of Aryl Hydrocarbon (Ah) Receptor Activity that Exhibits Anti-Inflammatory Properties  

UK PubMed Central (United Kingdom)

The aryl hydrocarbon receptor (AHR) is a ligand-activated transcription factor that mediates the toxicity of 2,3,7,8-tetrachlorodibenzo-p-dioxin. However, the role of the AHR...Full Text Available

2010-05-17

129

Deletion of the Receptor for Advanced Glycation End Products Reduces Glomerulosclerosis and Preserves Renal Function in the Diabetic OVE26 Mouse  

UK PubMed Central (United Kingdom)

OBJECTIVEPrevious studies showed that genetic deletion or pharmacological blockade of the receptor for advanced glycation end products (RAGE) prevents the early structural changes...Full Text Available

2010-08-01

130

Cloning of the mouse hepatitis virus (MHV) receptor: expression in human and hamster cell lines confers susceptibility to MHV.  

UK PubMed Central (United Kingdom)

The cellular receptor for murine coronavirus mouse hepatitis virus (MHV)-A59 is a member of the carcinoembryonic antigen (CEA) family of glycoproteins in the immunoglobulin superfamily. We isolated...Full Text Available

1991-12-01

131

Characterisation of the Expression of NMDA Receptors in Human Astrocytes  

UK PubMed Central (United Kingdom)

Astrocytes have long been perceived only as structural and supporting cells within the central nervous system (CNS). However, the discovery that these glial cells may potentially express receptors capable...Full Text Available

132

Biochemical characterization of the molecular interaction between recombinant basic fibroblast growth factor and a recombinant soluble fibroblast growth factor receptor.  

UK PubMed Central (United Kingdom)

The extracellular domain of human fibroblast growth factor receptor (XC-FGF-R) was expressed in Escherichia coli. The protein was purified to homogeneity and the interaction with basic fibroblast growth...Full Text Available

1993-09-15

133

Attenuation of Cocaine's Reinforcing and Discriminative Stimulus Effects via Muscarinic M1 Acetylcholine Receptor StimulationS?  

UK PubMed Central (United Kingdom)

Muscarinic cholinergic receptors modulate dopaminergic function in brain pathways thought to mediate cocaine's abuse-related effects. Here, we sought to confirm and ...Full Text Available

2010-01-01

134

Association Analysis of Nuclear Receptor Rev-erb Alpha Gene (NR1D1) and Japanese Methamphetamine Dependence  

UK PubMed Central (United Kingdom)

Several investigations suggested abnormalities in circadian rhythms are related to the pathophysiology of psychiatric disorders, including drug addiction. Recently, orphan nuclear receptor rev-erb alpha...Full Text Available

2011-03-01

135

Antigenic analysis of the second extra-cellular loop of the human beta-adrenergic receptors.  

UK PubMed Central (United Kingdom)

Polyclonal antibodies were raised in rabbits by immunization with free peptides corresponding to positions 197-222 of the human beta 1-adrenergic receptor (beta 1 peptide) and the corresponding sequence...Full Text Available

1989-10-01

136

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

UK PubMed Central (United Kingdom)

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

137

An analysis by low-angle neutron scattering of the structure of the acetylcholine receptor from Torpedo californica in detergent solution.  

UK PubMed Central (United Kingdom)

The acetylcholine receptor from the electric tissue of Torpedo californica is a large, integral membrane protein containing four different types of polypeptide chains. The structure of the purified...Full Text Available

1979-12-01

138

Activated PPAR? Targets Surface and Intracellular Signals That Inhibit the Proliferation of Lung Carcinoma Cells  

UK PubMed Central (United Kingdom)

Peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors belonging to the nuclear hormone receptor superfamily. Their discovery in the 1990s provided insights...Full Text Available

2008-01-01

139

Acetylcholine receptor kinetics. A description from single-channel currents at snake neuromuscular junctions.  

UK PubMed Central (United Kingdom)

Single-channel currents from acetylcholine receptor channels of garter snake neuromuscular junctions were recorded using the patch-clamp technique. Low concentrations of acetylcholine or carbamylcholine...Full Text Available

1982-09-01

140

A multigene predictor of metastatic outcome in early stage hormone receptor-negative and triple-negative breast cancer  

UK PubMed Central (United Kingdom)

IntroductionVarious multigene predictors of breast cancer clinical outcome have been commercialized, but proved to be prognostic only for hormone receptor (HR) subsets overexpressing...Full Text Available

2010-01-01

141

A Randomized Clinical Trial Investigating the Relationship Between Aprotinin and Hypercoagulability in Off-Pump Coronary Surgery  

UK PubMed Central (United Kingdom)

BACKGROUNDOff-pump coronary artery bypass (OPCAB) surgery is associated with a hypercoagulable state in which the platelet thrombin receptor, protease-activated receptor-1...Full Text Available

2009-11-01

142

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

UK PubMed Central (United Kingdom)

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

144
145

Purinergic receptors are involved in tooth-pulp evoked nocifensive behavior and brainstem neuronal activity  

UK PubMed Central (United Kingdom)

BackgroundTo evaluate whether P2X receptors are involved in responses to noxious pulp stimulation, the P2X3 and P2X2/3 receptor agonist α,β-methyleneATP...Full Text Available

146

P2X1 receptor mobility and trafficking; regulation by receptor insertion and activation  

UK PubMed Central (United Kingdom)

P2X1 receptors for ATP contribute to signalling in a variety of cell types and following stimulation undergo rapid desensitisation (within 1 s), and require ∼5 min to recover. In HEK293 cells...Full Text Available

2010-06-01

147

Nuclear receptor co-repressor SMRT regulates mitochondrial oxidative metabolism and mediates aging related metabolic deterioration  

UK PubMed Central (United Kingdom)

SummaryThe transcriptional co-repressor SMRT utilizes two major receptor interacting domains (RID1 and RID2) to mediate nuclear receptor (NR) signaling through epigenetic modification....Full Text Available

2010-12-01

148

Mechano-transduction in Osteoblastic Cells Involves Strain-regulated Estrogen Receptor ?-mediated Control of Insulin-like Growth Factor (IGF) I Receptor Sensitivity to Ambient IGF, Leading to Phosphatidylinositol 3-Kinase/AKT-dependent Wnt/LRP5 Receptor-independent Activation of ?-Catenin Signaling*  

UK PubMed Central (United Kingdom)

The capacity of bones to adjust their mass and architecture to withstand the loads of everyday activity derives from the ability of their resident cells to respond appropriately to the strains engendered....Full Text Available

2010-03-19

149

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

UK PubMed Central (United Kingdom)

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

150

Forkhead Box Transcription Factor FOXO3a Regulates Estrogen Receptor Alpha Expression and Is Repressed by the Her-2/neu/Phosphatidylinositol 3-Kinase/Akt Signaling Pathway  

UK PubMed Central (United Kingdom)

The expression status of the estrogen receptor alpha (ERα) and that of the epidermal growth factor receptor Her-2/neu frequently correlate inversely in breast cancers. While ERα-dependent...Full Text Available

2004-10-01

151

Extraribosomal functions associated with the C terminus of the 37/67?kDa laminin receptor are required for maintaining cell viability  

UK PubMed Central (United Kingdom)

The 37/67 kDa laminin receptor (LAMR) is a multifunctional protein, acting as an extracellular receptor, localizing to the nucleus, and playing roles in rRNA processing and ribosome assembly....Full Text Available

2010-05-01

152

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

UK PubMed Central (United Kingdom)

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

153

Cloning and characterization of a 77-kDa oestrogen receptor isolated from a human breast cancer cell line.  

UK PubMed Central (United Kingdom)

We have cloned and characterized a 77-kDa oestrogen receptor (ER) from an oestrogen-independent subclone of the MCF-7 human breast cancer cell line. This receptor contains an in-frame, tandem duplication...Full Text Available

1997-01-01

154

Characterization of an oligopeptide chemoattractant receptor on human blood monocytes using a new radioligand  

Energy Technology Data Exchange (ETDEWEB)

The study of chemoattractant receptors on human monocytes had been limited by the lack of a radioligand suitable for use with the small numbers of cells routinely available from human donors. A new synthetic oligopeptide radioligand f(/sup 35/S)Met-leu-phe, with a higher specific radioactivity than was available with the tritiated compound, was used to characterize a chemoattractant receptor on freshly isolated human blood monocytes. These cells bind f(/sup 35/)met-leu-phe with a dissociation constant (KD) of 30.2 +/- 5.6 nM and contain 84,000 +/- 11,300 receptors per cell. f(/sup 35/)met-leu-phe does not bind specifically to blood lymphocytes. The specificity of the oligopeptide receptor on monocytes is indistinguishable from the oligopeptide chemoattractant receptor on human polymorphonuclear leukocytes. Using f(/sup 35/)met-leu-phe, it will now be feasible to study the ...

1984-03-01

155

Role of E-cadherin in the induction of apoptosis of HPV16-positive CaSki cervical cancer cells during multicellular tumor spheroid formation.  

Science.gov (United States)

Multicellular tumor spheroids (MCTS) are three dimensional cell culture systems induced by suspension culture. MCTS are widely used in cancer research because of their similarity to solid tumors. CaSki cells are derived from a metastatic cervical cancer containing human papillomavirus 16 (HPV16). Cell death of CaSki cells in MCTS has been previously reported, and our model is used to better characterize the mechanisms of cell death of HPV16-positive keratinocytes. In this study, we found that apoptosis of CaSki cells was induced by suspension culture along with the formation of MCTS after 24 h of incubation. In suspended CaSki cells, monoclonal antibodies blocking E-cadherin function inhibited MCTS formation and suppressed suspension-induced apoptosis in a dose-dependent manner. Western blot for E-cadherin detected upregulation of the authentic 120 kDa band from MCTS of CaSki cells as well as a shorter 100 kDa band. Addition of EGF, whose receptor is known to form ...

2008-01-01

156

Chelation of intracellular calcium blocks insulin action in the adipocyte  

Energy Technology Data Exchange (ETDEWEB)

The hypothesis that intracellular Ca/sup 2 +/ is an essential component of the intracellular mechanism of insulin action in the adipocyte was evaluated. Cells were loaded with the Ca/sup 2 +/ chelator quin-2, by preincubating them with quin-2 AM, the tetrakis(acetoxymethyl) ester of quin-2. Quin-2 loading inhibited insulin-stimulated glucose transport without affecting basal activity. The ability of insulin to stimulate glucose uptake in quin-2-loaded cells could be partially restored by preincubating cells with buffer supplemented with 1.2 mM CaCl/sub 2/ and the Ca/sup 2 +/ ionophore A23187. These conditions had no effect on basal activity and omission of CaCl/sub 2/ from the buffer prevented the restoration of insulin-stimulated glucose uptake by A23187. Quin-2 loading also inhibited insulin-stimulated glucose oxidation and the ability of insulin to inhibit cAMP-stimulated lipolysis without affecting their basal activities. Incubation of cells with 100 ..mu..M quin-2 or quin-2 AM had ...

1987-02-01

157

Chelation of intracellular calcium blocks insulin action in the adipocyte  

International Nuclear Information System (INIS)

The hypothesis that intracellular Ca"2"+ is an essential component of the intracellular mechanism of insulin action in the adipocyte was evaluated. Cells were loaded with the Ca"2"+ chelator quin-2, by preincubating them with quin-2 AM, the tetrakis(acetoxymethyl) ester of quin-2. Quin-2 loading inhibited insulin-stimulated glucose transport without affecting basal activity. The ability of insulin to stimulate glucose uptake in quin-2-loaded cells could be partially restored by preincubating cells with buffer supplemented with 1.2 mM CaCl_2 and the Ca"2"+ ionophore A23187. These conditions had no effect on basal activity and omission of CaCl_2 from the buffer prevented the restoration of insulin-stimulated glucose uptake by A23187. Quin-2 loading also inhibited insulin-stimulated glucose oxidation and the ability of insulin to inhibit cAMP-stimulated lipolysis without affecting their basal activities. Incubation of cells with 100 #mu#M quin-2 or quin-2 AM had no effect on intracellular ...

158

Insulin-like growth factor II receptor is phosphorylated by a tyrosine kinase in adipocyte plasma membranes  

Energy Technology Data Exchange (ETDEWEB)

Incorporation of /sup 32/P from (gamma-32P)ATP into tyrosine residues of the insulin-like growth factor (IGF)-II receptor was observed in a Triton X-100-insoluble fraction of rat adipocyte plasma membranes. IGF-II receptor phosphorylation proceeded to a stoichiometry of approximately 0.5 mol of phosphate/IGF-II binding site after 10 min of incubation at 4 degrees C. A Km for ATP of 6 microM was calculated for this phosphorylation reaction. Addition of IGF-II caused an approximately 2-fold increase in tyrosine phosphorylation of the IGF-II receptor in this preparation. In contrast, phosphorylation of angiotensin II by the Triton X-100 washed membranes was not stimulated by IGF-II. Incubation of purified receptor immobilized on IGF-II agarose or of receptor-enriched low density microsomal membranes with (gamma-32P)ATP did not result in appreciable incorporation of (/sup 32/P)phosphate ...

1986-06-15

159

Dissociation of insulin receptor phosphorylation and stimulation of glucose transport in BC3H-1 myocytes  

Energy Technology Data Exchange (ETDEWEB)

The authors have investigated insulin receptor phosphorylation in differentiated cultured BC3H-1 myocytes. As for other insulin-responsive cell systems in partially purified wheat germ agglutinin receptor preparations, insulin stimulates the phosphorylation of its own receptor (95K ..beta..-subunits) in a dose dependent manner (0-400 nM), as identified by immunoprecipitation with antiinsulin receptor antibodies and SDS-PAGE. In the same preparations they show that 12-0-tetradecanyl phorbol acetate (TPA), which in many respect ..beta..-subunits in the same dose dependent manner (0-5 ..mu..M). In addition, antiinsulin receptor antibodies (B-10) also induced phosphorylation of mimics insulin action, also induced phosphorylation of the insulin receptor and HPLC tryptic maps of the /sup 32/P-labeled ..beta..-subunit were identical to those for insulin-induced ...

1986-05-01

160

Formation and stability of astatide-mercury complexes  

International Nuclear Information System (INIS)

The formation of astatide-mercury complexes was investigated in aqueous solutions.The obtained complexes were examined by paper electrophoresis. It was found that Hg(OH)At and Hg(OH)I complexes were formed in neutral solution. The stability constants of the obtained complexes were determined by ion-exchange. The preliminary results indicate that the complex of mercury with astatide is much more stable than similar complexes with iodide. (author)

2006-04-01

161

The development of sigma-receptor specific radiopharmaceuticals for spect imaging of human tumors  

International Nuclear Information System (INIS)

The authors have been involved for the last few years in developing high affinity sigma-receptor-specific radiopharmaceuticals for use in nuclear medicine. They recently demonstrated that sigma-1 receptors are expressed in human melanoma cells and that sigma receptors could be used as external markers for non-invasive imaging. In order to determine the presence of sigma receptors in other human tumors they have screened numerous non-small cell lung carcinoma, melanoma and breast cancer cell lines. All of these cell lines expressed high sigma receptor densities using commercially available ["3H]-(+)-pentazocine or ["3H]DTG tritiated sigma ligands. Therefore, a sigma ligand with high affinity in both sigma-1 and sigma-2 subtype pharmacological assays could be potentially useful for imaging a variety of primary and metastatic sites of various origins. The authors describe recent ...

1994-08-21

162

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

Science.gov (United States)

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 ...

1986-01-01

163

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

Energy Technology Data Exchange (ETDEWEB)

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 ...

1986-05-01

164

Algebraic complexities and algebraic curves over finite fields  

UK PubMed Central (United Kingdom)

We consider the problem of minimal (multiplicative) complexity of polynomial multiplication and multiplication in finite extensions of fields. For infinite fields minimal complexities are known [Winograd,...Full Text Available

1987-04-01

167

The interaction of trazodone with rat brain muscarinic cholinoceptors.  

UK PubMed Central (United Kingdom)

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

168

The hepcidin-binding site on ferroportin is evolutionarily conserved  

UK PubMed Central (United Kingdom)

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

169

The androgen receptor governs the execution, but not programming, of male sexual and territorial behaviors  

UK PubMed Central (United Kingdom)

SUMMARYTestosterone and estrogen are essential for male behaviors in vertebrates. How these two signaling pathways interact to control masculinization of the brain and behavior...Full Text Available

2010-04-29

170

THE STIMULATING EFFECT OF GLYCOLS AND THEIR POLYMERS ON THE TARSAL RECEPTORS OF BLOWFLIES  

UK PubMed Central (United Kingdom)

The rejection thresholds of Phormia regina Meigen for twenty-four glycols have been determined. A definite relationship between the concentration of the test material and the distribution...Full Text Available

1948-11-20

171

Site-Specific Methylation of the Promoter Alters Deoxyribonucleic Acid-Protein Interactions and Prevents ...  

Science.gov (United States)

... and R. L. Momparler. DNA methylation of retinoic acid receptor beta in breast cancer and possible therapeutic role of ... ...

172

Role of the 5HT3 Receptor in Alcohol Drinking and ...  

Science.gov (United States)

... Proc Natl Acad Sci USA 97:11032-7 27. Duman RS 2002 Genetics of childhood disorders: XXXIX. Stem cell research, part 3: ...

2005-09-01

173

Role of Obesity in Prostate Cancer Development  

Science.gov (United States)

... estrogen receptor status. Cancer Lett., 253, 291-300. 39. Xin,X ... and resistant mice. Brain Res.Bull., 52, 235-242. 40. Foster,BA ...

2011-04-01

174

Purinergic receptors in the splanchnic circulation  

UK PubMed Central (United Kingdom)

There is considerable evidence that purines are vasoactive molecules involved in the regulation of blood flow. Adenosine is a well known vasodilator that also acts as a modulator of the response to...Full Text Available

2008-09-01

176

Molecular Aspects of Thyroid Hormone Actions  

UK PubMed Central (United Kingdom)

Cellular actions of thyroid hormone may be initiated within the cell nucleus, at the plasma membrane, in cytoplasm, and at the mitochondrion. Thyroid hormone nuclear receptors (TRs) mediate the biological...Full Text Available

2010-04-01

177

Missense mutations in the growth hormone receptor dimerization region in Laron syndrome  

Energy Technology Data Exchange (ETDEWEB)

Laron syndrome (LS) is an autosomal recessively inherited condition characterized by insensitivity to endogenous and exogenous GH. Affected individuals have severe episodes and other characteristic features. GH receptor gene mutations are present in all affected individuals in whom molecular studies have been reported. The GH receptor is a plasma membrane-spanning protein in which the extracellular domain binds circulating GH and the intracellular domain interacts with the JAK-2 kinase and possibly other intracellular signaling molecules. GH receptor dimerization occurs on GH binding and is thought to be required for normal signal transduction. We have studied the GH receptor genes of four unrelated individuals affected with LS from the United States, Italy, Saudi Arabia, and India. We have identified four different missense mutations that alter consecutive amino acids 152 to 155 in or near the ...

1994-09-01

178

Influence of KDEL on the Fate of Trimeric or Assembly-Defective Phaseolin  

UK PubMed Central (United Kingdom)

The tetrapeptide KDEL is commonly found at the C terminus of soluble proteins of the endoplasmic reticulum (ER), and it contributes to their localization by interacting with a receptor that recycles...Full Text Available

2001-05-01

179

Hypothyroidism Enhances Tumor Invasiveness and Metastasis Development  

UK PubMed Central (United Kingdom)

BackgroundWhereas there is increasing evidence that loss of expression and/or function of the thyroid hormone receptors (TRs) could result in a selective advantage for tumor development,...Full Text Available

180

Effect of propylbenzilylcholine mustard on contraction and radioligand binding parameters of muscarinic receptors in guinea pig ileum  

Energy Technology Data Exchange (ETDEWEB)

The receptor occupancy-biological effect relationship for muscarinic receptors in guinea pig ileal smooth muscle has been studied by comparison of radioligand binding and contractile response. Muscarinic receptors in homogenates of ileal smooth muscle were labeled with (/sub 3/H)-1-Quinuclidinyl benzilate. Treatment with propylbenzilylcholine mustard (PrBCM), to inactivate irreversibly muscarinic receptors, caused a large dose dependent rightward shift of the dose-response curve to three agonistic furtrethonium derivatives with a concomitant decrease in maximal response. Using those data, the fraction of receptors remaining unoccupied (q-values) and true affinity constants (-log K/sub A/-values) were calculated. Exposure to 20 or 60 nM PrBCM for 15 minutes resulted in a 39% and a 61% reduction in specific (/sup 3/H)-1-Quinuclidinyl benzilate binding sites respectively to be compared ...

1987-10-26

181

ERG Expression Levels in Prostate Tumors Reflect Functional ...  

Science.gov (United States)

... Title : ERG Expression Levels in Prostate Tumors Reflect Functional Status of the Androgen Receptor (AR) as a Consequence of Fusion of ERG ...

182

Characterization of lymphocyte receptors for glycosaminoglycans.  

UK PubMed Central (United Kingdom)

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

183

Cardioprotection conferred by exercise training is blunted by blockade of the opioid system  

UK PubMed Central (United Kingdom)

OBJECTIVES:To investigate the effect of opioid receptor blockade on the myocardial protection conferred by chronic exercise and to compare exercise training with different strategies...Full Text Available

2011-01-01

184

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

UK PubMed Central (United Kingdom)

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

185

Acetylcholine Receptor Binding Characteristics of Snake and ...  

Science.gov (United States)

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

2011-05-13

186

AN ELECTROPHYSIOLOGICAL ANALYSIS OF THE ACTION OF CARBOHYDRATES ON THE SUGAR RECEPTOR OF THE BLOWFLY*  

UK PubMed Central (United Kingdom)

Measurements of the taste thresholds of blowflies for a wide variety of carbohydrates, presented individually and in combination, showed that the stimulating effects of the compounds are not always...Full Text Available

1969-01-01

190

Complex fluid analysis with the advanced distillation curve approach.  

Science.gov (United States)

An improved method for measuring distillation curves reveals the physicochemical properties of complex fluids such as fuels. PMID:20041713

2010-02-01

191

Mechanism of zirconium complexing with biphenyl mono- and biscatecholylazo derivatives  

Energy Technology Data Exchange (ETDEWEB)

The complex formation of zirconium with biphenyl mono- and biscatecholyazo derivatives has been studied spectrophotometrically. The composition of the complexes, form and charge of complex-forming zirconium ions have been established. A procedure is suggested for calculation of molar absorptivities and stability constants for each of the complexes formed simultaneously in the system. Possible complex formation schemes have been studied. The data obtained were used to develop a spectrophotometric method of determining zirconium in the presence of large amounts of copper.

1982-05-01

192

Visualization of inositol 1,4,5-trisphosphate receptors on the nuclear envelope outer membrane by deep etching electron microscopy  

UK PubMed Central (United Kingdom)

SummaryThe receptors for the second messenger InsP3 comprise a family of closely related ion channels that release Ca2+ from intracellular stores, most prominently...Full Text Available

2010-09-01

193

The Expression Level of CB1 and CB2 Receptors Determines Their Efficacy at Inducing Apoptosis in Astrocytomas  

UK PubMed Central (United Kingdom)

BackgroundCannabinoids represent unique compounds for treating tumors, including astrocytomas. Whether CB1 and CB2 receptors mediate this therapeutic effect...Full Text Available

194

The C'-terminal interaction domain of the thyroid hormone receptor confers the ability of the DNA site to dictate positive or negative transcriptional activity  

Energy Technology Data Exchange (ETDEWEB)

To investigate mechanisms responsible for positive and negative transcriptional control, the authors have utilized two types of promoters that are diffferentially regulated by thyroid hormone (T{sub 3}) receptors. Promoters containing the palindromic T{sub 3} response element TCAGGTCA TGACCTGA are positively regulated by the T{sub 3} receptor after the administration of T{sub 3}, whereas otherwise identical promoters containing the estrogen response element TCAGGTCA CTG TGACCTGA can be regulated negatively; converse effects are observed with the estrogen receptor. They describe evidence that the transcriptional inhibitory effects of the T{sub 3} or estrogen receptors on the estrogen or T{sub 3} response elements, respectively, are imposed by amino acid sequences in the C'-terminal region that colocalize with dimerization and hormone-binding domains and that these sequences can transfer ...

1990-10-01

195

Synergistic epigenetic reactivation of estrogen receptor-? (ER?) by combined green tea polyphenol and histone deacetylase inhibitor in ER?-negative breast cancer cells  

UK PubMed Central (United Kingdom)

BackgroundThe status of estrogen receptor-α (ERα) is critical to the clinical prognosis and therapeutic approach in breast cancer. ERα-negative breast cancer...Full Text Available

196

Selective stimulation of catecholamine release from bovine adrenal chromaffin cells by an ionotropic purinergic receptor sensitive to 2-methylthio ATP  

UK PubMed Central (United Kingdom)

Background2-Methylthioadenosine 5'-triphosphate (2-MeSATP), formerly regarded as a specific P2Y (metabotropic) purinergic receptor agonist, stimulates Ca2+ influx and...Full Text Available

197

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

UK PubMed Central (United Kingdom)

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

198

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)  

UK PubMed Central (United Kingdom)

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

199

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

UK PubMed Central (United Kingdom)

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

200

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

UK PubMed Central (United Kingdom)

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

201

Reduced expression of a human V beta 6.1 T-cell receptor allele.  

UK PubMed Central (United Kingdom)

We have previously described an allelic polymorphism in the V beta 6.1 T-cell receptor gene. The V beta 6.1B allele is associated with disease in a subgroup of patients with juvenile rheumatoid arthritis....Full Text Available

1993-05-15

202

Prolactin and Its Receptor Are Expressed in Murine Hair Follicle Epithelium, Show Hair Cycle-Dependent Expression, and Induce Catagen  

UK PubMed Central (United Kingdom)

Here, we provide the first study of prolactin (PRL) and prolactin receptor (PRLR) expression during the nonseasonal murine hair cycle, which is, in contrast to sheep, comparable with the human scalp...Full Text Available

2003-05-01

203

Pore properties and pharmacological features of the P2X receptor channel in airway ciliated cells  

UK PubMed Central (United Kingdom)

Airway ciliated cells express an ATP-gated P2X receptor channel of unknown subunit composition (P2Xcilia) which is modulated by Na+ and by long exposures to ATP. P2Xcilia...Full Text Available

2006-03-15

204

Pharmacokinetics and pharmacodynamics of terbogrel, a combined thromboxane A2 receptor and synthase inhibitor, in healthy subjects  

UK PubMed Central (United Kingdom)

AimsTo characterize the pharmacokinetics of terbogrel, a new combined thromboxane A2 (TxA2) receptor and synthase inhibitor, in healthy human subjects after...Full Text Available

2004-07-01

205

Myocardial metabolic regulation through peroxisome proliferator-activated receptor alpha after myocardial infarction  

UK PubMed Central (United Kingdom)

Although peroxisome proliferator-activated receptor alpha (PPARα) is closely associated with myocardial fatty acid metabolism, the pathophysiological role of PPARα in myocardial infarction...Full Text Available

2003-01-01

206

Molecular recognition of nitrated fatty acids by PPAR[gamma  

Energy Technology Data Exchange (ETDEWEB)

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

207

Low concentrations of primaquine inhibit degradation but not receptor-mediated endocytosis of asialoorosomucoid by HepG2 cells  

Energy Technology Data Exchange (ETDEWEB)

Asialoorosomucoid (ASOR) is internalized and degraded by HepG2 cells after binding to the asialoglycoprotein (ASGP) receptor, internalization through the coated pit/coated vesicle pathway, and trafficking to lysosomes. Primaquine, an 8-aminoquinoline antimalarial compound, inhibits ASOR degradation at concentrations greater than 0.2 mM by neutralizing intracellular acid compartments. This leads to alterations in surface receptor number, receptor-ligand dissociation, and receptor recycling. We have investigated the effects of primaquine on 125I-ASOR uptake and degradation as a function of primaquine concentration and duration of exposure. Concentrations below those required for neutralization of acidic compartments block 125I-ASOR degradation in HepG2 cells and lead to intracellular ligand accumulation. This effect is maximal at 80 microM primaquine. The intracellular 125I-ASOR is undegraded, dissociated ...

1991-02-01

208

Low concentrations of primaquine inhibit degradation but not receptor-mediated endocytosis of asialoorosomucoid by HepG2 cells  

International Nuclear Information System (INIS)

Asialoorosomucoid (ASOR) is internalized and degraded by HepG2 cells after binding to the asialoglycoprotein (ASGP) receptor, internalization through the coated pit/coated vesicle pathway, and trafficking to lysosomes. Primaquine, an 8-aminoquinoline antimalarial compound, inhibits ASOR degradation at concentrations greater than 0.2 mM by neutralizing intracellular acid compartments. This leads to alterations in surface receptor number, receptor-ligand dissociation, and receptor recycling. We have investigated the effects of primaquine on 125I-ASOR uptake and degradation as a function of primaquine concentration and duration of exposure. Concentrations below those required for neutralization of acidic compartments block 125I-ASOR degradation in HepG2 cells and lead to intracellular ligand accumulation. This effect is maximal at 80 microM primaquine. The intracellular 125I-ASOR is undegraded, dissociated ...

209

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

Energy Technology Data Exchange (ETDEWEB)

(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 binding equilibrium constant varied ...

1991-03-01

210

Immunohistochemical localization of low density lipoprotein receptor-related protein 1 and ?2-Macroglobulin in retinal and choroidal tissue of proliferative retinopathies  

UK PubMed Central (United Kingdom)

The immunolocalization of the low density lipoprotein receptor-related protein 1 (LRP1) and its ligand alpha 2-Macroglobulin (α2M) was examined in tissues from human donor...Full Text Available

2010-08-01

211

Growth differentiation factor-9 stimulates progesterone synthesis in granulosa cells via a prostaglandin E2/EP2 receptor pathway  

UK PubMed Central (United Kingdom)

Growth differentiation factor-9 (GDF-9), an oocyte-secreted member of the transforming growth factor β superfamily, progesterone receptor, cyclooxygenase 2 (Cox2; Ptgs2), and the EP2 prostaglandin...Full Text Available

2000-08-29

212

Enhanced ?2-adrenergic receptor (?2AR) signaling by adeno-associated viral (AAV)-mediated gene transfer  

UK PubMed Central (United Kingdom)

Backgroundβ2-Adrenergic receptors2AR) play important regulatory roles in a variety of cells and organ systems and are important therapeutic...Full Text Available

213

Discordant expression and variable numbers of neighboring GGA- and GAA-rich triplet repeats in the 3' untranslated regions of two groups of messenger RNAs encoded by the rat polymeric immunoglobulin receptor gene.  

UK PubMed Central (United Kingdom)

An unusual S1-nuclease sensitive microsatellite (STMS) has been found in the single copy, rat polymeric immunoglobulin receptor gene (PIGR) terminal exon. In Fisher rats, elements within or beyond the...Full Text Available

1995-04-11

214

Decay-accelerating factor CD55 is identified as the receptor for echovirus 7 using CELICS, a rapid immuno-focal cloning method.  

UK PubMed Central (United Kingdom)

Using an anti-receptor mAb that blocks the attachment of echovirus 7 and related viruses (echoviruses 13, 21, 29 and 33), we have isolated a complementary DNA clone that encodes the human decay-accelerating...Full Text Available

1994-11-01

215

CD5 Is Dissociated from the B-Cell Receptor in B Cells from Bovine Leukemia Virus-Infected, Persistently Lymphocytotic Cattle: Consequences to B-Cell Receptor-Mediated Apoptosis  

UK PubMed Central (United Kingdom)

Bovine leukemia virus (BLV), a retrovirus related to human T-cell leukemia virus types 1 and 2, can induce persistent nonneoplastic expansion of the CD5+ B-cell population, termed...Full Text Available

2001-02-01

216

Autocrine regulation of T-cell activation by ATP release and P2X7 receptors  

UK PubMed Central (United Kingdom)

T-cell activation requires the influx of extracellular calcium, although mechanistic details regarding such activation are not fully defined. Here, we show that P2X7 receptors play a key...Full Text Available

2009-06-01

217

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  

UK PubMed Central (United Kingdom)

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

218

An activated renin-angiotensin system maintains normal blood pressure in aryl hydrocarbon receptor heterozygous mice but not in null mice  

UK PubMed Central (United Kingdom)

It has been postulated that fetal vascular abnormalities in aryl hydrocarbon receptor null (ahr−/−) mice may alter cardiovascular homeostasis in adulthood....Full Text Available

2010-07-15

219

Adenosine A1 receptors (A1Rs) play a critical role in osteoclast formation and function  

UK PubMed Central (United Kingdom)

Adenosine regulates a wide variety of physiological processes via interaction with one or more G-protein-coupled receptors (A1R, A2AR, A2BR, and A3R)....Full Text Available

2010-07-01

220

Acute Ca2+-Dependent Desensitization of 5-Ht1A Receptors is Mediated by Activation of Pka in Rat Serotonergic Neurons  

UK PubMed Central (United Kingdom)

This report investigates acute changes in the sensitivity of 5-HT1A receptors in dorsal raphe (dr) neurons in response to elevated serotonin. DR neurons were isolated from adult rats...Full Text Available

2010-08-11

221

?1-Fetoprotein Transcription Factor (FTF)/Liver Receptor Homolog-1 (LRH-1) Is an Essential Lipogenic Regulator  

UK PubMed Central (United Kingdom)

α1-Fetoprotein transcription factor (FTF), also known as liver receptor homolog 1 (LRH-1) is highly expressed in liver and intestine, where it is implicated in the regulation...Full Text Available

2010-04-01

222

5'-Azido-[3,6-3H2]-1-napthylphthalamic acid, a photoactivatable probe for naphthylphthalamic acid receptor proteins from higher plants: identification of a 23-kDa protein from maize coleoptile plasma membranes.  

UK PubMed Central (United Kingdom)

1-Naphthylphthalamic acid (NPA) is a specific inhibitor of polar auxin transport that blocks carrier-mediated auxin efflux from plant cells. To allow identification of the NPA receptor thought to be...Full Text Available

1992-01-15

223

(-)-Epigallocatechin Gallate Regulates CD3-mediated T Cell Receptor Signaling in Leukemia through the Inhibition of ZAP-70 Kinase*  

UK PubMed Central (United Kingdom)

The ζ chain-associated 70-kDa protein (ZAP-70) of tyrosine kinase plays a critical role in T cell receptor-mediated signal transduction and the immune response. A high level of ZAP-70 expression...Full Text Available

2008-10-17

224

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

Energy Technology Data Exchange (ETDEWEB)

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

225

Radioiodination of chicken luteinizing hormone without affecting receptor binding potency  

Energy Technology Data Exchange (ETDEWEB)

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 was 12-16%, nonspecific binding was as low as 2-4% in the ...

1989-12-01

226

Chromosomal localization of the human retinoid X receptors  

Energy Technology Data Exchange (ETDEWEB)

The recently described retinoid X receptors (RXRs) respond to the novel retinoid 9-cis-retinoic acid and also serve as heterodimeric partners for the vitamin D, thyroid hormone, and retinoic acid receptors (VDR, TR, and RAR, respectively). In this work, the authors report high-resolution localization of the human RXR genes within cytogenetic bands and also within a standard reference map of cosmid DNA markers on human chromosomes. They have determined the location of the human RXR genes by pairwise hybridization of the RXR cosmids and reference markers, using fluorescence in situ hybridization. They localized (i) RXR[alpha] (RXRA) to chromosome 9 band q34.3; (ii) RXR[beta] (RXRB) to chromosome 6 band 21.3; and (iii) RXR[gamma] (RXRG) to chromosome 1 band q22-q23. Six retinoid-responsive transcription factors have been identified so far, including three retinoic acid receptors in addition to the three RXRs. Interestingly, ...

1994-04-01

227

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

Energy Technology Data Exchange (ETDEWEB)

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 ...

2004-09-15

228

Computational Complexity of Cyclotomic Fast Fourier Transforms over Characteristic-2 Fields  

CERN Document Server

Cyclotomic fast Fourier transforms (CFFTs) are efficient implementations of discrete Fourier transforms over finite fields, which have widespread applications in cryptography and error control codes. They are of great interest because of their low multiplicative and overall complexities. However, their advantages are shown by inspection in the literature, and there is no asymptotic computational complexity analysis for CFFTs. Their high additive complexity also incurs difficulties in hardware implementations. In this paper, we derive the bounds for the multiplicative and additive complexities of CFFTs, respectively. Our results confirm that CFFTs have the smallest multiplicative complexities among all known algorithms while their additive complexities render them asymptotically suboptimal. However, CFFTs remain valuable as they have the smallest overall ...

2011-01-01

229

Complexing of vanadium(3) with chromotropic acid derivatives  

International Nuclear Information System (INIS)

A spectrophotometric study has been made of the complex formation of vanadium (3) with arsenazo(1), arsenazo(3) and some monosubstituted derivatives of chromotropic acid and sulphanylamides. In acid medium vanadium (3) reacts with each of these reagents to produce a 1:1 complex. Optimum conditions of the complex formation was found. The effect of H"+ on the complex formation of vanadium (3) with chromotropic acid derivatives was established. It was found by the graphical method that the formation of the complex is accompanied by the elimination of one proton. Patterns were found of the influence of the nature of substituents in the organic compound on the ionization constants of acid groups and stability of complexes. Molar extinction coefficients, equilibrium constants of the formation reactions and instability constants for the complexes ...

1976-01-01

230

Use of receptor affinity chromatography in purification of the growth hormone-like factor produced by plerocercoids of the tapeworm Spirometra mansonoides.  

Science.gov (United States)

The plerocercoid stage of the tapeworm Spirometra mansonoides produces a functional analog of human growth hormone (hGH). Among the similarities between plerocercoid growth factor (PGF) and hGH is competition for the same receptors on rabbit liver membranes. To take advantage of this characteristic in a purification scheme for PGF, rabbit liver microsomes were solubilized in Triton X-100 and the hGH receptors were purified over an hGH affinity column. The purified receptors from six rabbit livers were coupled to Affi-Gel-10 to create a receptor affinity column which was used to purify PGF. Chromatography of crude PGF over the receptor column resulted in a 1044 fold increase in specific activity. SDS-PAGE in the presence of 2-mercaptoethanol showed that the affinity-purified PGF contained three protein bands with apparent Mrs of 27.5 K, 22 K, and 16.7 K. Injections of the ...

1988-01-01

231

Topographical distribution of decrements and recovery in muscarinic receptors from rat brains repeatedly exposed to sublethal doses of soman  

Energy Technology Data Exchange (ETDEWEB)

(3H)Quinuclidinyl benzilate binding to rat brain muscarinic receptors decreased after repeated exposure to soman, a potent organophosphorus cholinesterase inhibitor. The topographical distribution of this decrement was analyzed by quantitative receptor autoradiography. After 4 weeks of soman, three times a week, quinuclidinyl benzilate binding decreased to 67 to 80% of control in frontal and parietal cortex, caudate-putamen, lateral septum, hippocampal body, dentate gyrus, superior colliculus, nucleus of the fifth nerve, and central grey. Minor or no decreases were observed in thalamic or hypothalamic nuclei, reticular formation, pontine nuclei, inferior colliculus, nucleus of the seventh nerve, and cerebellum. Scatchard analyses of saturation curves using frontal cortex sections from soman-treated rats revealed a decrease in maximal quinuclidinyl benzilate binding from that in control rats and a return toward control levels by 24 days without ...

1984-08-01

232

Topographical distribution of decrements and recovery in muscarinic receptors from rat brains repeatedly exposed to sublethal doses of soman  

International Nuclear Information System (INIS)

[3H]Quinuclidinyl benzilate binding to rat brain muscarinic receptors decreased after repeated exposure to soman, a potent organophosphorus cholinesterase inhibitor. The topographical distribution of this decrement was analyzed by quantitative receptor autoradiography. After 4 weeks of soman, three times a week, quinuclidinyl benzilate binding decreased to 67 to 80% of control in frontal and parietal cortex, caudate-putamen, lateral septum, hippocampal body, dentate gyrus, superior colliculus, nucleus of the fifth nerve, and central grey. Minor or no decreases were observed in thalamic or hypothalamic nuclei, reticular formation, pontine nuclei, inferior colliculus, nucleus of the seventh nerve, and cerebellum. Scatchard analyses of saturation curves using frontal cortex sections from soman-treated rats revealed a decrease in maximal quinuclidinyl benzilate binding from that in control rats and a return toward control levels by 24 days without ...

1984-01-01

233

Natriuretic peptides in vascular physiology and pathology.  

Science.gov (United States)

Four major natriuretic peptides have been isolated: atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP), C-type natriuretic peptide (CNP), and Dendroaspis-type natriuretic peptide (DNP). Natriuretic peptides play an important role in the regulation of cardiovascular homeostasis maintaining blood pressure and extracellular fluid volume. The classical endocrine effects of natriuretic peptides to modulate fluid and electrolyte balance and vascular smooth muscle tone are complemented by autocrine and paracrine actions that include regulation of coronary blood flow and, therefore, myocardial perfusion; modulation of proliferative responses during myocardial and vascular remodeling; and cytoprotective anti-ischemic effects. The actions of natriuretic peptides are mediated by the specific binding of these peptides to three cell surface receptors: type A natriuretic peptide receptor (NPR-A), type B natriuretic peptide ...

2008-01-01

234

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

International Nuclear Information System (INIS)

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 ...

2011-02-01

235

Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells.  

Science.gov (United States)

Several examples of agonist-directed trafficking of receptor signalling at 5-HT2A and 5-HT2C receptors have been reported that involve independent downstream transduction pathways. We now report the functional selectivity of a series of chemically diverse agonists at human (h)5-HT2A, h5-HT2B and h5-HT2C-VSV by examining two related responses, the upstream activation of Gq/11 proteins in comparison with its associated cascade of calcium mobilisation. At the h5-HT2A receptor, d-lysergic acid diethylamide (LSD) and the antiparkinsonian agents lisuride, bromocriptine and pergolide exhibit a higher potency for Gq/11 activation than calcium release in contrast with all the other tested ligands such as 5-HT, mCPP and BW723C86, that show an opposite preference of signalling pathway. Comparable observations are made at h5-HT2B and h5-HT2C-VSV receptors, suggesting a similar mechanism of functional selectivity ...

2008-07-30

236

Stable halogen complexes of astatine cations in aqueous solutions  

International Nuclear Information System (INIS)

Halide complexes of astatine cations At"+ and AtO"+ were prepared and their rate of migration was measured. The complexes are of the type AtX_2"- and AtOX_2"- (X = Cl"-, Br"-, I"-). The bromo complexes, AtBr_2"- and AtOBr_2"-, have a higher stability than the chloro complexes. The hydrolysis in weakly alkaline solution of AtX_2"- resulted At"-, and that of AtOX_2"- AtO_2"-. (author).

237

Imaging of gastrinomas by nuclear medicine methods  

International Nuclear Information System (INIS)

Somatostatin receptor scintigraphy (SRS) is a valuable method for the detection of somatostatin receptor-positive lesions. Most gastrinomas (over-)express the somatostatin receptor subtype 2 which can be targeted by In-111 labeled Octreotide. Different studies show a high sensitivity of SRS for the localization and staging of gastrinomas. SRS seems to be superior to other non-invasive imaging modalities and has been proven to significantly contribute to patient management. However, the sensitivity depends on the size and exact localization of the tumors. Smaller lesions and lesions located in the duodenum show a significantly lower sensitivity. In any case, SRS belongs to the routine imaging procedure for gastrinomas for localization and staging and can also be used for evaluation of the tumor progression. (author)

238

Generation and Characterization of Monoclonal Antibodies to Human Keratinocyte Growth Factor Receptor  

British Library Electronic Table of Contents (United Kingdom)

Keratinocyte growth factor receptor (KGFR) and fibroblast growth factor receptor (FGFR) 2c share identical amino acid sequences, except for a 46-amino acid domain in the extracellular region. Monoclonal antibodies (MAbs) specific to KGFR have not been reported nor are commercially available. In this study, we generated murine MAbs specific to KGFR in non-obese diabetic (NOD) mice using a modified Repeated Immunizations at Multiple Sites (RIMMS) technology. Stable cell lines expressing the full-length human KGFR or FGFR2c were produced to facilitate the identification of KGFR-specific MAbs. Following the initial screening of hybridoma clones with a fluorescence-based, confocal cell detection method and ELISA, KGFR-specific MAbs were selected and confirmed by flow cytometry and Western blot ...

2006-01-01

239

The complexity of gene expression dynamics revealed by permutation entropy  

UK PubMed Central (United Kingdom)

BackgroundHigh complexity is considered a hallmark of living systems. Here we investigate the complexity of temporal gene expression patterns using the concept of Permutation Entropy...Full Text Available

240

Subunits of the Drosophila CCR4-NOT complex and their roles in mRNA deadenylation  

UK PubMed Central (United Kingdom)

The CCR4-NOT complex is the main enzyme catalyzing the deadenylation of mRNA. We have investigated the composition of this complex in Drosophila melanogaster by immunoprecipitation...Full Text Available

2010-07-01

241

Rapamycin inhibits trypanosome cell growth by preventing TOR complex 2 formation  

UK PubMed Central (United Kingdom)

Target of rapamycin (TOR) kinases control cell growth through two functionally distinct multiprotein complexes. TOR complex 1 (TORC1) controls temporal cell growth and is sensitive to rapamycin, whereas...Full Text Available

2008-09-23

242

Photochemistry and charge transfer chemistry of the platinum group elements  

Energy Technology Data Exchange (ETDEWEB)

During the past 3 years, progress was made in elucidating the excited state structures of Pt(diimine)(dithiolate) complexes, while more recent efforts focused on the photochemistry of these complexes and electronic structure of other dithiolate systems. A carbonyl-Ir-maleonitrile dithiolate complex is also studied.

1992-12-01

243

On the ease of predicting the thermodynamic properties of beta-cyclodextrin inclusion complexes  

UK PubMed Central (United Kingdom)

BackgroundIn this study we investigated the predictability of three thermodynamic quantities related to complex formation. As a model system we chose the host-guest complexes of...Full Text Available

244

Dynamics of ligand substitution in labile cobalt complexes resolved by ultrafast T-jump  

UK PubMed Central (United Kingdom)

Ligand exchange of hydrated metal complexes is common in chemical and biological systems. Using the ultrafast T-jump, we examined this process, specifically the transformation of aqua cobalt (II) complexes...Full Text Available

2008-09-02

245

Application of ?- and ?-Isomerism of Octahedral Metal Complexes for Inducing Chiral Nematic Phases  

UK PubMed Central (United Kingdom)

The Δ- and Λ-isomerism of octahedral metal complexes is employed as a source of chirality for inducing chiral nematic phases. By applying a wide range of chiral metal complexes as a...Full Text Available

246

metabotropic glutamate receptor 5 (mGluR5) has a critical role in inhibitory learning  

UK PubMed Central (United Kingdom)

The mechanisms that contribute to the extinction of previously acquired memories are not well understood. These processes, often referred to as inhibitory learning, are thought to be parallel...Full Text Available

2009-03-25

247

Zebrafish TRPA1 Channels are Required for Chemosensation but not for Thermosensation or Mechanosensory Hair Cell Function  

UK PubMed Central (United Kingdom)

Transient receptor potential (TRP) ion channels have been implicated in detecting chemical, thermal and mechanical stimuli in organisms ranging from mammals to Caenorhabditis elegans....Full Text Available

2008-10-01

248

Vitamin A Enhances Antitumor Effect of a Green Tea Polyphenol on Melanoma by Upregulating the Polyphenol Sensing Molecule 67-kDa Laminin Receptor  

UK PubMed Central (United Kingdom)

BackgroundGreen tea consumption has been shown to have cancer preventive qualities. Among the constituents of green tea, (-)-Epigallocatechin-3-O-gallate (EGCG)...Full Text Available

249

Tumor-derived extracellular mutations of PTPRT/PTP? are deficient in cell adhesion  

UK PubMed Central (United Kingdom)

Receptor protein tyrosine phosphatase T (PTPRT/PTPρ) is frequently mutated in human cancers including colon, lung, gastric and skin cancers. More than half of the identified tumor-derived...Full Text Available

2008-07-01

250

Trigeminal injury causes kappa opioid-dependent allodynic, glial and immune cell responses in mice  

UK PubMed Central (United Kingdom)

BackgroundThe dynorphin-kappa opioid receptor (KOR) system regulates glial proliferation after sciatic nerve injury. Here, we investigated its role in cell proliferation following...Full Text Available

251

Tone-Specific and Nonspecific Plasticity of the Auditory Cortex Elicited by Pseudoconditioning: Role of Acetylcholine Receptors and the Somatosensory Cortex  

UK PubMed Central (United Kingdom)

Experience-dependent plastic changes in the central sensory systems are due to activation of both the sensory and neuromodulatory systems. Nonspecific changes of cortical auditory neurons elicited by...Full Text Available

2008-09-01

252

Time-limited modulation of appetitive Pavlovian memory by D1 and NMDA receptors in the nucleus accumbens  

UK PubMed Central (United Kingdom)

Recent research has implicated the nucleus accumbens (NAc) in consolidating recently acquired goal-directed appetitive memories, including spatial learning and other instrumental processes. However,...Full Text Available

2005-04-26

253

The stereospecificity of LY253352 for alpha 1-adrenoceptor binding sites in the brain and prostate.  

UK PubMed Central (United Kingdom)

1. The stereospecificity of the enantiomers of LY253352, a potent and selective alpha 1-adrenoceptor antagonist, were studied in the human prostate and canine brain using radioligand receptor binding...Full Text Available

1988-09-01

254

The potential role of phrenic nucleus glutamate receptor subunits in mediating spontaneous crossed phrenic activity in neonatal rat  

UK PubMed Central (United Kingdom)

Cervical spinal cord hemisection rostral to the phrenic nucleus leads to paralysis of the ipsilateral hemidiaphragm in adult rats. Respiratory function can be restored to the paralyzed hemidiaphragm...Full Text Available

2009-08-01

255

The photoaffinity ligand [3,5-"3H] 4-azidoclonidine. Synthesis and characterization details  

International Nuclear Information System (INIS)

[3,5-"3H] 4-Azidoclonidine 6 was prepared from [3,5-"3H] 4-aminoclonidine 4 and has emerged as a valuable tool to study the alpha-2-adrenergic receptor. (author)

2004-07-01

256

The orphan nuclear receptor small heterodimer partner mediates male infertility induced by diethylstilbestrol in mice  

UK PubMed Central (United Kingdom)

Studies in rodents have shown that male sexual function can be disrupted by fetal or neonatal administration of compounds that alter endocrine homeostasis, such as the synthetic nonsteroidal estrogen...Full Text Available

2009-12-01

258

The effects of histamine and leukotriene receptor antagonism on nasal mannitol challenge in allergic rhinitis  

UK PubMed Central (United Kingdom)

AimsIt is unclear as to which mediators are involved in mediating the response to nasal mannitol challenge, a novel osmotic stimulus.MethodsA...Full Text Available

2003-06-01

259

The Receptor Tyrosine Kinase FGFR4 Negatively Regulates NF-kappaB Signaling  

UK PubMed Central (United Kingdom)

BackgroundNFκB signaling is of paramount importance in the regulation of apoptosis, proliferation, and inflammatory responses during human development and homeostasis, as...Full Text Available

260

The Case for Selection at CCR5-?32  

UK PubMed Central (United Kingdom)

The C-C chemokine receptor 5, 32 base-pair deletion (CCR5-Δ32) allele confers strong resistance to infection by the AIDS virus HIV. Previous studies have suggested...Full Text Available

2005-11-01

261

Temperature-induced opening of TRPV1 ion channel is stabilized by the pore domain  

UK PubMed Central (United Kingdom)

SummaryTRPV1 is the founding and best-studied member of the family of temperature-activated transient receptor potential ion channels (thermoTRPs). Voltage, chemicals, and heat...Full Text Available

2010-06-01

262

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?  

UK PubMed Central (United Kingdom)

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

263

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

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

264

Steroid hormones and brain development: some guidelines for understanding actions of pseudohormones and other toxic agents.  

UK PubMed Central (United Kingdom)

Gonadal, adrenal, and thyroid hormones affect the brain directly, and the sensitivity to hormones begins in embryonic life with the appearance of hormone receptor sites in discrete populations of neurons....Full Text Available

1987-10-01

265

Somatostatin receptor scintigraphy might be useful for detecting skeleton abnormalities in patients with multiple myeloma and plasmacytoma  

International Nuclear Information System (INIS)

Somatostatin receptor expression has been demonstrated on a number of plasma cell lines. Therefore, we questioned whether somatostatin receptor scintigraphy (SRS) can be used to demonstrate in vivo multiple myeloma (MM) activity. SRS was performed in newly diagnosed (n = 9) or relapsing (n = 18) MM patients or in patients with localized plasmacytoma (n = 2). The results were compared with radiographic findings. A positive SRS was demonstrated in 44% of the newly diagnosed patients, in 83% of the relapsed patients and in both patients with plasmacytoma. The SRS findings corresponded with radiographic abnormalities in 40% of the patients. However, in relapsed patients 60% demonstrated increased SRS uptake in areas without new radiographic abnormalities. The positive SRS corresponded with histologically proven disease activity and responded upon treatment. Moreover, immunohistochemical staining of MM material demonstrated concordant somatostatin ...

2010-01-01

266

Sigma-1 receptor agonist fluvoxamine for postoperative delirium in older adults: report of three cases  

UK PubMed Central (United Kingdom)

BackgroundPostoperative delirium is a topic of great importance in the geriatric surgical specialty. Although antipsychotic drugs are the medications most frequently used to treat...Full Text Available

267

Serum RANKL, osteoprotegerin (OPG), and RANKL/OPG ratio in nephrotic children  

UK PubMed Central (United Kingdom)

Receptor activator of NF-kB ligand (RANKL) and osteoprotegerin (OPG) play key roles in the pathogenesis of glucocorticoid-induced osteoporosis (GIO). The aim of our study was to determine whether the...Full Text Available

2010-10-01

268

Serum HER2 Level Measured by Dot Blot: A Valid and Inexpensive Assay for Monitoring Breast Cancer Progression  

UK PubMed Central (United Kingdom)

Human epidermal growth factor receptor 2 (HER2) is one of the most important prognostic and predictive factors for breast cancer patients. Recently, serum HER2...Full Text Available

269

Selective imaging of adherent targeted ultrasound contrast agents  

UK PubMed Central (United Kingdom)

The goal of ultrasonic molecular imaging is the detection of targeted contrast agents bound to receptors on endothelial cells. We propose imaging methods that can distinguish adherent microbubbles...Full Text Available

2007-04-21

270

Selective endothelin A-receptor blockade attenuates coronary microvascular dysfunction after coronary stenting in patients with type 2 diabetes  

UK PubMed Central (United Kingdom)

Background:Endothelin-1 may be involved in the development of diabetic microangiopathy. We studied the effect of endothelin-1 blockade on myocardial microcirculation during coronary...Full Text Available

2009-01-01

271

STIMULATION OF TARSAL RECEPTORS OF THE BLOWFLY BY ALIPHATIC ALDEHYDES AND KETONES  

UK PubMed Central (United Kingdom)

Rejection of eight aldehydes, eight ketones, five secondary alcohols, and 3-pentanol has been studied in the blowfly Phormia regina Meigen. The data agree with results previously reported...Full Text Available

1949-03-20

272

Role of adenosine in regulating glucose uptake during contractions and hypoxia in rat skeletal muscle  

UK PubMed Central (United Kingdom)

The effect of A1-adenosine receptor antagonism via 8-cyclopentyl-1,3-dipropyl-xanthine (CPDPX) on the stimulation of skeletal muscle glucose uptake by...Full Text Available

1999-02-15

273

Role of Estrogen Receptor-? in the Regulation of Claudin-6 Expression in Breast Cancer Cells  

UK PubMed Central (United Kingdom)

PurposeIn our previous studies we showed that upregulating claudin-6 (CLDN6) expression may contribute to preventing breast cancer, and that 17β-estradiol induces a concentration-...Full Text Available

2011-03-01

274

Residence time probability analysis of sulfur concentrations at Grand Canyon National Park  

Energy Technology Data Exchange (ETDEWEB)

A statistical method is developed to determine the locations of major pollutant sources affecting a distant downwind receptor, provided that air trajectories can be estimated. Probability density functions are estimated which indicate the overall residence time of air parcels over a given geographic region as they travel toward a receptor and residence time for the case of high pollutant concentrations at the receptor. These functions are used to estimate a conditional probability function which indicates the potential for a source region to contribute to high air pollution concentrations. Finally, a source contribution function is formulated to indicate the relative contribution of different source regions to high concentrations at the receptor. The method is tested using data collected at Grand Canyon National Park in 1980. The dominant pathway for air masses arriving at Grand Canyon during this ...

1985-01-01

275

Radiolabelled D_2 agonists as prolactinoma imaging agents: Progress report for period February 1, 1988--January 31, 1989  

International Nuclear Information System (INIS)

Targeted studies completed include the evaluation of tritiated N-0437, evaluation of "3"5S-cysteamine, evaluation of "1"8F-FDG and initiation of synthetic efforts towards the synthesis of iodinated N-0437 and pergolide analogs. The direction of the project has been changed due to several factors which include the decided lack of favorable experimental results, the excellence of results using muscarinic receptor ligands in pituitary, brain and heart and the contention of the DOE review panel that the original grant proposal was based on flawed assumptions together with their perceived lack of importance to pituitary imaging. In the final year of this grant, three studies will be completed. The first study is the continuation of synthetic efforts to prepare iodinated N-0437 and pergolide analogs for possible use as brain imaging agents. The second study is directed towards completion of biochemical evaluation of various muscarinic receptor ...

276

Radiolabelled D/sub 2/ agonists as prolactinoma imaging agents: Progress report for period February 1, 1988--January 31, 1989  

Energy Technology Data Exchange (ETDEWEB)

Targeted studies completed include the evaluation of tritiated N-0437, evaluation of /sup 35/S-cysteamine, evaluation of /sup 18/F-FDG and initiation of synthetic efforts towards the synthesis of iodinated N-0437 and pergolide analogs. The direction of the project has been changed due to several factors which include the decided lack of favorable experimental results, the excellence of results using muscarinic receptor ligands in pituitary, brain and heart and the contention of the DOE review panel that the original grant proposal was based on flawed assumptions together with their perceived lack of importance to pituitary imaging. In the final year of this grant, three studies will be completed. The first study is the continuation of synthetic efforts to prepare iodinated N-0437 and pergolide analogs for possible use as brain imaging agents. The second study is directed towards completion of biochemical evaluation of various muscarinic ...

1988-10-15

277

RXR activators molecular signalling: involvement of a PPAR?-dependent pathway in the liver and kidney, evidence for an alternative pathway in the heart  

UK PubMed Central (United Kingdom)

In this study we compared the molecular signalling elicited by rexinoids, selective retinoid X receptor (RXR)-activators, in several organs (i.e. liver, kidney,...Full Text Available

2003-03-01

278

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

UK PubMed Central (United Kingdom)

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

279

Putative Biomarkers and Targets of Estrogen Receptor Negative Human Breast Cancer  

UK PubMed Central (United Kingdom)

Breast cancer is a progressive and potentially fatal disease that affects women of all ages. Like all progressive diseases, early and reliable diagnosis is the key for successful treatment and annihilation....Full Text Available

280

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

UK PubMed Central (United Kingdom)

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

281

Prognostic Significance of Peritumoral Lymphatic Vessel Density and Vascular Endothelial Growth Factor Receptor 3 in Invasive Squamous Cell Cervical Cancer  

UK PubMed Central (United Kingdom)

Cervical cancer is known to metastasize primarily by the lymphatic system. Dissemination through lymphatic vessels represents an early step in regional tumor progression, and the presence of lymphatic...Full Text Available

282

Pretreatment with a soluble activin type IIB receptor/Fc fusion protein improves hypoxia-induced muscle dysfunction  

UK PubMed Central (United Kingdom)

Hypoxia, or reduced oxygen, occurs in a variety of clinical and environmental situations. Hypoxic exposure is associated with decreased muscle mass and a concomitant reduction in exercise capacity,...Full Text Available

2010-01-01

283

Prenatal cocaine reduces AMPA receptor synaptic expression through hyperphosphorylation of the synaptic anchoring protein GRIP  

UK PubMed Central (United Kingdom)

Prenatal cocaine exposure produces sustained neurobehavioral and brain synaptic changes closely resembling those of animals with defective alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic...Full Text Available

2009-05-13

284

Pore-forming toxins trigger shedding of receptors for interleukin 6 and lipopolysaccharide.  

UK PubMed Central (United Kingdom)

Cleavage of membrane-associated proteins with the release of biologically active macromolecules is an emerging theme in biology. However, little is known about the nature and regulation of the involved...Full Text Available

1996-07-23

285

Plasma membrane as the target site of cholic acid analogs.  

Science.gov (United States)

Although the mechanism is unknown, Calculus Bovis and its active components, cholic acid analogs (CAAs), have been used in China to treat a wide range of diseases. Based on the previous finding that the potency of CAA is strongly dependent on the intrinsic surface activity, this paper aimed to investigate the role of the plasma membrane in the pharmacological activity of CAAs. First, CAAs (0.1 mM) caused a surface activity-dependent depression on ATPase activity in the cell membrane extract, but it had no effects on other cellular extracts, suggesting an indispensable role of the membrane environment for pharmacological activity. Second, CAAs lowered the membrane fluidity of cultured Caco-2 cells with the same rank-order of potency sequence. Third, the hypothesis that any functional protein located on the membrane is influenced by changes in cellular membrane fluidity was supported by: ileal contraction that was induced by acetylcholine and mediated by the muscarinic ...

2011-08-03

286

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

UK PubMed Central (United Kingdom)

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

287

Parallel helix bundles and ion channels: molecular modeling via simulated annealing and restrained molecular dynamics.  

UK PubMed Central (United Kingdom)

A parallel bundle of transmembrane (TM) alpha-helices surrounding a central pore is present in several classes of ion channel, including the nicotinic acetylcholine receptor (nAChR). We have modeled...Full Text Available

1994-10-01

288

Paradoxical function for the receptor for advanced glycation end products in mouse models of pulmonary fibrosis  

UK PubMed Central (United Kingdom)

Idiopathic pulmonary fibrosis (IPF) is a progressive disease with poor survival. The identification of therapeutic targets is essential to improving outcomes. Previous studies found that expression...Full Text Available

2011-03-31

289

P2Y2 Nucleotide Receptor-Mediated Responses in Brain Cells  

UK PubMed Central (United Kingdom)

Acute inflammation is important for tissue repair; however, chronic inflammation contributes to neurodegeneration in Alzheimer’s disease (AD) and occurs when glial cells undergo prolonged...Full Text Available

2010-06-01

290

Ontogenetic Profile of the Expression of Thyroid Hormone Receptors in Rat and Human Corpora Cavernosa of the Penis  

UK PubMed Central (United Kingdom)

IntroductionIn the last few years, various studies have underlined a correlation between thyroid function and male sexual function, hypothesizing a direct action of thyroid hormones...Full Text Available

2010-04-01

291

Nuclear receptor ERR? and coactivator PGC-1? are effectors of IFN-?-induced host defense  

UK PubMed Central (United Kingdom)

Macrophage activation by the proinflammatory cytokine interferon-γ (IFN-γ) is a critical component of the host innate response to bacterial pathogenesis. However, the precise nature...Full Text Available

2007-08-01

292

Nuclear Receptor Rev-erb Alpha (Nr1d1) Functions in Concert with Nr2e3 to Regulate Transcriptional Networks in the Retina  

UK PubMed Central (United Kingdom)

The majority of diseases in the retina are caused by genetic mutations affecting the development and function of photoreceptor cells. The transcriptional networks directing these processes are regulated...Full Text Available

293

Noradrenergic ?1 Receptors as a Novel Target for the Treatment of Nicotine Addiction  

UK PubMed Central (United Kingdom)

Nicotine is the main psychoactive ingredient in tobacco and its rewarding effects are considered primarily responsible for persistent tobacco smoking and relapse. Although dopamine has been extensively...Full Text Available

2010-07-01

294

Nonsteroidal Selective Androgen Receptor Modulators Enhance Female Sexual Motivation  

UK PubMed Central (United Kingdom)

Women experience a decline in estrogen and androgen levels after natural or surgically induced menopause, effects that are associated with a loss of sexual desire and bone mineral density. Studies in...Full Text Available

2010-08-01

295

Neuroprotective effect of paeoniflorin on cerebral ischemic rat by activating adenosine A1 receptor in a manner different from its classical agonists  

UK PubMed Central (United Kingdom)

The effects of paeoniflorin (PF), a compound isolated from Paeony radix, on neurological impairment and histologically measured infarction volume...Full Text Available

2005-10-01

296

Neural injury following stroke: are Toll-like receptors the link between the immune system and the CNS?  

UK PubMed Central (United Kingdom)

The CNS can exhibit features of inflammation in response to injury, infection or disease, whereby resident cells generate inflammatory mediators, including cytokines, prostaglandins, free radicals and...Full Text Available

2010-08-01

297

NMDA Receptor Blockade with Memantine Attenuates White Matter Injury in a Rat Model of Periventricular Leukomalacia  

UK PubMed Central (United Kingdom)

Hypoxia–ischemia (H/I) in the premature infant leads to white matter injury termed periventricular leukomalacia (PVL), the leading cause of subsequent neurological deficits. Glutamatergic...Full Text Available

2008-06-25

298

Myelin associated glycoprotein cross-linking triggers its partitioning into lipid rafts, specific signaling events and cytoskeletal rearrangements in oligodendrocytes  

UK PubMed Central (United Kingdom)

Myelin-associated glycoprotein (MAG) has been implicated in inhibition of nerve regeneration in the CNS. This results from interactions between MAG and the Nogo receptor and gangliosides on...Full Text Available

2004-02-01

299

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

UK PubMed Central (United Kingdom)

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

300

Molecular Mechanistic Insights into the Endothelial Receptor Mediated Cytoadherence of Plasmodium falciparum-Infected Erythrocytes  

UK PubMed Central (United Kingdom)

Cytoadherence or sequestration is essential for the pathogenesis of the most virulent human malaria species, Plasmodium falciparum (P. falciparum). Similar to leukocyte-endothelium...Full Text Available

301

Modulation of the human hair follicle pigmentary unit by corticotropin-releasing hormone and urocortin peptides  

UK PubMed Central (United Kingdom)

Human skin is a local source of corticotropin-releasing hormone (CRH) and expresses CRH and CRH receptors (CRH-R) at mRNA and protein levels. Epidermal melanocytes respond to CRH by induction...Full Text Available

2006-05-01

302

Microglial Fc Receptors Mediate Physiological Changes Resulting From Antibody Cross-Linking of Myelin Oligodendrocyte Glycoprotein  

UK PubMed Central (United Kingdom)

Antibodies to myelin oligodendrocyte glycoprotein (MOG) have been implicated in Multiple Sclerosis demyelination through activation of complement and/or macrophage-effector processes. We presented...Full Text Available

2008-05-30

303

MFR, a Putative Receptor Mediating the Fusion of Macrophages  

UK PubMed Central (United Kingdom)

We had previously identified a macrophage surface protein whose expression is highly induced, transient, and specific, as it is restricted to actively fusing macrophages in vitro and in vivo. This protein...Full Text Available

1998-11-01

304

Long-Lasting Adaptations of the NR2B-containing NMDA Receptors in the Dorsomedial Striatum Play a Crucial Role in Alcohol Consumption and Relapse  

UK PubMed Central (United Kingdom)

A growing number of studies suggest that the development of compulsive drug seeking and taking depends on dorsostriatal mechanisms. We previously observed that ex vivo acute...Full Text Available

2010-07-28

305

Lnk controls mouse hematopoietic stem cell self-renewal and quiescence through direct interactions with JAK2  

UK PubMed Central (United Kingdom)

In addition to its role in megakaryocyte production, signaling initiated by thrombopoietin (TPO) activation of its receptor, myeloproliferative leukemia virus protooncogene (c-Mpl, or Mpl), controls...Full Text Available

2008-08-01

306

Listeria monocytogenes Infection Induces Prosurvival Metabolic Signaling in Macrophages?  

UK PubMed Central (United Kingdom)

Host cells use metabolic signaling through the LXRα nuclear receptor to defend against Listeria monocytogenes infection. 25-Hydroxycholesterol is a natural ligand of LXRs that...Full Text Available

2011-04-01

307

Lack of Association Between Prokineticin 2 Gene and Japanese Methamphetamine Dependence  

UK PubMed Central (United Kingdom)

Disruption of circadian rhythms may be involved in the pathophysiology of psychiatric disorders, including drug addiction. Recently, we detected the significant association between prokineticin 2 receptor...Full Text Available

2011-03-01

308

JAK/STAT Pathways in Cytokine Signaling and Myeloproliferative Disorders  

UK PubMed Central (United Kingdom)

Hematopoiesis is the cumulative result of intricately regulated signaling pathways that are mediated by cytokines and their receptors. Studies conducted over the past 10 to 15 years have revealed that...Full Text Available

2010-10-01

309

Interaction of Platelet Membrane Receptors with von Willebrand Factor, Ristocetin, and the Fc Region of Immunoglobulin G  

UK PubMed Central (United Kingdom)

The agglutination of human platelets by ristocetin and von Willebrand factor was inhibited by aggregated immunoglobulin (Ig)G and by Fc fragments of IgG, but not by Fab, F(ab′)2 or...Full Text Available

1978-11-01

310

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

UK PubMed Central (United Kingdom)

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

311

Insulin receptor signaling in the development of neuronal structure and function  

UK PubMed Central (United Kingdom)

Sensory experience plays a crucial role in regulating neuronal shape and in developing synaptic contacts during brain formation. These features are required for a neuron to receive, integrate, and transmit...Full Text Available

312

Inactivating cholecystokinin-2 receptor inhibits progastrin-dependent colonic crypt fission, proliferation, and colorectal cancer in mice  

UK PubMed Central (United Kingdom)

Hyperproliferation of the colonic epithelium, leading to expansion of colonic crypt progenitors, is a recognized risk factor for colorectal cancer. Overexpression of progastrin, a nonamidated and incompletely...Full Text Available

2009-09-01

313

Immunolocalization of endothelin-B receptor in mouse intestinal tract.  

Science.gov (United States)

The endothelin-B (ETB) receptor is a G-protein-coupled receptor that binds endothelin ligands and is essential for the development of epidermal melanocytes and enteric neurons. Recent reports indicate that ETB is localized to nuclei in cardiac ventricular myocytes, although it has been thought that ETB is localized mainly on the plasma membrane. It remains unknown, however, whether this unique distribution of ETB occurs in other tissues. To elucidate the subcellular distribution of ETB in the intestine, we performed immunofluorescence of ETB in mouse intestine using a specific antibody. ETB-like immunoreactivity was detected in both the mucosal and muscle layers. In the mucosal layer, villous epithelial cells, stromal cells of the lamina propria, and cryptic cells were immunostained. Subcellularly, ETB is localized mainly to the nuclei of villous epithelial cells. In the muscle layer, immunoreactivity of ETB was localized to the myenteric ...

2004-11-01

314

Identification of circulating neuropilin-1 and dose-dependent elevation following anti-neuropilin-1 antibody administration  

UK PubMed Central (United Kingdom)

Neuropilin-1 (NRP1) acts as a co-receptor for class 3 semaphorins and vascular endothelial growth factor and is an attractive angiogenesis target for cancer therapy. In addition to the transmembrane...Full Text Available

2009-07-01

315

Identification and characterization of Aedes aegypti aminopeptidase N as a putative receptor of Bacillus thuringiensis Cry11A toxin  

UK PubMed Central (United Kingdom)

Bacillus thuringiensis subsp. israelensis, which is used worldwide to control Aedes aegypti larvae, produces Cry11Aa and other toxins during...Full Text Available

2009-10-01

316

Human placental transport of cimetidine.  

UK PubMed Central (United Kingdom)

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

317

Histamine Regulation in Glucose and Lipid Metabolism via Histamine Receptors  

UK PubMed Central (United Kingdom)

Histamine has been proposed to be an important regulator of energy intake and expenditure. The aim of this study was to evaluate histamine regulation of glucose and lipid metabolism and development...Full Text Available

2010-08-01

318

Glutamatergic regulation of ghrelin-induced activation of the mesolimbic dopamine system  

UK PubMed Central (United Kingdom)

Recently, we demonstrated that the central ghrelin signalling system, involving the ghrelin receptor (GHS-R1A), is important for alcohol reinforcement. Ghrelin targets a key mesolimbic circuit involved...Full Text Available

2011-01-01

319

Glutamate Receptor-Mediated Restoration of Experience-Dependent Place Field Expansion Plasticity in Aged Rats  

UK PubMed Central (United Kingdom)

Place fields of hippocampal pyramidal cells expand asymmetrically when adult rats repeatedly follow the same route. This behaviorally-induced expression of neuronal plasticity utilizes an NMDAR-dependent,...Full Text Available

2008-06-01

320

Genetic Elucidation of Human Hyperosmia to Isovaleric Acid  

UK PubMed Central (United Kingdom)

The genetic basis of odorant-specific variations in human olfactory thresholds, and in particular of enhanced odorant sensitivity (hyperosmia), remains largely unknown. Olfactory receptor (OR) segregating...Full Text Available

2007-11-01

321

Gene-silencing reveals the functional significance of pheromone biosynthesis activating neuropeptide receptor (PBAN-R) in a male moth  

UK PubMed Central (United Kingdom)

The role of pheromone biosynthesis activating neuropeptide (PBAN) in the regulation of pheromone biosynthesis of several female moth species is well elucidated, but its role in the males has been a...Full Text Available

2010-09-28

322

Gadolinium-containing phosphatidylserine liposomes for molecular imaging of atherosclerosis  

UK PubMed Central (United Kingdom)

Exteriorized phosphatidylserine (PS) residues in apoptotic cells trigger rapid phagocytosis by macrophage scavenger receptor pathways. Mimicking apoptosis with liposomes containing PS may represent...Full Text Available

2009-11-01

323

Fungal recognition is mediated by the association of dectin-1 and galectin-3 in macrophages  

UK PubMed Central (United Kingdom)

Dectin-1, the major β-glucan receptor in leukocytes, triggers an effective immune response upon fungal recognition. Here we use sortase-mediated transpeptidation, a technique that allows placement...Full Text Available

2011-08-23

324

Functional significance of UDP-glucuronosyltransferase (UGT) variants in the metabolism of active tamoxifen metabolites  

UK PubMed Central (United Kingdom)

Tamoxifen (TAM) is a selective estrogen receptor modulator widely used in the prevention and treatment of breast cancer. A major mode of metabolism of the major active metabolites of TAM, 4-OH-TAM...Full Text Available

2009-03-01

325

FGF18 is required for normal cell proliferation and differentiation during osteogenesis and chondrogenesis  

UK PubMed Central (United Kingdom)

Fibroblast growth factor (FGF) signaling is involved in skeletal development of the vertebrate. Gain-of-function mutations of FGF receptors (FGFR) cause craniosynostosis, premature fusion of the skull,...Full Text Available

2002-04-01

326

Expression of leukotriene receptors in the rat dorsal root ganglion and the effects on pain behaviors  

UK PubMed Central (United Kingdom)

BackgroundLeukotrienes (LTs) belong to the large family of lipid mediators implicated in various inflammatory conditions such as asthma and rheumatoid arthritis. Four distinct types...Full Text Available

327

EphB Receptors Couple Dendritic Filopodia Motility to Synapse Formation  

UK PubMed Central (United Kingdom)

SUMMARYMotile dendritic filopodial processes are thought to be precursors of spine synapses, but how motility relates to cell-surface cues required for axon-dendrite recognition...Full Text Available

2008-07-10

328

Eosinophils Utilize Multiple Chemokine Receptors for Chemotaxis to the Parasitic Nematode Strongyloides stercoralis  

UK PubMed Central (United Kingdom)

Protective innate immunity to the nematode Strongyloides stercoralis requires eosinophils in the parasite killing process. Experiments were performed to determine if an extract of S....Full Text Available

2009-10-01

329

Effects of Long-Term Pioglitazone Treatment on Peripheral and Central Markers of Aging  

UK PubMed Central (United Kingdom)

BackgroundThiazolidinediones (TZDs) activate peroxisome proliferator-activated receptor gamma (PPARγ) and are used clinically to help restore peripheral insulin sensitivity...Full Text Available

330

Effective In Vitro Clearance of Porphyromonas gingivalis by Fc? Receptor I (CD89) on Gingival Crevicular Neutrophils  

UK PubMed Central (United Kingdom)

Porphyromonas gingivalis has been implicated as a causative pathogen in periodontitis. Immunotherapeutic approaches have recently been suggested to aid in the clearance of P....Full Text Available

2001-05-01

331

Effect of differentiation on specific receptor sites and endocytosis of transferrin in a cell (HT-29) derived from human colic adenocarcinoma  

International Nuclear Information System (INIS)

The specific receptor sites and the endocytosis of transferrin (Tf) are evidenced in a cell line (HT-29) derived from a human colic adenocarcinoma by means of "1"2"5I radiolabeled Tf. The receptor density is studied in undifferentiated (UD) or differentiated (D) cells with respective doubling times of about 24 hours and 46 hours. The number of binding sites for Tf is 162,000 (K_d = 7.8 nmol/l in ND cells and 68,000 (K_d = 7.40 nmol/l) in D cells. The distribution between the Tf bound to the cell surface and the internalized Tf is investigated by elimination of Tf bound to the surface by an acid wash method. The intracellular cycle of Tf seems to be characterized by a slower kinetics in UD cells. The high density of Tf receptor sites in HT-29 UD cells should allow the detection or the treatment of highly evolutive colic adenocarcinoma by means of Tf.

332

Effect of Peroxisome Proliferator-Activated Receptor Gamma Agonist (Pioglitazone) and Methotrexate on Disease Activity in Rheumatoid Arthritis (Experimental and Clinical Study)  

UK PubMed Central (United Kingdom)

Objective:To investigate the combined effect of both pioglitazone and methotrexate on disease activity of rheumatoid arthritis in a biphasic study; experimental and clinical.Methods:Experimentally:...Full Text Available

333

Editing Antigen Presentation: Antigen Transfer between Human B Lymphocytes and Macrophages Mediated by Class A Scavenger Receptors1  

UK PubMed Central (United Kingdom)

B lymphocytes can function independently as efficient APCs. However, our previous studies demonstrate that both dendritic cells and macrophages are necessary to propagate immune responses initiated...Full Text Available

2008-09-15

334

EGFR Signaling Through an Akt-SREBP-1-Dependent, Rapamycin-Resistant Pathway Sensitizes Glioblastomas to Anti-Lipogenic Therapy  

UK PubMed Central (United Kingdom)

Glioblastoma, the most common malignant brain tumor, is among the most lethal and difficult cancers to treat. Although epidermal growth factor receptor (EGFR) mutations are frequent in glioblastoma,...Full Text Available

335

Dynamin-dependent NMDAR endocytosis during LTD and its dependence on synaptic state  

UK PubMed Central (United Kingdom)

BackgroundThe N-methyl-D-aspartate (NMDA)-type glutamate receptor expressed at excitatory glutamatergic synapses is required for learning and memory and is critical for normal brain...Full Text Available

336

Differential recognition of viral RNA by RIG-I  

UK PubMed Central (United Kingdom)

Retinoic acid inducible gene I (RIG-I) is a pattern recognition receptor (PRR) responsible for detection of nucleic acids from pathogens in the cytoplasm of infected cells and induction of type I interferon...Full Text Available

2011-03-01

337

DIFFERENTIAL EXPRESSION OF HPA AXIS HOMOLOG IN THE SKIN  

UK PubMed Central (United Kingdom)

SummaryHuman skin expresses elements of the hypothalamo-pituitary-adrenal (HPA) axis including pro-opiomelanocortin (POMC), corticotropin releasing hormone (CRH), the CRH receptor-1...Full Text Available

2007-02-01

338

Cytokinin-Dependent Photorespiration and the Protection of Photosynthesis during Water Deficit1[W][OA  

UK PubMed Central (United Kingdom)

We investigated the effects of PSARK∷IPT (for Senescence-Associated Receptor Kinase∷Isopentenyltransferase) expression and cytokinin production...Full Text Available

2009-07-01

339

Cyclophilin B Interacts with Sodium-Potassium ATPase and Is Required for Pump Activity in Proximal Tubule Cells of the Kidney  

UK PubMed Central (United Kingdom)

Cyclophilins (Cyps), the intracellular receptors for Cyclosporine A (CsA), are responsible for peptidyl-prolyl cis-trans isomerisation and for chaperoning several membrane proteins. Those functions...Full Text Available

340

Coevolution of activating and inhibitory receptors within mammalian carcinoembryonic antigen families  

UK PubMed Central (United Kingdom)

BackgroundMost rapidly evolving gene families are involved in immune responses and reproduction, two biological functions which have been assigned to the carcinoembryonic antigen...Full Text Available

341

Co-localization of Sorting Nexin 2 and Androgen Receptor in the Song System of Juvenile Zebra Finches  

UK PubMed Central (United Kingdom)

Mechanisms regulating sexual differentiation of the zebra finch song system appear to include both genetic and hormonal factors. Sorting Nexin 2 (SNX2), which is involved in trafficking proteins...Full Text Available

2010-07-09

342

Chimeric Antigen Receptor Therapy for B-cell Malignancies  

UK PubMed Central (United Kingdom)

We presented data showing that the CART-19 cells expressing the 4-1BB signaling domain can have unprecedented and massive in-vivo expansion, traffic to tumor sites, persist long term in vivo, and induce...Full Text Available

343

Characterization of Cytokinin and Adenine Transport in Arabidopsis Cell Cultures1[OA  

UK PubMed Central (United Kingdom)

Cytokinins are distributed through the vascular system and trigger responses of target cells via receptor-mediated signal transduction. Perception and transduction of the signal can occur at the plasma...Full Text Available

2008-12-01

344

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

UK PubMed Central (United Kingdom)

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

345

Catabolite Repression of the Citrate Fermentation Genes in Klebsiella pneumoniae: Evidence for Involvement of the Cyclic AMP Receptor Protein  

UK PubMed Central (United Kingdom)

Klebsiella pneumoniae is able to grow anaerobically with citrate as a sole carbon and energy source by a fermentative pathway involving the Na+-dependent citrate...Full Text Available

2001-09-01

346

Calcium/Calmodulin-Dependent Protein Kinase II Mediates Hippocampal Glutamatergic Plasticity During Benzodiazepine Withdrawal  

UK PubMed Central (United Kingdom)

Benzodiazepine withdrawal anxiety is associated with potentiation of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate receptor (AMPAR) currents in hippocampal CA1 pyramidal...Full Text Available

2010-08-01

347

Calcium, Vitamin D, VDR Genotypes, and Epigenetic and Genetic Changes in Rectal Tumors  

UK PubMed Central (United Kingdom)

Calcium, vitamin D, exposure to sunshine, and vitamin D receptor (VDR) genotypes have been associated rectal cancer. We used data from 750 rectal tumors and 1,205 population-based...Full Text Available

2010-05-01

348

CRF receptors in the nucleus accumbens modulate partner preference in prairie voles  

UK PubMed Central (United Kingdom)

Recent evidence suggests a role for corticotropin-releasing factor (CRF) in the regulation of pair bonding in prairie voles. We have previously shown that monogamous and non-monogamous vole...Full Text Available

2007-04-01

349

CD44 as a receptor for colonization of the pharynx by group A Streptococcus  

UK PubMed Central (United Kingdom)

The pharynx is the primary reservoir for strains of group A Streptococcus (GAS) associated both with pharyngitis (streptococcal sore throat) and with invasive or “flesh-eating”...Full Text Available

2000-10-15

350

Breast Cancer Stem-Like Cells Are Inhibited by a Non-Toxic Aryl Hydrocarbon Receptor Agonist  

UK PubMed Central (United Kingdom)

BackgroundCancer stem cells (CSCs) have increased resistance to cancer chemotherapy. They can be enriched as drug-surviving CSCs (D-CSCs) by growth with chemotherapeutic drugs, and/or...Full Text Available

351

Bacterial Particle Endocytosis by Epithelial Cells Is Selective and Enhanced by Tumor Necrosis Factor Receptor Ligands?  

UK PubMed Central (United Kingdom)

Bacterial pathogens use virulence strategies to invade epithelial barriers, but active processes of epithelial cells may also contribute to the endocytosis of microbial particles. To focus on the latter,...Full Text Available

2009-03-01

352

Atrial natriuretic peptide signal pathway upregulated in stomach of streptozotocin-induced diabetic mice  

UK PubMed Central (United Kingdom)

AIM: To investigate atrial natriuretic peptide (ANP) secretion from gastric mucosa and the relationship between the ANP/natriuretic peptide receptor type A (NPR-A) pathway and diabetic gastroparesis.METHODS:...Full Text Available

2010-01-07

353

Association Study of Serine Racemase Gene with Methamphetamine Psychosis  

UK PubMed Central (United Kingdom)

Experimental studies have demonstrated that not only dopaminergic signaling but also glutamatergic/NMDA receptor signaling play indispensable roles in the development of methamphetamine psychosis. Our...Full Text Available

2011-03-01

354

Antianxiety and antidepressant-like effects of AC-5216, a novel mitochondrial benzodiazepine receptor ligand  

UK PubMed Central (United Kingdom)

We investigated the ability of N-benzyl-N-ethyl-2-(7,8-dihydro-7-methyl-8-oxo-2-phenyl-9H-purin-9-yl)acetamide...Full Text Available

2004-08-01

355

Angiotensin II Promotes Development of the Renal Microcirculation through AT1 Receptors  

UK PubMed Central (United Kingdom)

Pharmacologic or genetic deletion of components of the renin-angiotensin system leads to postnatal kidney injury, but the roles of these components in kidney development are unknown. To test the hypothesis...Full Text Available

2010-03-01

356

Analysis of Protein Covalent Modification by Xenobiotics using a Covert Oxidatively Activated Tag  

UK PubMed Central (United Kingdom)

Numerous xenobiotics, including therapeutics agents, are substrates for bioactivation to electrophilic reactive intermediates that may covalently modify biomolecules. Selective estrogen receptor...Full Text Available

2005-09-01

357

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

UK PubMed Central (United Kingdom)

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

358

Activation of PPAR? induces profound multilocularization of adipocytes in adult mouse white adipose tissues  

UK PubMed Central (United Kingdom)

We sought to determine the effects of activation of peroxisome proliferator-activated receptor-γ (PPAR-γ) on multilocularization of adipocytes in adult white adipose tissue (WAT). Male...Full Text Available

2009-12-31

359

A novel role of the aryl hydrocarbon receptor (AhR) in centrosome amplification - implications for chemoprevention  

UK PubMed Central (United Kingdom)

BackgroundCentrosome aberrations can cause genomic instability and correlate with malignant progression in common human malignancies such as breast and prostate cancer. Deregulation...Full Text Available

360

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

UK PubMed Central (United Kingdom)

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

361

A homozygous P86S mutation of the human glucagon receptor is associated with hyperglucagonemia, ? cell hyperplasia, and islet cell tumor  

UK PubMed Central (United Kingdom)

ObjectiveThe goal of the study was to investigate the genetic and molecular basis of a novel syndrome of marked hyperglucagonemia and pancreatic α cell hyperplasia...Full Text Available

2009-11-01

362

A Comparison of intra-oral digital imaging modalities: Charged Couple Device versus Storage Phosphor Plate  

UK PubMed Central (United Kingdom)

BackgroundThis in vitro study was conducted to compare the accuracy of two digital image receptors in identifying the location of tip of a fine endodontic file and radiographic apex...Full Text Available

2010-11-01

363

Targeting a Ruthenium Complex to the Nucleus with Short Peptides  

UK PubMed Central (United Kingdom)

In an effort to develop octahedral metal complexes as chemotherapeutic and diagnostic agents targeted to DNA, it is critical to optimize the properties of their cellular uptake. Appending d-octaarginine...Full Text Available

2010-05-15

365

General Disclaimer One or more of the Following Statements may ...  

Science.gov (United States)

complexe sur paroi non-isotherme, LContri5ution to the Study thermal ... paroi chaude essentiellement non-isotherme, LVaporization in a Complex ...

366

Catalytic hydration of alkynes with platinum(II) complexes  

Energy Technology Data Exchange (ETDEWEB)

Platinum(II) complexes have been investigated in the hydration of alkynes. These catalysts offer improved regioselectivity over Hg(II) counterparts. 1 fig., 2 tabs.

1993-12-17

367

AN EVALUATION OF AN IMPORTANT ADVANCE IN ...  

Science.gov (United States)

... No. 52. Metal Complexes-I. Preparation and Physical Properties of Transition Metal Complexes of 6-Mercaptopurine and 4-Mercapto-6, 7-Diphenyl ...

1965-03-01

368

PPAR action in insulin resistance unraveled by metabolomics: potential clinical implications.  

Science.gov (United States)

ABSTRACT: Metabolomic analysis will provide the next large set of clues to further our understanding of human health and disease. A recent study has elucidated the significant differences in the metabolomes of adipocytes, serum and an adipocyte cell line after activation of two nuclear receptors, peroxisome proliferator activated receptor ?/? (PPAR?/?) and PPAR?. These findings hold great promise for explaining fundamental differences in the mechanisms of PPAR agonists and for identifying targets for the treatment of diabetes.See related research article: http://genomebiology.com/2011/12/8/R75. PMID:21861850

2011-08-23

369

Immunity and tolerance to infections in experimental hematopoietic transplantation  

British Library Electronic Table of Contents (United Kingdom)

Resistance and tolerance are two types of host defense mechanisms that increase fitness in response to fungi. Several genetic polymorphisms in pattern recognition receptors, most remarkably Toll-like receptors (TLRs), have been described to influence resistance and tolerance to aspergillosis in distinct clinical settings. TLRs on dendritic cells pivotally contribute in determining the balance between immunopathology and protective immunity to the fungus. Epithelial cells also contribute to this balance via selected TLRs converging on indoleamine-2,3-dioxygenase (IDO). Studies in experimental hematopoietic transplantation confirmed the dichotomy of pathways leading to resistance and tolerance to the fungus providing new insights on the relative contribution of the hematopoietic/nonhematopoi...

2011-01-01

370

Design of a new serotonin receptor 5-HT_1_A imaging agent based on "9"9"mTc  

International Nuclear Information System (INIS)

Serotonin is one of the neurotransmitters found in the brain and mediates brain functions. It is very well known that serotonin related brain abnormalities are exerted mainly via serotonin receptors in a similar manner to other neurotransmitters found in the brain. Recently, it has also been found that serotonin is involved in Alzheimer's disease either directly or indirectly by its actions on serotonergic neurons. To understand and treat the diseases caused by abnormalities in the serotonergic system in the brain, it is certain that its mechanism of function has to be well investigated. So far several 5-HT receptors and receptor subtypes have been well characterized. Moreover, serotonin agonists and antagonists acting on specific receptors are chemically synthesized and are now available for the prevention or treatment of serotonergic related diseases. In recent years, a great demand for developing ...

2004-07-01

371

A case study of trastuzumab treatment for metastatic breast cancer in pregnancy: fetal risks and management of cerebral metastases  

British Library Electronic Table of Contents (United Kingdom)

Trastuzumab increases survival amongst women with human epidermal growth factor receptor (HER)-2 receptor positive metastatic breast cancer, but maternal and fetal risks are associated with advanced disease and its treatment in pregnancy. We present a case of a primigravid with HER-2 positive metastatic breast cancer who received trastuzumab throughout pregnancy. She presented with cerebral metastases, requiring surgical decompression and resection. Reversible oligohydramnios developed during pregnancy. Fetal safety data on trastuzumab in pregnancy is limited, but case reports suggest a recurring pattern of (mostly reversible) oligohydramnios.

2011-01-01

372

[New cardiotonic agents].  

Science.gov (United States)

The possibilities for therapy in the field of severe cardiac insufficiency have been extended in recent years by the introduction of novel agents endowed with a positive inotropic action. These substances may be arranged in two large classes: sympathomimetic agents and "non sympathomimetic--non digitalis-like" inotropic agents. The stimulant action of noradrenaline, adrenaline and isoproterenol on beta-adrenergic myocardial receptors has been clearly demonstrated but the usefulness of these medicines is limited by their positive chronotropic and arrhythmogenic actions. Dopamine and dobutamine have proved to be very useful in the treatment of patients in intensive care units. However, the exclusively intravenous route of administration limits their importance to the medium or long term. Several compounds, which are active by the oral route, have been the subject of therapeutic trials for the short or medium term. The problems posed by their use result, in the first ...

1985-12-01

373

Localisation of the neuropeptide PACAP and its receptors in the rat parathyroid and thyroid glands.  

Science.gov (United States)

PACAP (pituitary adenylate cyclase activating polypeptide) is widely distributed neuropeptide acting via three subtypes of receptors, PAC(1), VPAC(1) and VPAC(2). Here we examined the localisation and nature of PACAP-immunoreactive nerves in the rat thyroid and parathyroid glands and defined the distribution of PAC(1), VPAC(1) and VPAC(2) receptor mRNA's. In the parathyroid gland a large number of nerve fibres displaying PACAP-immunoreactivity were distributed beneath the capsule, around blood vessels and close to glandular cells. Most of the PACAP-nerves were sensory, since they co-stored CGRP (calcitonin-gene-related peptide) and were sensitive to capsaicin-treatment. mRNA's for PAC(1) and VPAC(2) receptors occurred in the parathyroid gland, mainly located in the glandular cells. In the thyroid gland PACAP-immunoreactive nerve fibres were associated with blood vessels, thyroid follicles and parafollicular C-cells. A high ...

2010-12-19

374

Cloning of the cDNA for the human. beta. /sub 1/-adrenergic receptor  

Energy Technology Data Exchange (ETDEWEB)

Screening of a human placenta lambdagt11 library has led to the isolation of the cDNA for the human ..beta../sub 1/-adrenergic receptor (..beta../sub 1/AR). Used as the probe was the human genomic clone termed G-21. This clone, which contains an intronless gene for a putative receptor, was previously isolated by virtue of its cross hybridization with the human ..beta../sub 2/-adrenergic receptor (..beta../sub 2/AR). The 2.4-kilobase cDNA for the human ..beta../sub 1/AR encodes a protein of 477 amino acid residues that is 69% homologous with the avian ..beta..AR but only 54% homologous with the human ..beta../sub 2/AR. This suggests that the avian gene encoding ..beta..AR and the human gene encoding ..beta../sub 1/AR evolved from a common ancestral gene. RNA blot analysis indicates a message of 2.5 kilobases in rat tissues, with a pattern of tissue distribution consistent with ..beta../sub 1/AR binding. This pattern is quite ...

1987-11-01

379

The complexities of skeletal biology  

Science.gov (United States)

For a long time, the skeleton was seen as an amorphous tissue of little biological interest. But

2003-01-01

381

Radionuclides Migration Prevention  

International Science & Technology Center (ISTC)

Prevention of Radionuclide Migration from the Soil of Semipalatinsk Nuclear Test Site by Using of Interpolymer Complexes

382

Preparation of radioactive lead complexes utilizing Chelex methodology  

Energy Technology Data Exchange (ETDEWEB)

The use of Chelex resin for the synthesis of radioactive lead complexes has been explored. The process involved immobilization of {sup 203}Pb on the resin and subsequent elution of complexed lead by chelating agents. {sup 203}Pb complexes derived from meso- and racemic dimercaptosuccinic acid (meso-DMSA, rac-DMSA) were prepared and assessed for stability in vitro.

1996-11-01

383

Preparation of radioactive lead complexes utilizing Chelex methodology  

International Nuclear Information System (INIS)

The use of Chelex resin for the synthesis of radioactive lead complexes has been explored. The process involved immobilization of "2"0"3Pb on the resin and subsequent elution of complexed lead by chelating agents. "2"0"3Pb complexes derived from meso- and racemic dimercaptosuccinic acid (meso-DMSA, rac-DMSA) were prepared and assessed for stability in vitro.

1996-11-01

384

Permutation Complexity Related to the Letter Doubling Map  

CERN Document Server

Given a countable set X (usually taken to be the natural numbers or integers), an infinite permutation, \\pi, of X is a linear ordering of X. This paper investigates the combinatorial complexity of infinite permutations on the natural numbers associated with the image of uniformly recurrent aperiodic binary words under the letter doubling map. An upper bound for the complexity is found for general words, and a formula for the complexity is established for the Sturmian words and the Thue-Morse word.

2011-01-01

385

Organic electronic conductors and precursors. Pt. 15. Novel dithiolene-nickel complexes based on benzenehexathiolate derivatives  

Energy Technology Data Exchange (ETDEWEB)

Dithiolato-nickel complexes with multisulfur ligands derived from benzenehexathiolate have been synthesized. The properties of the monomeric and polymeric complexes have been characterized by ESR spectroscopic and magnetochemical data and by electrical conductivity measurements. The prepared complexes are paramagnetic and have characteristic absorptions between 800 and 1000 nm. (orig.).

1992-04-01

387

Mo"5 and W"5 complexing with tri-tret-butyl phenyl ether of 1.2-naphthoquinonediazide-(2)-5-sulfochloride  

International Nuclear Information System (INIS)

The complexing of paramagnetic salts of molybdenum and tungsten with tri-tert-butylphenyl ester of 1,2-naphthoquinone-diazide-(2)-5-sulfochloride is studied by PMR and EPR methods. From the changes of half-widths of lines in PMR spectra and analysis of g-factor in EPR spectra, the kinetic and thermodynamic parameters of the complexing are determined, and the composition of the complexes formed is established, and the schemes of their formation are suggested.

389

Fluorescent Silicate Materials for the Detection of Paraoxon  

Science.gov (United States)

... significantly lower limits of detection. The complex fluorescence spectra of these constructs indicated that only a portion ...

2010-03-19

394
395

Complex Abdominal Wall Repair  

Medline Plus

... presentation will be archived on the OR-Live website. 00:46:02 ANNOUNCER: This has been a ...

396

Calculation of some energetic parameters of astatine compounds  

International Nuclear Information System (INIS)

... astatine complexes astatine compounds coulomb energy effective charge

400

,>22u  

Science.gov (United States)

(Watkins and. Corbett,. 1964) which is a phosphorous-vacancy complex, i.e., ...... Grover. 1965. Semiconductor. Surfaces. ...

401

Palladium polypyridyl complexes: synthesis, characterization, DNA interaction and biological activity on Leishmania (L.) mexicana  

Energy Technology Data Exchange (ETDEWEB)

This paper describes the search for new potential chemotherapeutic agents based on transition metal complexes with planar ligands. In this study, palladium polypyridyl complexes were synthesized and characterized by elemental analysis, NMR, UV-VIS and IR spectroscopies. The interaction of the complexes with DNA was also investigated by spectroscopic methods. All metal-to-ligand charge transfer (MLCT) bands of the palladium polypyridyl complexes exhibited hypochromism and red shift in the presence of DNA. The binding constant and viscosity data suggested that the complexes [PdCl{sub 2}(phen)] and [PdCl{sub 2}(phendiamine)] interact with DNA by electrostatic forces. Additionally, these complexes induced an important leishmanistatic effect on L. (L.) mexicana promastigotes at the final concentration of 10 {mu}mol L{sup -1} in 48 h. (author)

2008-07-01

402

Behavior of Np(VII, VI, V) in Silicate Solutions  

Energy Technology Data Exchange (ETDEWEB)

Spectrophotometric methods were used to investigate the properties of neptunium(VII), (VI), and (V) in silicate solution. The transition of cationic neptunium(VII) to anionic species in non-complexing environments proceeds in the range of ?? 5.5 to 7.5. In the presence of carbonate, this transition occurs at ?? 10.0 to 11.5 and in silicate solutions at ?? 10.5-12.0. These findings show that cationic neptunium(VII) forms complexes with both carbonate and silicate and that the silicate complex is stronger than that of the carbonate. The competition of complex formation reactions for neptunium(VI) with carbonate and silicate and on the known complex stability constant of NpO2(CO3)34- allowed the NpO2SiO3 complex stability constant, log ? = 16.5, to be estimated. Determination of the formation constant of Np(V) complexes with SiO32- was not ...

2004-11-30

403

Achieving a vanishing SNR-gap to exact lattice decoding at a subexponential complexity  

CERN Document Server

The work identifies the first lattice decoding solution that achieves, in the general outage-limited MIMO setting and in the high-rate and high-SNR limit, both a vanishing gap to the error-performance of the (DMT optimal) exact solution of preprocessed lattice decoding, as well as a computational complexity that is subexponential in the number of codeword bits. The proposed solution employs lattice reduction (LR)-aided regularized (lattice) sphere decoding and proper timeout policies. These performance and complexity guarantees hold for most MIMO scenarios, all reasonable fading statistics, all channel dimensions and all full-rate lattice codes. In sharp contrast to the above manageable complexity, the complexity of other standard preprocessed lattice decoding solutions is shown here to be extremely high. Specifically the work is first to quantify the complexity of these lattice ...

2011-01-01

404

Developments of PET radioligands for NMDA receptors  

International Nuclear Information System (INIS)

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 cerebral cortex than ...

2002-09-01

405

Redox reactions of Cu(II)-amine complexes in aqueous solutions  

Energy Technology Data Exchange (ETDEWEB)

A number of amines can be employed for all volatile treatment (AVT) of steam generator (SG) systems of nuclear power reactors. These amines form complexes with Cu{sup 2+} and Ni{sup 2+} ions which come into water due to corrosion. The redox reactions of a number of Cu(II)-AVT amine complexes and the stability of the transient species formed have been studied by pulse radiolysis technique. Rate constants for the reaction of e{sub aq}{sup -} with a number of Cu(II)-amine complexes have been determined by following the decay of e{sub aq}{sup -} absorption. Stability of Cu(I)-amine complexes was studied by following the kinetics of the bleaching signal formed at the {lambda}{sub max} of the Cu(II) amine complex. Except for Cu(I)-triethanolamine complex all other Cu(I)-amine complexes were found to be stable. One-electron oxidation of Cu(II) ...

2003-03-01

406

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

Energy Technology Data Exchange (ETDEWEB)

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 ...

1992-01-25

407

The effect of phosphonic acid substituents on europium(III) complex stability in acidic solutions  

Science.gov (United States)

The thermodynamics of protonation and europium(III) complex formation with substituted methane diphosphonic acids have been reported recently. These ligands form strong complexes with europium in moderately acidic solutions ((H{sup +}) {ge} 0.1 M), conditions not conducive to complexation by most carboxylate and aminopolycarboxylate ligands. A correlation of log {beta} vs pK{sub a} values for phosphonate and carboxylate ligands is used to explore the effect of ligand structure on complex stability. 5 refs., 1 fig.

1990-01-01

408

Mechanism of the metal-mediated carbalkoxylation of vinyl electrophiles. 1. Preparation, molecular structure, and alcoholysis of vinylic acyl platinum(II) complexes  

Energy Technology Data Exchange (ETDEWEB)

Carbalkoxylation of vinyl electrophiles was investigated using platinum complexes. This reaction occurs in two steps: (a) carbonyl insertion of {sigma}-vinyl Pt(II) halides and (b) alcoholysis of vinylic acyl Pt(II) complexes. Alcoholysis of vinylic acyl Pt(II) triflate complexes is investigated kinetically. Vinylic acyl Pt(II) complexes were isolated and characterized. 51 refs., 5 figs., 6 tabs.

1992-03-01

409

Investigation of formation of Sn-PM tetracycline and Sn-PM-tetracycline-_9_9Tc complexes  

International Nuclear Information System (INIS)

The formation and stability constants of the [sup(99m)Tc]PM tetracycline have been investigated by the potentiometric method. The pK value of the complex formed was measured as pK = 5.49 +- 0.19. The spectrophotometric study has been performed on the formation of a complex of Sn(II) and TcO"4"- in the presence of PM Tetracycline. This study shows that Sn(II) forms with PMT a complex at a mole ratio of 1:1. The molar extinction coefficients of the Sn-PMT and [_9_9Tc]PMT complexes have been measured. (author).

1983-01-01

410

First investigations of complex formation of At(I) with phosphorous organic compounds  

Energy Technology Data Exchange (ETDEWEB)

Reaction of At(I) with triphenylphosphine, triethylphosphite and tri-n-octylphosphine oxide was investigated in ethanolic solution by means of electromigration. A cationic complex with triphenylphosphine was identified being stable at pH = 1,9 in the concentration range of the ligand between c = 10{sup -5} to 10{sup -3} M. At a higher ligand concentration and at pH>2, the reduction effect of phosphine is superimposed on the complex formation. Complex formation is confirmed by ligand exchange reactions with Br{sup -} and I{sup -}. A comparatively weak complex is formed by triethylphosphite and At(I). No compound is formed by tri-n-octylphosphine oxide and At(I). (orig.).

1989-01-01

411

First investigations of complex formation of At(I) with phosphorous organic compounds  

International Nuclear Information System (INIS)

Reaction of At(I) with triphenylphosphine, triethylphosphite and tri-n-octylphosphine oxide was investigated in ethanolic solution by means of electromigration. A cationic complex with triphenylphosphine was identified being stable at pH = 1,9 in the concentration range of the ligand between c = 10"-"5 to 10"-"3 M. At a higher ligand concentration and at pH>2, the reduction effect of phosphine is superimposed on the complex formation. Complex formation is confirmed by ligand exchange reactions with Br"- and I"-. A comparatively weak complex is formed by triethylphosphite and At(I). No compound is formed by tri-n-octylphosphine oxide and At(I). (orig.).

412

Aluminium, gallium and indium complexing with methylthymol blue  

International Nuclear Information System (INIS)

Al, Ga and In complexing with methylthymol blue (H_6R) purified by gel filtration is studied. in the case of metal excess complexes with the ratio of components M:H_6R=2:1 with #lambda#=587(Al), 590(Ga) and 593 nm(In) appear. In the case of reacting agent excess complexes with the ratio of component 1:1 with #lambda#_m_a_x=480-490 (Al) and 480 nm(Ga, In) appear. The mechanism of complexing reactions is studied. Molar extinction coefficients and stability constants are calculated.

1988-01-01

413

cap alpha. -2 adrenergic receptor: a radiohistochemical study  

Energy Technology Data Exchange (ETDEWEB)

..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 ...

1984-01-01

414

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

International Nuclear Information System (INIS)

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

415

Humic substances in natural waters and their complexation with trace metals and radionuclides: a review. [129 references  

Energy Technology Data Exchange (ETDEWEB)

Dissolved humic substances (humic and fulvic acids) occur in surface waters and groundwaters in concentrations ranging from less than 1 mg(C)/L to more than 100 mg(C)/L. Humic substances are strong complexing agents for many trace metals in the environment and are also capable of forming stable soluble complexes or chelates with radionuclides. Concentrations of humic materials as low as 1 mg(C)/L can produce a detectable increase in the mobility of some actinide elements by forming soluble complexes that inhibit sorption of the radionuclides onto rock materials. The stability of trace metal- or radionuclide-organic complexes is commonly measured by an empirically determined conditional stability constant (K'), which is based on the ratio of complexed metal (radionuclide) in solution to the product concentration of uncomplexed metal and humic complexant. ...

1985-07-01

416

Visualization of growth factor receptor sites in rat forebrain  

International Nuclear Information System (INIS)

It is now known that various growth factors may also act in the central nervous system. Among them, it has recently been shown that epidermal growth factor (EGF) and insulin-like growth factor I (IGF-I) may possess trophic effects in the mammalian brain. We report here on the respective autoradiographic distribution of ["1"2"5I]EGF and ["1"2"5I]IGF-I receptor binding sites in the rat brain, both during ontogeny and in adulthood. It appears that ["1"2"5I]EGF sites are mostly found in the rat forebrain during brain development. On the other hand, ["1"2"5I]IGF-I sites are more widely distributed both during ontogeny and in adulthood. These results reveal the plasticity of the expression of EGF and IGF-I receptor sites in the mammalian brain. This could be relevant for the respective role of these two growth factors in the development and maintenance of neuronal function.

417

The synthesis of (1',3'- sup 3 H)4-(4'-azido-5',6',7',8'-tetrahydro-5',5',8',8'-tetramethyl -2'-anthracenyl)benzoic acid as a probe of the retinoic acid receptor  

Energy Technology Data Exchange (ETDEWEB)

The synthesis of (1',3'-{sup 3}H)4-(4'-azido-5',6',7',8'-tetrahydro-5'5'8',8'-tetramethyl-2'-anthracenyl)benzoic acid is described. This retinoid was designed as a photoaffinity probe of the receptor sites of cellular retinoic acid-binding protein and the nuclear retinoic acid receptor protein. The ({sup 3}H)azidoretinoid was prepared from 1,2,3,4-tetrahydro-1,1,4,4-tetra-methyl-7-(4-methylphenyl)-5-nitroanthracene in five steps in 15% yield (89% radiochemical purity by HPLC). {sup 1}H and {sup 3}H NMR was used to confirm the sites of {sup 3}H substitution on the ring. (author).

1990-01-01

418

Radiopharmaceuticals for the imaging of functional abnormalities of the developing brain  

International Nuclear Information System (INIS)

The measurement of physiological parameters in man is possible with the help of positron emission tomography (PET) and radiopharmaceuticals labeled with short lived positron emitters as C 11, N 13, O 15 and F 18. With the use of this substances it is possible to make a tomographic map defining regional metabolic parameters in normal and diseased brain. This technique has therefore also be named 'in vivo autoradiography'. The possibility of applying C 11 or F 18 labeled deoxyglucose with PET for detecting regional and local changes in cerebral metabolic rate of glucose in brain development in children of 5 days to 1 year of age is discussed. Beyond this a relationship between cerebral metabolic rate of glucose, cerebral blood flow and cerebral metabolic rate of oxygen by use of this technique after inhalation of O 15 and C 11-labeled CO_2 is shown. Attention is drawn to the application of C 11-methyl-spiperone and PET to visualize dopamine receptor density in the ...

419

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

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

420

Natriuretic peptides in the pathophysiology of congestive heart failure.  

Science.gov (United States)

A hallmark of congestive heart failure (CHF) is the activation of the cardiac endocrine system, in particular atrial natriuretic peptide (ANP) and brain natriuretic peptide (BNP). The natriuretic peptides are a group of structurally similar but genetically distinct peptides that have diverse actions in cardiovascular, renal, and endocrine homeostasis. ANP and BNP are of myocardial cell origin and C-type natriuretic peptide (CNP) is of endothelial origin. ANP and BNP bind to the natriuretic peptide-A receptor (NPR-A), which, via 3',5'-cyclic guanosine monophosphate (cGMP), mediates natriuresis, vasodilatation, renin inhibition, antimitogenesis, and lusitropic properties. CNP lacks natriuretic actions but possesses vasodilating and growth inhibiting actions via the guanylyl cyclase-linked natriuretic peptide-B receptor. All three peptides are cleared by the natriuretic peptide-C receptor and degraded by the ectoenzyme neutral ...

2000-05-01

421

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

Energy Technology Data Exchange (ETDEWEB)

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 imaging. The ...

1990-01-01

422

Cloning and mapping of the mouse {alpha}7-neuronal nicotinic acetylcholine receptor  

Energy Technology Data Exchange (ETDEWEB)

We report the isolation of cDNA clones for the mouse {alpha}7 neuronal nicotinic acetylcholine receptor subunit (gene symbol Acra7), the only nicotinic receptor subunit known to bind a-bungarotoxin in mammalian brain. This gene may have relevance to nicotine sensitivity and to some electrophysiologic findings in schizophrenia. The mouse {alpha}7 subunit gene encodes a protein of 502 amino acids with substantial identity to the rat (99.6%), human (92.8%), and chicken (87.5%) amino acid sequences. The {alpha}7 gene was mapped to mouse chromosome 7 near the p locus with the following gene order from proximal to distal: Myod1-3.5 {+-}1.7 cM-Gas2-0.9 cM {+-} 0.9 cM-D7Mit70-1.8 {+-} 1.2 cM- Acra7-4.4 {+-}1.0 cM-Hras1-ps11/Igf1r/Snrp2a. The human gene was confirmed to map to the homologous region of human chromosome 15q13-q14. 26 refs., 3 figs.

1995-03-20

423

Atrial natriuretic peptide receptor heterogeneity and effects on cyclic GMP accumulation  

Energy Technology Data Exchange (ETDEWEB)

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 sites. Most of the ANP-binding sites in cultured cells have a ...

1988-01-01

424

Assessment of epidermal growth factor receptor (EGFR, ErbB1) and HER2 (ErbB2) protein expression levels and response to lapatinib (Tykerb, GW572016) in an expanded panel of human normal and tumour cell lines  

British Library Electronic Table of Contents (United Kingdom)

Abstract. Objective: Lapatinib (Tykerb, GW572016), a potent inhibitor of the catalytic activities of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) (ErbB2), inhibits population growth of selected EGFR and HER2 overexpressing cell lines. Previous studies with a small number of cell lines suggest a correlation between overexpression of EGFR and/or HER2 and sensitivity to growth inhibition by lapatinib; however, the precise determinants of lapatinib selectivity for tumour and/or other cells remain unclear. Materials and methods: To clarify the determinants of its selectivity in cultured cells, lapatinib-induced cell population growth inhibition and relative EGFR and HER2 protein expression were quantified in 61 different human tumour cell lines fro...

2007-01-01

425

An FGF1:FGF2 chimeric growth factor exhibits universal FGF receptor specificity, enhanced stability and augmented activity useful for epithelial proliferation and radioprotection  

British Library Electronic Table of Contents (United Kingdom)

Structural instability of wild-type fibroblast growth factor (FGF)-1 and its dependence on exogenous heparin for optimal activity diminishes its potential utility as a therapeutic agent. Here we evaluated FGFC, an FGF1:FGF2 chimeric protein, for its receptor affinity, absolute heparin-dependence, stability and potential clinical applicability. Using BaF3 transfectants overexpressing each FGF receptor (FGFR) subtype, we found that, like FGF1, FGFC activates all of the FGFR subtypes (i.e., FGFR1c, FGFR1b, FGFR2c, FGFR2b, FGFR3c, FGFR3b and FGFR4) in the presence of heparin. Moreover, FGFC activates FGFRs even in the absence of heparin. FGFC stimulated keratinocytes proliferation much more strongly than FGF2, as would be expected from its ability to activate FGFR2b. FGFC showed greater struct...

2008-01-01

426

The phosphate complexation of neptunium(V)  

International Nuclear Information System (INIS)

The phosphate complexation of Np(V) is investigated in the pH range from 6.4 to 10.0 in 0.1 M NaClO_4 at 22#+-#2 C by absorption spectroscopy. The formation of two phosphate complexes is confirmed by spectroscopic speciation: NpO_2HPO"-_4 at 988.8 nm and NpO_2PO"2"-_4 at 993.6 nm with molar extinction coefficients of 251#+-#8 and 201#+-#11 1/mol cm, respectively. The complexation constants are determined to be log #beta# = 2.54#+-#0.02 for NpO_2HPO"-_4 and log #beta# = 6.33#+-#0.08 for NpO_2PO"2"-_4. The competition of the phosphate complexation with the carbonate complexation is demonstrated by speciation calculation under different geochemical conditions. (orig.).

1996-01-01

427

Relating Complex Fluid Composition and Thermophysical Properties with the Advanced Distillation Curve Approach  

British Library Electronic Table of Contents (United Kingdom)

Complex fluids have long posed a significant challenge in our ability to characterize and model fluid properties. Here, we consider complex fluids to be mixtures with many components that can differ significantly in polarity and polarizability. The penultimate complex fluid is crude oil, although many other fluids such as finished fuels are also highly complex. We have recently introduced a measurement strategy that can simplify these efforts and provides the added potential of linking chemical composition (i.e. analytical) information with physical property information. In addition to chemical characterization, the approach provides the ability to calculate thermodynamic and transport properties for such complex heterogeneous streams. The technique is based on the advanced distillation cu...

2010-01-01

428

A variable gene delivery carrier-biotinylated chitosan/polyethyleneimine  

International Nuclear Information System (INIS)

A variable gene delivery system has been developed based on conjugating chitosan to biotin through a functionalized poly(ethylene glycol) (PEG) spacer, which can be used to further bind different molecules on the outer layer of a polymer/DNA complex by streptavidin (SA)-biotin linkage. In this study, TAT-conjugated SA was used as the model molecule to prove the conjugation function of the prepared complex. In addition, low-molecular-weight poly(ethyleneimine) (PEI) was added into the polymer/DNA complex to increase the transfection efficiency. The results of the luciferase assay show that the transfection efficiency of the prepared complex was significantly correlated with the amount of PEI and was further enhanced when TAT was conjugated to the complex by SA-biotin linkage. Considered to have negligible cytotoxic effects, the variable gene delivery complex ...

2010-12-01

429

Toll-like receptor 2 polymorphism and gram-positive bacterial infections after liver transplantation  

British Library Electronic Table of Contents (United Kingdom)

Abstract Toll-like receptor 2 (TLR2) is an immune sensor for gram-positive bacterial cell wall components. Single-nucleotide polymorphisms (SNPs) in the TLR2 gene that impair its function may, therefore, influence the risk and outcomes of gram-positive bacterial infections. In a cohort of 694 liver transplant recipients, we assessed the TLR2 SNP that is translated into an amino acid substitution of arginine for glutamine at position 753 (R753Q), and we found that its presence was associated with the clinical characteristics and outcomes of gram-positive bacterial infections. The proportions of patients with the TLR2 R753Q SNP did not significantly differ between those with gram-positive bacterial infections and those without gram-positive bacterial infections (9.6% versus 9.6%, P = 0.999)....

2011-01-01

430

The use of healthy volunteers instead of patients to inform drug dosing studies: a [11C]raclopride PET study  

British Library Electronic Table of Contents (United Kingdom)

Rationale Receptor occupancy study has been performed to evaluate pharmacokinetic profiles in new antipsychotic drug development. While these findings highlight the value of positron emission tomography (PET) for dose-finding study, what is unclear is if it is necessary to conduct these studies in patients with schizophrenia or whether studies in healthy volunteers are adequate. Objectives To determine if it is necessary to conduct dopamine receptor occupancy studies in patients with schizophrenia or whether studies in healthy volunteers are adequate for dose-finding study, we compared the concentration?occupancy relationship in terms of EC50 between patients and healthy volunteers. Methods Ten healthy volunteers and eight patients with schizophrenia participated in the study. We measured ...

2011-01-01

431

Targeting the nicotinic alpha7 acetylcholine receptor to enhance cognition in disease  

British Library Electronic Table of Contents (United Kingdom)

A promising drug target currently under investigation to improve cognitive deficits in neuropsychiatric and neurological disorders is the neuronal nicotinic alpha7 acetylcholine receptor (a7nAChR). Improving cognitive impairments in diseases such as Alzheimer's (AD) and schizophrenia remains a large unmet medical need, and the a7nAChR has many properties that make it an attractive therapeutic target. The a7nAChR is a ligand gated ion channel that has particularly high permeability to Ca^2^+ and is expressed in key brain regions involved in cognitive processes (e.g., hippocampus). The a7nAChRs are localized both pre-synaptically, where they can regulate neurotransmitter release, and post-synaptically where they can activate intracellular signaling cascades and influence downstream processes...

2011-01-01

432

Spermatozoa of Sharpsnout sea bream (Diplodus puntazzo) and European sea bass (Dicentrarchus labrax) express opioid receptors  

British Library Electronic Table of Contents (United Kingdom)

Endogenous opioid peptides (EOP) are molecules affecting many biological functions influencing productive and reproductive performance. They increase in stress conditions and interact with specific opioidergic receptors (OR): delta, kappa and mu. Several studies in other animal species suggest that they can also affect sperm cell motility. In fish the ionic external environment modulates the increase of intracellular calcium ion that is required to activate sperm motility after spawning. In mammals OR are functionally associated to calcium channels and in fishes calcium is highly required for fish sperm activation. In this study the presence of OR on spermatozoa of two Perciform fish, the sharpsnout seabream (Diplodus puntazzo, family Sparidae) and the European sea bass (Dicentrarchus labr...

2010-01-01

433

Role of death receptor, mitochondrial and endoplasmic reticulum pathways in different stages of degenerative human lumbar disc  

British Library Electronic Table of Contents (United Kingdom)

Intervertebral disc (IVD) cell apoptosis has been suggested to play an important role in promoting the degeneration process. It has been demonstrated that IVD cell apoptosis occurs through either death receptor, mitochondrial or endoplasmic reticulum (ER) pathway. Our study aimed to explore the relationship among these three pathways and grade of IVD degeneration (IVDD). IVDs were collected from patients with lumbar fracture, vertebral tumor, disc herniation or spondylolisthesis. IVDs were distinguished by MRI and histomorphological examination, cell apoptosis was detected by TUNEL staining. Biomarkers of these three apoptosis pathways were detected by RT-PCR and Western blot. Furthermore, the correlation between apoptosis pathways biomarkers and disc pathology were analyzed. Nucleus pulpo...

2011-01-01

434

Role of Fgf receptor 2c in adipocyte hypertrophy in mesenteric white adipose tissue  

British Library Electronic Table of Contents (United Kingdom)

Fgf receptor 2c (Fgfr2c) was expressed in mature adipocytes of mouse white adipose tissue (WAT). To examine the role of Fgfr2c in mature adipocytes, we generated adipocyte-specific Fgfr2 knockout (Fgfr2 CKO) mice. The hypertrophy impairment of adipocytes in the mesenteric WAT but not in the subcutaneous WAT and decreased plasma free fatty acid (FFA) levels were observed in Fgfr2 CKO mice. Although the expression of genes involved in adipocyte differentiation and lipid metabolism in the mesenteric WAT was essentially unchanged, the expression of uncoupling protein 2 potentially involved in energy dissipation was significantly increased. Among potential Fgf ligands for Fgfr2c, Fgf9 was preferentially expressed in the mesenteric WAT. The present findings indicate that Fgfr2c potentially activ...

2008-01-01

435

Research update: Alpha7 nicotinic acetylcholine receptor mechanisms in Alzheimer's disease  

British Library Electronic Table of Contents (United Kingdom)

Aberrant amyloid-b peptide (Ab) accumulation along with altered expression and function of nicotinic acetylcholine receptors (nAChRs) stand prominently in the etiology of Alzheimer's disease (AD). Since the discovery that Ab is bound to a7 nAChRs under many experimental settings, including post-mortem AD brain, much effort has been expended to understand the implications of this interaction in the disease milieu. This research update will review the current literature on the a7 nAChR-Ab interaction in vitro and in vivo, the functional consequences of this interaction from sub-cellular to cognitive levels, and discuss the implications these relationships might have for AD therapies.

2011-01-01

436

Regulation of C-type natriuretic peptide expression  

British Library Electronic Table of Contents (United Kingdom)

C-type natriuretic peptide (CNP) is a member of the small family of natriuretic peptides that also includes atrial natriuretic peptide (ANP) and brain, or B-type natriuretic peptide (BNP). Unlike them, it performs its major functions in an autocrine or paracrine manner. Those functions, mediated through binding to the membrane guanylyl cyclase natriuretic peptide receptor B (NPR-B), or by signaling through the non-enzyme natriuretic peptide receptor C (NPR-C), include the regulation of endochondral ossification, reproduction, nervous system development, and the maintenance of cardiovascular health. To date, the regulation of CNP gene expression has not received the attention that has been paid to regulation of the ANP and BNP genes. CNP expression in vitro is regulated by TGF-b and recepto...

2011-01-01

437

Novel photoaffinity ligands for the GA-receptor  

Energy Technology Data Exchange (ETDEWEB)

Previous studies from this laboratory have shown that certain N-substituted phthalimides (NSPs) exhibit GA-like activity in a range of specific bioassays and that bioactive NSPs compete with ({sup 3}H)-GA{sub 4} for soluble binding sites in cucumber homogenates. As such, these compounds may prove useful in the purification and characterization of GA receptor proteins. To this end, five azido-NSPs have been synthesized and are currently being screened for biological activity and photochemical stability. Three azido-NSPs elicit {alpha}-amylase production in barley half-seeds and stimulate tissue elongation in d{sub 5} maize, lettuce, sunflower, and soybean. Further evaluations are in progress and these data as well as the utility of these compounds as photo-affinity ligands will be discussed.

1990-05-01

438

Immunohistochemical detection of epidermal growth factor receptor in radiation-induced lung tumors in Beagle dogs  

International Nuclear Information System (INIS)

Increased levels of epidermal growth factor receptor have been reported in a variety of tumors, including pulmonary squamous cell carcinomas in man. The purpose of this study was to determine if increased levels of epidermal growth factor (EGFR) were present in lung tumors from Beagle dogs that had been exposed to "2"3"9PuO_2- Using immunohistochemical techniques, sections from 17 lung tumors were examined for the presence of EGFR. Seven of the tumors were strongly positive for EGFR; the remainder of the tumors and the normal lung sections were negative. The positive immunostaining could not be correlated with the histologic phenotype of the tumors. Work is in progress to determine the level of EGFR in preneoplastic, proliferative epithelial foci in the Iung. (author)

1988-12-01

439

Hypomethylation and induction of retinoic acid receptor beta 2 by concurrent action of adenosine analogues and natural compounds in breast cancer cells  

British Library Electronic Table of Contents (United Kingdom)

DNA methylation is considered as a potential cause of aberrations in regulation of gene expression during carcinogenesis. Therefore, changes in DNA methylation patterns may be targets for chemoprevention. In the present study, we investigated effects of all-trans retinoic acid (ATRA), vitamin D3, and resveratrol alone and in combination with adenosine analogues: 2-chloro-2'-deoxyadenosine (2CdA) and 9-beta-d-arabinosyl-2-fluoroadenine (F-ara-A), on methylation and expression of retinoic acid receptor beta 2 (RARbeta2) in MCF-7 and MDA-MB-231 breast cancer cell lines. Alterations in methylation and expression levels after treatment of cells with the tested compounds were evaluated by methylation-sensitive restriction analysis (MSRA) and real-time PCR, respectively. RARbeta2 promoter in the ...

2010-01-01

440

Human type I pituitary adenylate cyclase activating polypeptide receptor (ADCYAP1R): Localization to chromosome band 7p14 and integration into the cytogenetic, physical, and genetic map of chromosome 7  

Energy Technology Data Exchange (ETDEWEB)

The gene encoding the human type I pituitary adenylate cyclase activating polypeptide receptor (ADCYAP1R1) was mapped to chromosome 7 by PCR analysis of genomic DNA from a human/rodent somatic cell hybrid mapping panel. This assignment was confirmed and the gene localized to chromosome band 7p14 by fluorescence in situ hybridization. A yeast artificial chromosome containing ADCYAP1R1 was identified in the CEPH {open_quotes}B{close_quotes} Mega-YAC library. This YAC includes two highly polymorphic dinucleotide repeat sequences that will facilitate genetic studies of the contribution of ADCYAP1R1 in disease states of the central nervous and neuroendocrine systems. 13 refs., 1 fig.

1994-10-01

441

Human and rat mast cell high-affinity immunoglobulin E receptors: Characterization of putative. alpha. -chain gene products  

Energy Technology Data Exchange (ETDEWEB)

The authors have cloned and determined the entire nucleotide sequence of cDNAs corresponding to the putative {alpha} subunits of the human and rat mast cell high-affinity IgE receptors. Both human and rat cDNAs encode an NH{sub 2}-terminal signal peptide, two immunoglobulin-like extracellular domains (encoded by discrete exons), a hydrophobic transmembrane region, and a positively charged cytoplasmic tail. The human and rat {alpha} subunits share an overall homology with one another and the immunoglobulin gene family, suggesting that they arose from a common ancestral gene and continue to share structural homology with their ligands. In addition, the rat gene is transcribed into at least three distinct forms, each of which yields a somewhat different coding sequence.

1988-03-01

442

Gonadal hormone modulation of neurogenesis in the dentate gyrus of adult male and female rodents  

British Library Electronic Table of Contents (United Kingdom)

Gonadal hormones modulate neurogenesis in the dentate gyrus differentially in male and female adult rodents. Neurogenesis is comprised of at least two components: cell proliferation (the production of new cells) and cell survival (the number of new neurons that survive to maturity). Previous studies have found sex differences in the level of cell proliferation in the dentate gyrus only when comparing females in a high estrogen state to males. This review focuses on the effects of acute and chronic levels of estrogens or androgens on hippocampal neurogenesis in the adult male and female rodent. Evidence is also reviewed for the co-localization of androgen receptors and estrogen receptors (ER) with markers for cell proliferation or immature new cell survival. Briefly, evidence suggests that ...

2008-01-01

443

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

Energy Technology Data Exchange (ETDEWEB)

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

444

Epigenetic regulation of Myc on retinoic acid receptor beta and PDLIM4 in RWPE1 cells  

British Library Electronic Table of Contents (United Kingdom)

BACKGROUND Hypermethylation of CpG islands is a common epigenetic alteration associated with cancer. Tumor suppressor genes retinoic acid receptor beta (RARb) and PDLIM4 are hypermethylated and silenced in prostate cancer (PCa) tissues and PCa cell lines compared to normal prostate cells. METHODS In this study, a benign prostate epithelial cell line RWPE1 was used as a model to study the epigenetic regulation of Myc on the RARb and PDLIM4 promoters. Forced Myc overexpression inhibited the RARb and PDLIM4 expression. RESULTS Pyrosequencing study showed that Myc overexpression increased methylation in several CpG sites of both promoters. A DNA methylation inhibitor 5-aza-2prime-deoxycytidine reversed the epigenetic alteration effect of Myc on both RARb and PDLIM4. CONCLUSION The epigenetic r...

2009-01-01

445

Clonidine, octopaminergic receptor agonist, reduces protein feeding in the blow fly, Phormia regina (Meigen)  

British Library Electronic Table of Contents (United Kingdom)

Results in this study are consistent with those of Murdock and his colleagues who clearly demonstrated that clonidine, an agonist of octopaminergic receptors in some insects, significantly increases sucrose feeding. Their studies, however, did not examine the effect of clonidine on protein feeding. Injection of a 20mg/ml/fly dose of clonidine significantly reduces protein feeding in both sexes of Phormia regina, instead of stimulating feeding as is observed with carbohydrate feeding. The manner in which the flies are fed prior to starvation and the method of testing influences the amounts of diet consumed. It is proposed that the biogenic amines influence the state of hunger (i.e., protein versus carbohydrates) while other chemicals and neural mechanisms (i.e., such as sulfakinins and stre...

2007-01-01

446

Change in number and activation of androgen receptor-immunoreactive cells in the medial amygdala in response to chemosensory input  

British Library Electronic Table of Contents (United Kingdom)

In many species social behaviors are dependent on integration of chemosensory and hormonal cues. Many chemosensory stimuli are detected by the vomeronasal organ, which projects to many regions that contain steroid receptors, including the medial amygdala. In male hamsters, testosterone is known to acutely increase in response to chemosensory stimulation, and can facilitate sexual behavior by direct action within the medial amygdala. Conspecific stimuli activate the anterior (MeA) and posterior (MeP) medial amygdala, while heterospecific stimuli activate only MeA. Chemosensory stimuli with different social significance differentially activate the dorsal and ventral subdivisions of MeA and MeP. Therefore, it is likely that steroids differentially facilitate stimulation of the medial amygdala...

2011-01-01

447

Tuberous Sclerosis Complex Activity is Required to Control Neuronal Stress Responses in an mTOR-Dependent Manner  

UK PubMed Central (United Kingdom)

Tuberous Sclerosis Complex (TSC) is a neurogenetic disorder caused by loss-of-function mutations in either the TSC1 or TSC2 genes and frequently results in...Full Text Available

2009-05-06

448

The requirement of yeast replication origins for pre-replication complex proteins is modulated by transcription  

UK PubMed Central (United Kingdom)

The mini-chromosome maintenance proteins Mcm2–7 are essential for DNA replication. They are loaded onto replication origins during G1 phase of the cell cycle to form a pre-replication complex...Full Text Available

2005-01-01

449

The effect of an ?-globulin preparation and of polyribonuclease complexes on humoral antibody formation  

UK PubMed Central (United Kingdom)

The effects of bovine α-globulin (BAG), bovine-ribonuclease serum albumin (BSA-RNase) and polyribonuclease (poly-RNase) complexes on the primary response of rodents to sheep erythrocytes have...Full Text Available

1968-06-01

450

The Nature of Arsenic-Phytochelatin Complexes in Holcus lanatus and Pteris cretica1  

UK PubMed Central (United Kingdom)

We have developed a method to extract and separate phytochelatins (PCs)—metal(loid) complexes using parallel metal(loid)-specific (inductively coupled plasma-mass spectrometry) and organic-specific...Full Text Available

2004-03-01

451

The Dystrophin Complex Controls BK Channel Localization and Muscle Activity in Caenorhabditis elegans  

UK PubMed Central (United Kingdom)

Genetic defects in the dystrophin-associated protein complex (DAPC) are responsible for a variety of pathological conditions including muscular dystrophy, cardiomyopathy, and vasospasm. Conserved DAPC...Full Text Available

2009-12-01

452

Stereospecific ligands and their complexes. Part VII. Synthesis, characterization and in vitro antitumoral activity of platinum(II) complexes with O,Oprime-dialkyl esters of (S,S)-ethylenediamine-N,Nprime-di-2-(4-methyl)pentanoic acid  

British Library Electronic Table of Contents (United Kingdom)

Platinum(II) complexes (1-4) with bidentate N,Nprime-ligands, O,Oprime-dialkyl esters (alkyl = ethyl, n-propyl, n-butyl and n-pentyl), of (S,S)-ethylenediamine-N,Nprime-di-2-(4-methyl)pentanoic acid were synthesized and characterized by IR, 1H NMR and 13C NMR spectroscopy and elemental analysis. DFT calculations were performed for the complexes and it was found that only one diastereoisomer could be formed. Cytotoxic activity of complexes 1-4 was determined against chronic lymphocytic leukemia cells (CLL) and compared to the activity of ligand precursors L12HCl-L42HCl and corresponding palladium(II) complexes, [PdCl2L] (L = L1-L4). The complexes were found to exhibit significantly higher antitumor activities than cisplatin on CLL cells. Cytotoxic effect of platinum(II) complexes on CLL cel...

2011-01-01

453

Spoligotype Profile of Mycobacterium tuberculosis Complex Strains from HIV-Positive and -Negative Patients in Nigeria: a Comparative Analysis ?  

UK PubMed Central (United Kingdom)

We ran a comparative analysis of all patients for whom a positive culture of Mycobacterium tuberculosis complex was available between April 2004 and October 2005 and whose HIV serology...Full Text Available

2011-01-01

454

Sodium ion cycling mediates energy coupling between complex I and ATP synthase  

UK PubMed Central (United Kingdom)

We show here sodium ion cycling between complex I from Klebsiella pneumoniae and the F1F0 ATP synthase from Ilyobacter tartaricus in a reconstituted...Full Text Available

2003-02-04

455

Selective Enrichment of Azide-Containing Peptides from Complex Mixtures  

UK PubMed Central (United Kingdom)

A general method is described to sequester peptides containing azides from complex peptide mixtures, aimed at facilitating mass spectrometric analysis to study different aspects of proteome...Full Text Available

2009-07-01

456

SIRT1 contributes to telomere maintenance and augments global homologous recombination  

UK PubMed Central (United Kingdom)

Yeast Sir2 deacetylase is a component of the silent information regulator (SIR) complex encompassing Sir2/Sir3/Sir4. Sir2 is recruited to telomeres through Rap1, and this complex spreads into subtelomeric...Full Text Available

2010-12-27

457

Resonance Raman enhancement of phenyl ring vibrational modes in phenyl iron complex of myoglobin.  

UK PubMed Central (United Kingdom)

Resonance Raman spectra are reported for the organometallic phenyl-FeIII complexes of horse heart myoglobin. We observed the resonance enhancement of the ring vibrational modes of the bound phenyl group....Full Text Available

1990-04-01

458

Resolving Individuals Contributing Trace Amounts of DNA to Highly Complex Mixtures Using High-Density SNP Genotyping Microarrays  

UK PubMed Central (United Kingdom)

We use high-density single nucleotide polymorphism (SNP) genotyping microarrays to demonstrate the ability to accurately and robustly determine whether individuals are in a complex genomic DNA mixture....Full Text Available

2008-08-01

459

Preparation and Evaluation of Taste Masked Famotidine Formulation Using Drug/?-cyclodextrin/Polymer Ternary Complexation Approach  

UK PubMed Central (United Kingdom)

The main aim of the present study was to evaluate potential of ternary complexation (comprising of drug, cyclodextrin and polymer) as an approach for taste masking. For this purpose famotidine with...Full Text Available

460

Potential of mTOR inhibitors for the treatment of subependymal giant cell astrocytomas in tuberous sclerosis complex  

UK PubMed Central (United Kingdom)

Rapamycin inhibits the mTOR (target of rapamycin) pathway and extends lifespan in multiple species. The tuberous sclerosis complex (TSC) protein is a negative regulator of mTOR. In humans, loss of the...Full Text Available

461

Oxidation of phosphine by iron(III) chloride complexes supported on activated charcoal  

Energy Technology Data Exchange (ETDEWEB)

It has been discovered that iron(III) chloride complexes supported on activated charcoal oxidize phosphine under normal conditions. The process accelerates as the concentration of the chloride ions and the proton acid increases.

1988-06-01

462

On scientific and technical maintenance of the nuclear power complex in Ukraine  

International Nuclear Information System (INIS)

The article gives a brief description of the state of the nuclear power engineering in Ukraine and in the world as of today. There are basic organizational and practical actions on scientific and technical maintenance of the Ukraine nuclear power complex presented in the article.

2006-01-01

463

Nuclear Pore Complex Number and Distribution throughout the Saccharomyces cerevisiae Cell Cycle by Three-Dimensional Reconstruction from Electron Micrographs of Nuclear Envelopes  

UK PubMed Central (United Kingdom)

The number of nuclear pore complexes (NPCs) in individual nuclei of the yeast Saccharomyces cerevisiae was determined by computer-aided reconstruction of entire nuclei from electron...Full Text Available

1997-11-01

464

Multivesicular bodies in the enigmatic amoeboflagellate Breviata anathema and the evolution of ESCRT 0  

UK PubMed Central (United Kingdom)

Endosomal sorting complexes required for transport (ESCRTs) are heteromeric protein complexes required for multivesicular body (MVB) morphogenesis. ESCRTs I, II, III and III-associated are ubiquitous...Full Text Available

2011-02-15

465

Method of removing hydrogen sulfide and carbon dioxide from gases  

Energy Technology Data Exchange (ETDEWEB)

A process for the recovery of nitrilotriacetic acid values from solutions containing polyvalent metal complexes of nitrilotriacetic and the decomposition products thereof is described, the process being characterized by the addition to such solutions of sufficient strong acid to dissociate the complex under conditions to precipitate the nitrilotriacetic acid.

1984-04-17

466

Long-lived quantum coherence in photosynthetic complexes at physiological temperature  

UK PubMed Central (United Kingdom)

Photosynthetic antenna complexes capture and concentrate solar radiation by transferring the excitation to the reaction center that stores energy from the photon in chemical bonds. This process occurs...Full Text Available

2010-07-20

467

Intracellular ribonucleoprotein complexes of visna virus are infectious.  

UK PubMed Central (United Kingdom)

Sheep choroid plexus cells infected with visna virus produce intracytoplasmic viral ribonucleoprotein complexes with sedimentation values of 120S to 200S and buoyant densities of 1.29 to 1.32 g/cm3....Full Text Available

1982-06-01

468

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

UK PubMed Central (United Kingdom)

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

469

Influence of major histocompatibility complex genotype on mating success in a free-ranging reptile population  

UK PubMed Central (United Kingdom)

Major histocompatibility complex (MHC) genes are highly polymorphic components of the vertebrate immune system, which play a key role in pathogen resistance. MHC genes may also function as odour-related...Full Text Available

2009-05-07

470

Identification of Triploid Individuals and Clonal Lines in Carassius Auratus Complex Using Microsatellites  

UK PubMed Central (United Kingdom)

The Carassius auratus complex in natural populations includes diploid triploid and polyploidy individuals. Diploid individuals belong to the species Carassius auratus...Full Text Available

471

Genetic architecture of complex traits: Large phenotypic effects and pervasive epistasis  

UK PubMed Central (United Kingdom)

The genetic architecture of complex traits underlying physiology and disease in most organisms remains elusive. We still know little about the number of genes that underlie these traits, the magnitude...Full Text Available

2008-12-16

472

Failure to detect circulating DNA--anti-DNA complexes by four radioimmunological methods in patients with systemic lupus erythematosus.  

UK PubMed Central (United Kingdom)

The presence of DNA-anti-DNA complexes in sera from patients with systemic lupus erythematosus (SLE) was investigated by two new radioimmunoassays (RIA) developed for this purpose and by measuring the...Full Text Available

1977-12-01

473

Developmental plasticity and the evolution of animal complex life cycles  

UK PubMed Central (United Kingdom)

Metazoan life cycles can be complex in different ways. A number of diverse phenotypes and reproductive events can sequentially occur along the cycle, and at certain stages a variety of developmental...Full Text Available

2010-02-27

474

Design complexity in termite-fishing tools of chimpanzees (Pan troglodytes)  

UK PubMed Central (United Kingdom)

Adopting the approach taken with New Caledonian crows (Corvus moneduloides), we present evidence of design complexity in one of the termite-fishing tools of chimpanzees (Pan...Full Text Available

2009-06-23

475

Cellulase-Xylanase Synergy in Designer Cellulosomes for Enhanced Degradation of a Complex Cellulosic Substrate  

UK PubMed Central (United Kingdom)

Designer cellulosomes are precision-engineered multienzyme complexes in which the molecular architecture and enzyme content are exquisitely controlled. This system was used to examine enzyme cooperation...Full Text Available

476

Carney-Complex: Multiple resections of recurrent cardiac myxoma  

UK PubMed Central (United Kingdom)

We report a case of a female patient who was operated at the third relapse of an atrial myxoma caused by Carney complex. The difficult operation was performed without any complications despite extensive...Full Text Available

477

Animal and human studies of a new /sup 99m/Tc labelled phosphine-isocyanide complex with possible applications to radionuclide ventriculography  

Energy Technology Data Exchange (ETDEWEB)

A new /sup 99m/Tc-phosphine-isocyanide complex with the general structure (/sup 99m/Tc (DEPE)/sub 2/(CNR)/sub 2/)/sup +/ has been synthesised and tested in animals and one human. In three animal species (rat, rabbit, dog), the complex is an efficient myocardial imaging agent, while in humans it remains in the blood pool. The complex is 100% protein bound in animals and humans, but whereas in humans it is attached to a 51.5 kdalton protein (probably prealbumin), in rabbits it appears to be bound to a larger macromolecule (M.W.>100 kdalton). The efficiency of the complex for blood pool labelling was tested in a human volunteer and compared with the standard in vivo red cell labelling technique with stannous pyrophosphate. A satisfactory radionuclide angiogram could be performed with less than 370 MBq of the complex. The count rate for the complex (cps/MBq) was ...

1987-04-01

478

A genome-wide survey of Major Histocompatibility Complex (MHC) genes and their paralogues in zebrafish  

UK PubMed Central (United Kingdom)

BackgroundThe genomic organisation of the Major Histocompatibility Complex (MHC) varies greatly between different vertebrates. In mammals, the classical MHC consists of a large number...Full Text Available

479

A functional comparison of the hyolingual complex in pygmy and dwarf sperm whales (Kogia breviceps and K. sima), and bottlenose dolphins (Tursiops truncatus)  

UK PubMed Central (United Kingdom)

The function of the hyolingual complex in three odontocete species was investigated to compare adaptations of divergent feeding strategies, suction and ram feeding. Pygmy and dwarf sperm whales, members...Full Text Available

2007-07-01

480

'Sheltered disruption' of Neurospora crassa MOM22, an essential component of the mitochondrial protein import complex.  

UK PubMed Central (United Kingdom)

MOM22 is a component of the protein import complex of the mitochondrial outer membrane of Neurospora crassa. Using the newly developed procedure of 'sheltered disruption', we created a heterokaryotic...Full Text Available

1995-03-15

482

Treatment of multi-ruptured complex pseudoaneurysm with injection of fibrin sealant into lumens: report of one case with literature review  

International Nuclear Information System (INIS)

This paper is to report a case of multi-ruptured complex pseudoaneurysm confirmed by three-dimensional DSA. Under three-dimensional DSA guidance, the thrombin was injected into lumens in the attempt to cure the pseudoaneurysm. As the result was unsatisfactory, fibrin sealant was used to inject into the lumens again, and good curative effect was obtained. In clinical interventional practice, the incidence of pseudoaneurysm has been steadily increasing and the lesions have become more and more complex. In this paper the authors have discussed the diagnostic and therapeutic methods of complex pseudoaneurysm in order to provide clinical physicians with useful information. (authors)

2009-03-01

483

The electronic structure of organometallic complexes of the f elements XXV. Crystal field splitting pattern of the anionic complex [Cp_3Pr. NCS]"-  

International Nuclear Information System (INIS)

The absorption, emission and magnetic circular dichroism spectra of the anionic complex (Cp_3Pr. NCS)"- were measured at room and low temperatures. On the basis of these spectra the electronic structure in the f-f range could be derived. The parameters of an empirical Hamiltonian were fitted to the experimentally determined crystal field splitting pattern. Compared with the previously examined neutral Cp_3 Pr.X complexes the quadratic crystal field parameter B_0"2 is considerably reduced.

485

Syntheses and phosphorus-31 NMR studies of five-coordinate platinum(II) complexes of tris(2-(diphenylphosphino)ethyl)phosphine and monodentate phosphorus ligands  

Energy Technology Data Exchange (ETDEWEB)

The first preparation and characterization of the platinum (II) complexes containing five phosphorus ligands are reported herein. The complexes are represented by the formulae (Pt(PP/sub 3/)(P(OR)/sub 3/)Cl/sub 2/, where R = Me or Et, and (Pt(PP/sub 3/)(PEt/sub 3/))Cl/sub 2/. The /sup 31/P spectra of the complexes are presented. 10 references, 2 tables.

1987-12-02

486

Structure of Irradiated Materials  

International Science & Technology Center (ISTC)

Fundamental Research of Materials Structure and Properties Changes Resulted from Irradiation by Means of Complex of Modern Physical Methods

487

Solid-phase synthesis and pharmacological evaluation of novel nucleoside-tethered dinuclear platinum(II) complexes  

British Library Electronic Table of Contents (United Kingdom)

Three novel inosine-based dinuclear platinum complexes have been synthesized via a solid-phase strategy. In these compounds, the metal is linked both to the N-7 of the purine nucleus and to the terminal amine group of a hexylamine side chain installed on N-1. Cis- or trans- diamine as well as ethylenediamine ligands are coordinated to platinum along with a chloride. The synthesised complexes were tested against four different human tumor cell lines. One of these complexes proved to be more cytotoxic than cisplatin against the MCF7 cancer cell line in a short-term exposure assay.

2011-01-01

488

Proceedings of ARO Workshop Biostructures as Composite ...  

Science.gov (United States)

... interactive surfaces and interfaces, and 3) the more complex a ... carbonate or calcium phosphate with a thin interface ... diameter) for nerve prosthesis. ...

1990-03-01

490

On Phase Transition of Compressed Sensing in the Complex Domain  

CERN Document Server

The phase transition is a performance measure of the sparsity-undersampling tradeoff in compressed sensing (CS). This letter reports, for the first time, the existence of an exact phase transition for the $\\ell_1$ minimization approach to the complex valued CS problem. This discovery is not only a complementary result to the known phase transition of the real valued CS but also shows considerable superiority of the phase transition of complex valued CS over that of the real valued CS. The results are obtained by extending the recently developed ONE-L1 algorithms to complex valued CS and applying their optimal and iterative solutions to empirically evaluate the phase transition.

2011-01-01

491

Magnetic properties of oxovanadium(IV) complexes with bidentate on donor Schiff bases  

International Nuclear Information System (INIS)

(Feb 1977). Japan Syamal, A. Bombay Univ. (India). Univ. Dept. of Chemical

1977-01-01

492

KoderaUNEP_Uploaded web [Compatibility Mode  

Wastenet

complex -agriculture sector in a local community -blast furnace -cokes oven -cement kiln

493

ICDF Complex Operations Waste Management Plan  

Science.gov (United States)

This Waste Management Plan functions as a management and planning tool for managing waste streams generated as a result of operations at the Idaho CERCLA Disposal Facility (ICDF) Complex. The waste management activities described in this plan support the selected remedy presented in the Waste Area Group 3, Operable Unit 3-13 Final Record of Decision for the operation of the Idaho CERCLA Disposal Facility Complex. This plan identifies the types of waste that are anticipated during operations at the Idaho CERCLA Disposal Facility Complex. In addition, this plan presents management strategies and disposition for these anticipated waste streams.

2006-12-01

496

Ammoxidation of methanol to produce hydrogen cyanide  

Energy Technology Data Exchange (ETDEWEB)

Promoted antimony phosphate oxide complexes are excellent catalysts for the ammoxidation of methanol to HCN especially at high methanol throughputs.

1985-04-16

497

Thorium different-ligand complexes with morin as analytic form for extraction-photometric determination of thorium microamounts  

International Nuclear Information System (INIS)

Consideration is given to results of investigation into thorium complexing with morin (H_2Mor) in extraction systems containing different carboxylic acids as well as different salt background. The obtained data enabled to suggest the method of photometric determination of thorium in the form of Th(HMor)_2Benz_2 different-ligand complex (where Benz-anion of benzilic acid) with 0.25 #mu#g/ml detection limit.

1989-01-01

498

Testing modern protective relays  

Energy Technology Data Exchange (ETDEWEB)

Modern microprocessor-based relays for the protection of the various power system components such as generators, transformers, feeders, and high voltage transmission lines are becoming more sophisticated as increasingly more complex functions and capabilities can be included in the microprocessor. With this increasing complexity, and the increasing complexity of the power system itself, there is even more value in testing the suitability of relaying equipment for the intended applications. This paper reviews the testing philosophy, experience, and capabilities developed at Ontario Hydro over more than 25 years of testing protective relays.

1994-01-01

499

Solvent extraction studies using tetracycline as a complexing agent. Pt. 12. Determination of stability constants for the complexes of uranium and tetracycline  

Energy Technology Data Exchange (ETDEWEB)

Stability constants for uranium-tetracycline complexes were determined by the method of average number of ligands, the method of limiting values, the method of two parameters and the method of weighted least squares. Solvent extraction technique was used to obtain experimental data. (author). 10 refs.; 5 figs.

1985-09-01

500

Characterization of DTPA complexes and conjugated antibodies of astatine  

International Nuclear Information System (INIS)

The complex formation of astatine(I) cation with diethylene triamine pentaacetic acid (DTPA) and characterization of the complexes were investigated by electromigration in free electrolytes and by gel-chromatography on Sephadex G 25. The conjugation procedure for the production of At-DTPA conjugated polyclonal antibodies is described. (author) 15 refs.; 2 figs.