ADRA2B

Summary

Gene Symbol: ADRA2B
Description: adrenoceptor alpha 2B
Alias: ADRA2L1, ADRA2RL1, ADRARL1, ALPHA2BAR, FAME2, alpha-2BAR, alpha-2B adrenergic receptor, ADRA2B adrenergic, alpha-2B-, receptor, G-protein coupled receptor, alpha-2 adrenergic receptor subtype C2, alpha-2-adrenergic receptor-like 1, alpha-2B adrenoreceptor
Species: human

Top Publications

  1. ncbi An insertion/deletion polymorphism in the alpha2B-adrenergic receptor gene is a novel genetic risk factor for acute coronary events
    A Snapir
    Department of Pharmacology and Clinical Pharmacology, University of Turku, Finland
    J Am Coll Cardiol 37:1516-22. 2001
  2. pmc Regulation of α(2B)-adrenergic receptor-mediated extracellular signal-regulated kinase 1/2 (ERK1/2) activation by ADP-ribosylation factor 1
    Chunmin Dong
    Department of Pharmacology and Experimental Therapeutics, Louisiana State University Health Sciences Center, New Orleans, Louisiana 70112, USA
    J Biol Chem 286:43361-9. 2011
  3. ncbi Identification of a three-amino acid deletion in the alpha2B-adrenergic receptor that is associated with reduced basal metabolic rate in obese subjects
    P Heinonen
    Department of Pharmacology and Clinical Pharmacology, University of Turku, Finland
    J Clin Endocrinol Metab 84:2429-33. 1999
  4. ncbi Polymorphic deletion of three intracellular acidic residues of the alpha 2B-adrenergic receptor decreases G protein-coupled receptor kinase-mediated phosphorylation and desensitization
    K M Small
    Department of Medicine, University of Cincinnati College of Medicine, Cincinnati, OH 45267, USA
    J Biol Chem 276:4917-22. 2001
  5. ncbi Alpha(2B)-adrenergic receptor deletion polymorphism associates with autonomic nervous system activity in young healthy Japanese
    Naoko Suzuki
    Laboratories of Metabolism, Kyoto University Graduate School of Human and Environmental Studies, Japan
    J Clin Endocrinol Metab 88:1184-7. 2003
  6. ncbi Alpha2B-adrenergic receptor deletion polymorphism and cardiac autonomic nervous system responses to exercise in obese women
    L M Ueno
    Heart Institute InCor, Medical School, University of Sao Paulo, Sao Paulo, Brazil
    Int J Obes (Lond) 30:214-20. 2006
  7. pmc Expansion of the alpha 2-adrenergic receptor family: cloning and characterization of a human alpha 2-adrenergic receptor subtype, the gene for which is located on chromosome 2
    J W Lomasney
    Department of Pathology, Duke University Medical Center, Durham, NC 27710
    Proc Natl Acad Sci U S A 87:5094-8. 1990
  8. ncbi Cardiovascular and metabolic phenotypes in relation to the ADRA2B insertion/deletion polymorphism in a Chinese population
    Haifeng Zhang
    Department of Cardiology, Jiangsu Province Hospital, Nanjing Medical University, Nanjing, China
    J Hypertens 23:2201-7. 2005
  9. ncbi An insertion/deletion polymorphism in the alpha2B adrenoceptor gene is associated with age at onset of type 2 diabetes mellitus
    D Papazoglou
    Second Department of Internal Medicine, Medical School of Alexandroupolis, Democritus University of Thrace, Alexandroupolis, Greece
    Exp Clin Endocrinol Diabetes 114:424-7. 2006
  10. ncbi Effect of a three-amino acid deletion in the alpha2B-adrenergic receptor gene on long-term body weight change in Finnish non-diabetic and type 2 diabetic subjects
    K Sivenius
    Department of Clinical Nutrition, University of Kuopio, Kuopio, Finland
    Int J Obes Relat Metab Disord 25:1609-14. 2001

Research Grants

  1. Jeffrey L Benovic; Fiscal Year: 2015
  2. Endogenous G-Protein Coupled Receptor Antagonists
    Carrie Haskell-Luevano; Fiscal Year: 2012
  3. Ligand Directed Functional Selectivity of G-Protein Coupled Receptor Signalling
    Gerry S Oxford; Fiscal Year: 2012
  4. 2010 Ligand Recognition and Molecular Gating Gordon Research Conference
    NANCY RYAN GRAY; Fiscal Year: 2010
  5. G protein-coupled receptor kinase 3 regulation of leukocyte function in inflammat
    TERESA KATHLEEN TARRANT; Fiscal Year: 2013
  6. G PROTEIN COUPLED RECEPTOR ACTIVATION STUDIED IN YEAST
    Mark Dumont; Fiscal Year: 2009
  7. Brian K Kobilka; Fiscal Year: 2016
  8. G Protein Coupled Receptor Modulation of Synaptic Transmission
    EDAENI YISHAK HAMID; Fiscal Year: 2010
  9. Qin Wang; Fiscal Year: 2016
  10. Basis of Variability of Lung GPCR Signaling
    Stephen B Liggett; Fiscal Year: 2013

Detail Information

Publications1053 found, 100 shown here

  1. ncbi An insertion/deletion polymorphism in the alpha2B-adrenergic receptor gene is a novel genetic risk factor for acute coronary events
    A Snapir
    Department of Pharmacology and Clinical Pharmacology, University of Turku, Finland
    J Am Coll Cardiol 37:1516-22. 2001
    ..Our aim was to study whether an insertion/deletion (I/D) polymorphism in the alpha2B-adrenoceptor gene is associated with the risk for cardiovascular diseases...
  2. pmc Regulation of α(2B)-adrenergic receptor-mediated extracellular signal-regulated kinase 1/2 (ERK1/2) activation by ADP-ribosylation factor 1
    Chunmin Dong
    Department of Pharmacology and Experimental Therapeutics, Louisiana State University Health Sciences Center, New Orleans, Louisiana 70112, USA
    J Biol Chem 286:43361-9. 2011
    ..These data strongly demonstrate that the small GTPase ARF1 modulates ERK1/2 activation by α(2B)-AR and provide the first evidence indicating a novel function for ARF1 in regulating the MAPK signaling pathway...
  3. ncbi Identification of a three-amino acid deletion in the alpha2B-adrenergic receptor that is associated with reduced basal metabolic rate in obese subjects
    P Heinonen
    Department of Pharmacology and Clinical Pharmacology, University of Turku, Finland
    J Clin Endocrinol Metab 84:2429-33. 1999
    ..84; P = 0.009, by ANOVA). Thus, a genetic polymorphism of the alpha2B-adrenoceptor subtype can partly explain the variation in basal metabolic rate in an obese population and may therefore contribute to the pathogenesis of obesity...
  4. ncbi Polymorphic deletion of three intracellular acidic residues of the alpha 2B-adrenergic receptor decreases G protein-coupled receptor kinase-mediated phosphorylation and desensitization
    K M Small
    Department of Medicine, University of Cincinnati College of Medicine, Cincinnati, OH 45267, USA
    J Biol Chem 276:4917-22. 2001
    ..Thus the major phenotype of the Del301-303 alpha(2B)AR is one of impaired phosphorylation and desensitization by GRKs, and thus the polymorphisms renders the receptor incapable of modulation by this key mechanism of dynamic regulation...
  5. ncbi Alpha(2B)-adrenergic receptor deletion polymorphism associates with autonomic nervous system activity in young healthy Japanese
    Naoko Suzuki
    Laboratories of Metabolism, Kyoto University Graduate School of Human and Environmental Studies, Japan
    J Clin Endocrinol Metab 88:1184-7. 2003
    ..These findings suggest that the alpha(2B)AR deletion polymorphism might result in metabolic disorder by altering ANS function...
  6. ncbi Alpha2B-adrenergic receptor deletion polymorphism and cardiac autonomic nervous system responses to exercise in obese women
    L M Ueno
    Heart Institute InCor, Medical School, University of Sao Paulo, Sao Paulo, Brazil
    Int J Obes (Lond) 30:214-20. 2006
    ....
  7. pmc Expansion of the alpha 2-adrenergic receptor family: cloning and characterization of a human alpha 2-adrenergic receptor subtype, the gene for which is located on chromosome 2
    J W Lomasney
    Department of Pathology, Duke University Medical Center, Durham, NC 27710
    Proc Natl Acad Sci U S A 87:5094-8. 1990
    ..The unique pharmacology and tissue localization of this receptor suggest that this is an alpha 2AR subtype not previously identified by classical pharmacological or ligand binding approaches...
  8. ncbi Cardiovascular and metabolic phenotypes in relation to the ADRA2B insertion/deletion polymorphism in a Chinese population
    Haifeng Zhang
    Department of Cardiology, Jiangsu Province Hospital, Nanjing Medical University, Nanjing, China
    J Hypertens 23:2201-7. 2005
    The functional ADRA2B I/D polymorphism is associated with various cardiovascular and metabolic phenotypes in Caucasians...
  9. ncbi An insertion/deletion polymorphism in the alpha2B adrenoceptor gene is associated with age at onset of type 2 diabetes mellitus
    D Papazoglou
    Second Department of Internal Medicine, Medical School of Alexandroupolis, Democritus University of Thrace, Alexandroupolis, Greece
    Exp Clin Endocrinol Diabetes 114:424-7. 2006
    ..3% of its variance. This result indicates that the D allele may be implicated in impaired glucose metabolism leading to earlier manifestation of diabetes in predisposed subjects...
  10. ncbi Effect of a three-amino acid deletion in the alpha2B-adrenergic receptor gene on long-term body weight change in Finnish non-diabetic and type 2 diabetic subjects
    K Sivenius
    Department of Clinical Nutrition, University of Kuopio, Kuopio, Finland
    Int J Obes Relat Metab Disord 25:1609-14. 2001
    ..We investigated the effects of this polymorphism on changes in body weight in Finnish non-diabetic and type 2 diabetic subjects during a 10 y follow-up...
  11. ncbi Functional variant in the (alpha)2B adrenoceptor gene, a positional candidate on chromosome 2, associates with hypertension
    Fredrik von Wowern
    Department of Endocrinology, Wallenberg Laboratory, Ent 46, Floor 3, Malmo University Hospital, SE 205 02 Malmo, Sweden
    Hypertension 43:592-7. 2004
    ....
  12. ncbi Association between a deletion/insertion polymorphism in the alpha2B-adrenergic receptor gene and insulin secretion and Type 2 diabetes. The Finnish Diabetes Prevention Study
    N Siitonen
    Department of Clinical Nutrition and Food and Health Research Center, University of Kuopio, Kuopio, Finland
    Diabetologia 47:1416-24. 2004
    ..this study we investigated whether the 12Glu9 polymorphism in the gene encoding the alpha2B-adrenergic receptor ( ADRA2B) is associated with insulin secretion and/or the incidence of Type 2 diabetes in individuals with impaired glucose ..
  13. pmc Opioid modulation of extracellular signal-regulated protein kinase activity is ras-dependent and involves Gbetagamma subunits
    M M Belcheva
    E. A. Doisy Department of Biochemistry and Molecular Biology, St. Louis University School of Medicine, Missouri 63104-1079, USA
    J Neurochem 70:635-45. 1998
    ..These results suggest a mechanism involving Ras and betagamma subunits of Gi/o proteins in opioid agonist activation of ERK1 and ERK2, as well as opioid modulation of epidermal growth factor-induced ERK activity...
  14. pmc Cathepsin G and thrombin: evidence for two different platelet receptors
    M A Selak
    Department of Biochemistry and Molecular Biology, University of New Hampshire, Durham 03824
    Biochem J 297:269-75. 1994
    ....
  15. pmc Mode of action of thrombin in the rabbit aorta
    D Godin
    , , Canada
    Br J Pharmacol 115:903-8. 1995
    ..5. Altogether these results suggest the existence of subtle differences between the mode of action of thrombin and of synthetic peptides related to the N-terminal thrombin receptor sequence, in the rabbit aorta...
  16. pmc Gonadotropin-releasing hormone receptor in the teleost Haplochromis burtoni: structure, location, and function
    R R Robison
    Program in Neuroscience, Department of Psychology, Stanford University, Stanford, California 94305 2130, USA
    Endocrinology 142:1737-43. 2001
    ..Taken together, these data suggest that this H. burtoni GnRH receptor probably interacts in vivo with all three forms of GNRH:..
  17. ncbi Investigation of growth hormone releasing hormone receptor structure and activity using yeast expression technologies
    E M Kajkowski
    American Cyanamid Company, Princeton, New Jersey 08543, USA
    J Recept Signal Transduct Res 17:293-303. 1997
    ..These two yeast expression technologies should prove invaluable in additional structure/activity analyses of this ligand/receptor pair as well as other peptide ligands and receptors...
  18. pmc The C terminus of the Saccharomyces cerevisiae alpha-factor receptor contributes to the formation of preactivation complexes with its cognate G protein
    M Dosil
    Department of Molecular Genetics and Microbiology, State University of New York, Stony Brook, New York 11794 5222, USA
    Mol Cell Biol 20:5321-9. 2000
    ..These results suggest that the C-terminal cytoplasmic domain of the alpha-factor receptor, in addition to its role in receptor downregulation, promotes the formation of receptor-G-protein preactivation complexes...
  19. ncbi Internalization and down-regulation of human muscarinic acetylcholine receptor m2 subtypes. Role of third intracellular m2 loop and G protein-coupled receptor kinase 2
    H Tsuga
    Department of Neurochemistry, Faculty of Medicine, University of Tokyo, 7 3 1 Hongo, Bunkyo ku, Tokyo 113, Japan
    J Biol Chem 273:5323-30. 1998
    ....
  20. ncbi Substrate specificities of g protein-coupled receptor kinase-2 and -3 at cardiac myocyte receptors provide basis for distinct roles in regulation of myocardial function
    Leif Erik Vinge
    Institute for Surgical Research, Rikshospitalet Radiumhospitalet Medical Center, University of Oslo, Oslo, Norway
    Mol Pharmacol 72:582-91. 2007
    ....
  21. ncbi Sphingosylphosphorylcholine and lysophosphatidylcholine are ligands for the G protein-coupled receptor GPR4
    K Zhu
    Department of Cancer Biology, Cleveland Clinic Foundation, Cleveland, Ohio 44195, USA
    J Biol Chem 276:41325-35. 2001
    ..Taken together, our data indicate that GPR4 is a receptor with high affinity to SPC and low affinity to LPC, and that multiple cellular functions can be transduced via this receptor...
  22. ncbi beta-Arrestin/AP-2 interaction in G protein-coupled receptor internalization: identification of a beta-arrestin binging site in beta 2-adaptin
    Stephane A Laporte
    Howard Hughes Medical Institute Laboratories, The Department of Cell Biology, and the Department of Medicine, Duke University Medical Center, Durham, North Carolina 27710, USA
    J Biol Chem 277:9247-54. 2002
    ..These results suggest that the interaction of beta-arrestin with beta(2)-adaptin represents a selective endocytic trigger for several members of the GPCR family...
  23. ncbi Suppression of the morphine-induced rewarding effect and G-protein activation in the lower midbrain following nerve injury in the mouse: involvement of G-protein-coupled receptor kinase 2
    S Ozaki
    Department of Toxicology, Hoshi University School of Pharmacy and Pharmaceutical Sciences, Tokyo 142 8501, Japan
    Neuroscience 116:89-97. 2003
    ....
  24. ncbi Gbetagamma subunits mediate Src-dependent phosphorylation of the epidermal growth factor receptor. A scaffold for G protein-coupled receptor-mediated Ras activation
    L M Luttrell
    Howard Hughes Medical Institute and the Departments of Medicine and Biochemistry, Duke University Medical Center, Durham, North Carolina 27710, USA
    J Biol Chem 272:4637-44. 1997
    ....
  25. pmc Regulation of dynamin 2 and G protein-coupled receptor kinase 2 in rat nucleus accumbens during acute and repeated cocaine administration
    Joseph A Schroeder
    Department of Pharmacology and the Center for Substance Abuse Research, Temple University School of Medicine, Philadelphia, Pennsylvania 19140, USA
    Synapse 63:863-70. 2009
    ....
  26. ncbi A human gene encodes a putative G protein-coupled receptor highly expressed in the central nervous system
    P J Donohue
    Laboratory of Molecular Biology, National Institute on Deafness and Other Communication Disorders, Rockville, MD 20850, USA
    Brain Res Mol Brain Res 54:152-60. 1998
    ..We conclude that the natural ligand for this receptor is none of the known naturally occurring Bn-like peptides and the true agonist for GPCR/CNS remains to be elucidated...
  27. ncbi Association between physical activity and blood pressure is modified by variants in the G-protein coupled receptor 10
    Paul W Franks
    University of Cambridge, Department of Public Health and Primary Care, Cambridge, UK
    Hypertension 43:224-8. 2004
    ..Knowledge of GPR10 genotype may define those who are least likely to benefit from physical activity. These findings may have relevance in the targeted treatment of hypertensive disease...
  28. doi G-protein coupled receptor 35 (GPR35) activation and inflammatory pain: Studies on the antinociceptive effects of kynurenic acid and zaprinast
    Cristina Cosi
    Dipartimento di Farmacologia, Universita degli Studi di Firenze, Firenze, Italy
    Neuropharmacology 60:1227-31. 2011
    ..This article is part of a Special Issue entitled 'Trends in neuropharmacology: in memory of Erminio Costa'...
  29. ncbi G protein-coupled receptor kinases, beta-arrestin-2 and associated regulatory proteins in the human brain: postmortem changes, effect of age and subcellular distribution
    Muriel Grange-Midroit
    Clinical Research Unit, Department of Psychiatry, University of Geneva, H U G, Belle Idee, CH 1225 Chene Bourg, Switzerland
    Brain Res Mol Brain Res 101:39-51. 2002
    ....
  30. pmc The human herpesvirus 6 G protein-coupled receptor homolog U51 positively regulates virus replication and enhances cell-cell fusion in vitro
    Zhu Zhen
    Department of Microbiology and Immunology, University of Rochester School of Medicine and Dentistry, Rochester, NY 14642, USA
    J Virol 79:11914-24. 2005
    ..Overall, these studies suggest that HHV-6 U51 is a positive regulator of virus replication in vitro, perhaps because it may promote membrane fusion and facilitates cell-cell spread of this highly cell-associated virus...
  31. ncbi The leucine-rich repeat-containing G protein-coupled receptor 8 gene T222P mutation does not cause cryptorchidism
    Francesca Nuti
    Andrology Unit, Department of Clinical Physiopathology, University of Florence, Viale Pieraccini 6, 50139 Firenze, Italy
    J Clin Endocrinol Metab 93:1072-6. 2008
    ..This conclusion was based on both functional in vitro studies and the lack of mutation in a large group of controls. The geographical origin of the mutation carriers suggested a founder effect in the Mediterranean area...
  32. pmc A ligand channel through the G protein coupled receptor opsin
    Peter W Hildebrand
    Institut fur Medizinische Physik und Biophysik, Charite Universitatsmedizin Berlin, Berlin, Germany
    PLoS ONE 4:e4382. 2009
    The G protein coupled receptor rhodopsin contains a pocket within its seven-transmembrane helix (TM) structure, which bears the inactivating 11-cis-retinal bound by a protonated Schiff-base to Lys296 in TM7...
  33. ncbi Functional annotation of the putative orphan Caenorhabditis elegans G-protein-coupled receptor C10C6.2 as a FLP15 peptide receptor
    Teresa M Kubiak
    Animal Health Discovery Research, Pharmacia Corporation, Kalamazoo, MI 49001, USA
    J Biol Chem 278:42115-20. 2003
    ..To our knowledge, the FLP15 receptor is only the second deorphanized C. elegans neuropeptide GPCR reported to date...
  34. pmc Cloning, expression, and functional characterization of relaxin receptor (leucine-rich repeat-containing g protein-coupled receptor 7) splice variants from human fetal membranes
    Andras Kern
    The Pacific Biosciences Research Center, University of Hawaii, Honolulu, Hawaii 96822, USA
    Endocrinology 149:1277-94. 2008
    ....
  35. doi Association of G-protein-coupled receptor 154 with asthma and total IgE in a population of the Caribbean coast of Colombia
    C Vergara
    Institute for Immunological Research, University of Cartagena, Cartagena, Colombia
    Clin Exp Allergy 39:1558-68. 2009
    ..It has been subsequently associated with asthma and other inflammatory diseases in several populations with different ethnic origin. Replication of associations adds reliability to these findings...
  36. pmc Risperidone-induced inactivation and clozapine-induced reactivation of rat cortical astrocyte 5-hydroxytryptamine₇ receptors: evidence for in situ G protein-coupled receptor homodimer protomer cross-talk
    Carol Smith
    Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Ave, Albany, NY 12208, USA
    Mol Pharmacol 79:318-25. 2011
    ..The homodimer structure and protomer-protomer cross-talk offer new avenues of research into receptor dysfunction in disease states and the development of novel drugs...
  37. ncbi Role of sequence variations of the GnRH receptor and G protein-coupled receptor 54 gene in male idiopathic hypogonadotropic hypogonadism
    Fabio Lanfranco
    Institute of Reproductive Medicine of the University, D 48129 Munster, Germany
    Eur J Endocrinol 153:845-52. 2005
    ..To determine the frequency of mutations of the gonadotropin-releasing hormone receptor (GnRHR) and of the G protein-coupled receptor 54 (GPR54) genes in normosmic idiopathic hypogonadotropic hypogonadism (IHH)...
  38. ncbi Plausible interaction of an alpha-fetoprotein cyclopeptide with the G-protein-coupled receptor model GPR30: docking study by molecular dynamics simulated annealing
    A Hamza
    Unité de Modélisation Moléculaire, Institut Pasteur de Tunis, 13 Place Pasteur, BP 74, 1002 Tunis Belvedere, Tunisia
    J Biomol Struct Dyn 20:751-8. 2003
    ..Our modeling indicates a plausible interaction of the cyclopeptide with the seven transmembrane GPR30 protein. This may have profound implications for the treatment of breast cancer...
  39. ncbi G protein-coupled receptor 101 mRNA expression in the mouse brain: altered expression in the posterior hypothalamus and amygdala by energetic challenges
    K N Nilaweera
    Rowett Research Institute, Aberdeen Centre for Energy Regulation and Obesity ACERO, Bucksburn, Aberdeen, UK
    J Neuroendocrinol 19:34-45. 2007
    ..In the arcuate nucleus, GPCR101 mRNA was expressed in approximately half of the population of neurones expressing the mRNA for the anorexigenic neuropeptide, pro-opiomelanocortin, which suggests a potential functional relationship...
  40. pmc Monomeric G protein-coupled receptor rhodopsin in solution activates its G protein transducin at the diffusion limit
    Oliver P Ernst
    Institut fur Medizinische Physik und Biophysik, Charite Universitatsmedizin Berlin, Chariteplatz 1, D 10117 Berlin, Germany
    Proc Natl Acad Sci U S A 104:10859-64. 2007
    ..Whether docking in membranes involves the formation of rhodopsin dimers or oligomers remains to be elucidated...
  41. pmc Human G protein-coupled receptor GPR-9-6/CC chemokine receptor 9 is selectively expressed on intestinal homing T lymphocytes, mucosal lymphocytes, and thymocytes and is required for thymus-expressed chemokine-mediated chemotaxis
    B A Zabel
    LeukoSite, Inc, Cambridge, Massachusetts 02142, USA
    J Exp Med 190:1241-56. 1999
    ..The selective expression of TECK and GPR-9-6 in thymus and small intestine implies a dual role for GPR-9-6/CCR-9, both in T cell development and the mucosal immune response...
  42. ncbi High efficiency method for gene transfer in normal pituitary gonadotropes: adenoviral-mediated expression of G protein-coupled receptor kinase 2 suppresses luteinizing hormone secretion
    J D Neill
    Department of Physiology and Biophysics, University of Alabama, Birmingham 35294 0005, USA
    Endocrinology 140:2562-9. 1999
    ....
  43. ncbi Characterization of RANTES- and aminooxypentane-RANTES-triggered desensitization signals reveals differences in recruitment of the G protein-coupled receptor complex
    A J Vila-Coro
    Department of Immunology and Oncology, Centro Nacional de Biotecnologia, Consejo Superior de Investigaciones Cientificas Universidad Autonoma de Madrid, Spain
    J Immunol 163:3037-44. 1999
    ..We provide compelling evidence that the differences between RANTES and (AOP)-RANTES in G alpha i activation condition subsequent signaling events, including internalization and receptor recycling...
  44. ncbi Molecular cloning and characterization of another leukotriene B4 receptor
    M Kamohara
    Molecular Medicine Laboratories, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co, Ltd, 21 Miyukigaoka, Tsukuba, Ibaraki 305 8585, Japan
    J Biol Chem 275:27000-4. 2000
    ..The discovery of this second leukotriene B(4) receptor will eventually lead to a better understanding of the classification of leukotriene B(4) receptors and reconsideration of the pathophysiological role of leukotriene B(4)...
  45. ncbi Melatonin receptors and their regulation: biochemical and structural mechanisms
    Paula A Witt-Enderby
    Division of Pharmaceutical Sciences, Duquesne University School of Pharmacy, 421 Mellon Hall, Pittsburgh, PA 15282, USA
    Life Sci 72:2183-98. 2003
    ....
  46. pmc Evaluation of the role of the retinal G protein-coupled receptor (RGR) in the vertebrate retina in vivo
    Tadao Maeda
    Department of Ophthalmology, University of Washington, Seattle, WA 98195 6485, USA
    J Neurochem 85:944-56. 2003
    ....
  47. ncbi Role of mammalian vacuolar protein-sorting proteins in endocytic trafficking of a non-ubiquitinated G protein-coupled receptor to lysosomes
    James N Hislop
    Department of Psychiatry, University of California, San Francisco, California 94143 2140, USA
    J Biol Chem 279:22522-31. 2004
    ....
  48. ncbi Identification of a G protein-coupled receptor specifically responsive to beta-alanine
    Tokuyuki Shinohara
    Discovery Research Laboratories, Pharmaceutical Research Division, Takeda Chemical Industries Ltd, 10 Wadai, Tsukuba, Ibaraki 300 4293, Japan
    J Biol Chem 279:23559-64. 2004
    ..Our results suggest that TGR7 participates in the modulation of neuropathic pain...
  49. ncbi Phosphorylation of the platelet-derived growth factor receptor-beta by G protein-coupled receptor kinase-2 reduces receptor signaling and interaction with the Na(+)/H(+) exchanger regulatory factor
    Kerry L Hildreth
    Department of Medicine Cardiology, Duke University Medical Center, Durham, North Carolina 27710, USA
    J Biol Chem 279:41775-82. 2004
    ..Furthermore, this desensitization appears to involve GRK2-mediated phosphorylation of PDGFRbeta Ser(1104), with consequent dissociation of the PDGFRbeta from NHERF...
  50. pmc A day in the life of a G protein-coupled receptor: the contribution to function of G protein-coupled receptor dimerization
    G Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, Scotland, UK
    Br J Pharmacol 153:S216-29. 2008
    ....
  51. doi Heat stress alters G-protein coupled receptor-mediated function and endothelium-dependent relaxation in rat mesenteric artery
    Jie Li
    Department of Pharmacology, Xi an Jiaotong University College of Medicine, Xi an, Shaanxi 710061, PR China
    Eur J Pharmacol 588:280-5. 2008
    ..In conclusion, heat stress induces an enhanced vascular endothelin ETB-, 5-HT-receptors-mediated contraction, an enhanced CGRP-receptor-induced relaxation and damage to endothelium-dependent relaxation...
  52. pmc Reciprocal regulation of the platelet-derived growth factor receptor-beta and G protein-coupled receptor kinase 5 by cross-phosphorylation: effects on catalysis
    Xinjiang Cai
    Departments of Medicine Cardiology, Duke University Medical Center, Durham, North Carolina, USA
    Mol Pharmacol 75:626-36. 2009
    ..We conclude that GRK5 tyrosyl phosphorylation is required for the activation of GRK5 by the PDGFRbeta, but not by the beta(2)-adrenergic receptor, and that by activating GRK5, the PDGFRbeta triggers its own desensitization...
  53. pmc Myocardial adeno-associated virus serotype 6-betaARKct gene therapy improves cardiac function and normalizes the neurohormonal axis in chronic heart failure
    Giuseppe Rengo
    Center for Translational Medicine, Thomas Jefferson University, Philadelphia, PA 19107, USA
    Circulation 119:89-98. 2009
    ..This study was designed to evaluate long-term betaARKct expression in HF with the use of stable myocardial gene delivery with adeno-associated virus serotype 6 (AAV6)...
  54. doi [Apelin signalisation and vascular physiopathology]
    Bernard Masri
    Unité INSERM U858, Institut de Medecine Moleculaire de Rangueil, BP 84225, 31432 Toulouse, France
    J Soc Biol 203:171-9. 2009
    ..Taken together, apelin signalling is both involved in physiological angiogenesis and pathological neoangiogenesis, and therefore represents an interesting pharmacological target for anti-angiogenic therapies...
  55. pmc Role of helix 8 of the thyrotropin-releasing hormone receptor in phosphorylation by G protein-coupled receptor kinase
    Austin U Gehret
    Department of Pharmacology and Physiology, University of Rochester Medical Center, Rochester, NY 14642, USA
    Mol Pharmacol 77:288-97. 2010
    ..The results indicate that positive residues in helix 8 of GPCRs are important for GRK-dependent phosphorylation...
  56. ncbi Desensitization of human renal D1 dopamine receptors by G protein-coupled receptor kinase 4
    Hidetsuna Watanabe
    Department of Pathology, University of Virginia Health Sciences Center, Charlottesville, VA 22908, USA
    Kidney Int 62:790-8. 2002
    ..Because the renal D1 receptor is desensitized in genetic hypertension, we sought to determine the mechanism(s) of the desensitization of D1 receptors endogenously expressed in renal proximal tubules...
  57. ncbi Developmental expression of the G protein-coupled receptor 54 and three GnRH mRNAs in the teleost fish cobia
    J Shaik Mohamed
    Marine Science Institute, University of Texas at Austin, 750 Channel View Drive, Port Aransas, Texas 78373, USA
    J Mol Endocrinol 38:235-44. 2007
    ..This finding together with the localization of GPR54 mRNAs on GnRH neurons in fish and mammals suggests that the GPR54-GnRH interactions may be conserved in different vertebrate groups...
  58. ncbi A dominant negative mutant of the G protein-coupled receptor kinase 2 selectively attenuates adenosine A2 receptor desensitization
    S J Mundell
    Department of Pharmacology, School of Medical Sciences, University of Bristol, UK
    Mol Pharmacol 51:991-8. 1997
    ....
  59. ncbi The inhibitory gamma subunit of the type 6 retinal cyclic guanosine monophosphate phosphodiesterase is a novel intermediate regulating p42/p44 mitogen-activated protein kinase signaling in human embryonic kidney 293 cells
    K F Wan
    Department of Physiology and Pharmacology, Strathclyde Institute for Biomedical Sciences, University of Strathclyde, 27 Taylor Street, Glasgow G4 ONR, United Kingdom
    J Biol Chem 276:37802-8. 2001
    ..We conclude that PDEgamma is an entirely novel intermediate regulating mitogenic signaling from both receptor tyrosine kinase and G-protein-coupled receptors in human embryonic kidney 293 cells...
  60. ncbi Laser-captured single digoxigenin-labeled neurons of gonadotropin-releasing hormone types reveal a novel G protein-coupled receptor (Gpr54) during maturation in cichlid fish
    Ishwar S Parhar
    Department of Physiology, Nippon Medical School, Sendagi, Tokyo 113 8602, Japan
    Endocrinology 145:3613-8. 2004
    ....
  61. ncbi Kisspeptins are novel potent vasoconstrictors in humans, with a discrete localization of their receptor, G protein-coupled receptor 54, to atherosclerosis-prone vessels
    Emma J Mead
    Clinical Pharmacology Unit, University of Cambridge, Centre for Clinical Investigation, Addenbrooke s Hospital, Cambridge, CB2 2QQ, UK
    Endocrinology 148:140-7. 2007
    ....
  62. ncbi Signaling through a G Protein-coupled receptor and its corresponding G protein follows a stoichiometrically limited model
    Finly Philip
    Department of Physiology and Biophysics, Stony Brook University Medical Center, Stony Brook, New York 11794 8661, USA
    J Biol Chem 282:19203-16. 2007
    ....
  63. doi Endothelium-dependent relaxation by G protein-coupled receptor 30 agonists in rat carotid arteries
    Brad R S Broughton
    Dept of Pharmacology, Monash Univ, Clayton, Victoria, Australia
    Am J Physiol Heart Circ Physiol 298:H1055-61. 2010
    ..Additionally, G-1 appears to directly scavenge superoxide anion...
  64. ncbi G protein-coupled receptor kinases promote phosphorylation and beta-arrestin-mediated internalization of CCR5 homo- and hetero-oligomers
    Friederike Huttenrauch
    Department of Cellular and Molecular Immunology, Georg August University, Gottingen, Germany
    J Biol Chem 280:37503-15. 2005
    ..These results show that GRKs and beta-arrestin are involved in heterologous receptor regulation by cross-phosphorylating and co-internalizing unligated receptors within homo- or hetero-oligomeric protein complexes...
  65. pmc The Epstein-Barr virus BILF1 gene encodes a G protein-coupled receptor that inhibits phosphorylation of RNA-dependent protein kinase
    Patrick S Beisser
    Department of Medical Microbiology, University Hospital Maastricht, Maastricht, The Netherlands
    J Virol 79:441-9. 2005
    ..Neither of the observed effects required a ligand to interact with the BILF1 gene product, suggesting that BILF1 encodes a constitutively active GPCR capable of modulating various intracellular signaling pathways...
  66. ncbi Cloning and characterization of a family C orphan G-protein coupled receptor
    Donghui Kuang
    Department of Pharmaceutical Sciences, University of Toronto, Toronto, Ontario, Canada
    J Neurochem 93:383-91. 2005
    ..24 odorant receptor. These findings suggest that GPRC6A may function as the receptor component of a novel cellular transmitter system in mammals...
  67. ncbi Constitutive ERK1/2 activation by a chimeric neurokinin 1 receptor-beta-arrestin1 fusion protein. Probing the composition and function of the G protein-coupled receptor "signalsome"
    Farahdiba Jafri
    Department of Medicine, Medical University of South Carolina, Charleston, South Carolina 29425, USA
    J Biol Chem 281:19346-57. 2006
    ..These data suggest that beta-arrestin binding to GPCRs nucleates the formation of a stable "signalsome" that functions as a passive scaffold for the ERK1/2 cascade while confining ERK1/2 activity to an extranuclear compartment...
  68. ncbi Expression of G protein-coupled receptor 30 in the hamster ovary: differential regulation by gonadotropins and steroid hormones
    Cheng Wang
    Department of Obstetrics and Gynecology, University of Nebraska Medical Center, 984515 Nebraska Medical Center, Omaha, NE 68198 4515, USA
    Endocrinology 148:4853-64. 2007
    ..The unique pattern of GPR30 expression suggests that gonadotropin-regulated follicular cell functions may involve GPR30 activity...
  69. doi Obestatin induction of early-response gene expression in gastrointestinal and adipose tissues and the mediatory role of G protein-coupled receptor, GPR39
    Jian V Zhang
    Department of Obstetrics and Gynecology, Stanford University School of Medicine, Stanford, California 94305, USA
    Mol Endocrinol 22:1464-75. 2008
    ..The present findings indicate that obestatin is a metabolic hormone capable of binding to GPR39 to regulate the functions of diverse gastrointestinal and adipose tissues...
  70. pmc HK-2 human renal proximal tubule cells as a model for G protein-coupled receptor kinase type 4-mediated dopamine 1 receptor uncoupling
    John J Gildea
    University of Virginia, PO Box 801400, Charlottesville, VA 22908, USA
    Hypertension 56:505-11. 2010
    ..41+/-4.7% and -27.36+/-2.70%; P<0.001; n=6), which express wild-type GRK4. Despite the fact that HK-2 cells retain many functional characteristics of RPTCs, they are not normal from the perspective of dopaminergic function...
  71. ncbi The interleukin-8 receptor is encoded by a neutrophil-specific cDNA clone, F3R
    K M Thomas
    Department of Physiology, Boston University School of Medicine, Massachusetts 02118
    J Biol Chem 266:14839-41. 1991
    ..The molecular characterization of the IL-8 receptor should provide the basis for further studies on the identification of the binding domain of this inflammatory receptor...
  72. ncbi Cloning and expression of a new member of the melanocyte-stimulating hormone receptor family
    P Barrett
    Molecular Neuroendocrinology Group, Rowett Research Institute, Bucksburn, Aberdeen, UK
    J Mol Endocrinol 12:203-13. 1994
    ..These data indicate that this is a new and distinct member of the melanocortin receptor family...
  73. ncbi Molecular characterisation of a putative Atlantic salmon (Salmo salar) odorant receptor
    A Wickens
    Department of Biological Sciences, Brunel University, Uxbridge, UB8 3PH, Middlesex, UK
    Comp Biochem Physiol B Biochem Mol Biol 129:653-60. 2001
    ..Several conserved motifs unique to odorant receptors were also present. Through characterisation of this receptor, we hope to increase the understanding of the mechanisms underlying olfaction in salmonid species...
  74. ncbi G protein-coupled receptor endocytosis in ADP-ribosylation factor 6-depleted cells
    Tanguy Houndolo
    Department of Pharmacology, School of Medicine, University of Montreal, Montreal H3C 3J7, Canada
    J Biol Chem 280:5598-604. 2005
    ..However, this phenomenon is not general. In some cases, another ARF isoform or other proteins may be essential to regulate the endocytic process...
  75. pmc Characterisation of the mouse vasoactive intestinal peptide receptor type 2 gene, Vipr2, and identification of a polymorphic LINE-1-like sequence that confers altered promoter activity
    G Steel
    Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Royal College, 204 George Street, Glasgow, UK
    J Neuroendocrinol 19:14-25. 2007
    ..Our results suggest that the mouse Vipr2 gene may be differentially active in different mouse strains, depending on the presence of this LINE-1-like sequence in the promoter region...
  76. pmc Opposing roles of murine duffy antigen receptor for chemokine and murine CXC chemokine receptor-2 receptors in murine melanoma tumor growth
    Linda W Horton
    Department of Veteran Affairs, Vanderbilt University School of Medicine, Nashville, TN 37232, USA
    Cancer Res 67:9791-9. 2007
    ....
  77. doi Structural basis for ligand binding and specificity in adrenergic receptors: implications for GPCR-targeted drug discovery
    Thomas Huber
    Laboratory of Molecular Biology and Biochemistry, The Rockefeller University, 1230 York Avenue, New York, New York 10065, USA
    Biochemistry 47:11013-23. 2008
    ....
  78. pmc Perivascular human endometrial mesenchymal stem cells express pathways relevant to self-renewal, lineage specification, and functional phenotype
    Trimble L B Spitzer
    Center for Reproductive Sciences, Department of Obstetrics, Gynecology and Reproductive Sciences, University of California, San Francisco, USA
    Biol Reprod 86:58. 2012
    ....
  79. pmc Large multiple transmembrane domain fragments of a G protein-coupled receptor: biosynthesis, purification, and biophysical studies
    Zhanna Potetinova
    Department of Chemistry, College of Staten Island, The City University of New York, Staten Island, NY 10314, USA
    Biopolymers 98:485-500. 2012
    ..05%-trifluoroacetic acid was stable enough to conduct long multidimensional NMR measurements. The entire Ste2p GPCR was not readily reconstituted from the first two and last five or first three and last four transmembrane domains...
  80. doi Stimulation of δ subunit-containing GABAA receptor by DS1 increases GnRH receptor expression but reduces GnRH mRNA expression in GnRH-producing GT1-7 cells
    Unurjargal Sukhbaatar
    Department of Obstetrics and Gynecology, Shimane University School of Medicine, 89 1 Enya, Izumo City, Shimane Prefecture, 693 8501, Japan
    Endocrine 49:222-30. 2015
    ..Stimulation with DS1 increased the expression of GnRH receptor but decreased the basal expression of GnRH mRNA. ..
  81. ncbi Leveraging NMR and X-ray Data of the Free Ligands to Build Better Drugs Targeting Angiotensin II Type 1 G-Protein Coupled Receptor
    Tahsin F Kellici
    Department of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis Zografou 15771, Greece
    Curr Med Chem 23:36-59. 2016
    ..Various aspects derived from these comparisons regarding rational drug design are outlined. ..
  82. ncbi Galpha14 and Galphaq mediate the response to trypsin in Xenopus oocytes
    H Shapira
    Department of Physiology and Pharmacology, Sackler Faculty of Medicine, Tel Aviv University, Ramat Aviv 69978, Israel
    J Biol Chem 273:19431-6. 1998
    ..These results confirm the hypothesis that endogenous members of the Galphaq family discriminate among different native receptors in vivo...
  83. ncbi G-protein-mediated signaling and its control in macrophages and mammalian cells
    P Chakraborty
    Biomembrane Division, Indian Institute of Chemical Biology, Calcutta
    Crit Rev Microbiol 27:1-8. 2001
    ..Recent developments on the activation of phagocytic cells, especially macrophages, via ligation or cross-linking of GPCR and their postreceptor ligation effect against several intramacrophage pathogens are also discussed...
  84. ncbi The role of catecholamines in seizure susceptibility: new results using genetically engineered mice
    David Weinshenker
    Howard Hughes Medical Institute and Department of Biochemistry, University of Washington, Box 357370, Seattle, WA 98195, USA
    Pharmacol Ther 94:213-33. 2002
    ..New results from genetically engineered mice with altered catecholamine signaling, as well as possibilities for future experiments, are discussed...
  85. ncbi GPR54 and puberty
    William H Colledge
    Physiology Department, University of Cambridge, Cambridge, CB2 3EG, UK
    Trends Endocrinol Metab 15:448-53. 2004
    ..Thus, GPR54 is required for normal functioning of the hypothalamic-pituitary-gonadal axis, probably at the level of gonadotrophin-releasing-hormone secretion...
  86. ncbi Src-kinase-dependent epidermal growth factor receptor transactivation in salivary mucin secretion in response to beta-adrenergic G-protein-coupled receptor activation
    Bronislaw L Slomiany
    Research Center, Room C875, University of Medicine and Dentistry of New Jersey, 110 Bergen Street, Newark, NJ 07103 2400, USA
    Inflammopharmacology 12:233-45. 2004
    ....
  87. ncbi Metabolism of amyloid-beta peptide and Alzheimer's disease
    Nobuhisa Iwata
    Laboratory for Proteolytic Neuroscience, RIKEN Brain Science Institute, Wako Shi, Saitama 351 0198, Japan
    Pharmacol Ther 108:129-48. 2005
    ..Thus, it may be possible to pharmacologically control brain Abeta levels with somatostatin receptor agonists...
  88. ncbi Protease-activated receptor-2 regulates vascular endothelial growth factor expression in MDA-MB-231 cells via MAPK pathways
    Yingmei Liu
    Cancer Biology Division, La Jolla Institute for Molecular Medicine, San Diego, CA, USA
    Biochem Biophys Res Commun 344:1263-70. 2006
    ..Collectively, these data suggest that PAR2 signaling through MAPK pathways leads to the production of proangiogenic VEGF in breast cancer cells...
  89. ncbi [Study on the association of single nucleotide polymorphisms and haplotypes of GPR154 gene with allergic asthma in Han nationality in Hubei Chinese population]
    Hong yan Zhu
    Immunology Laboratory, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, Hubei, 430022 PR China
    Zhonghua Yi Xue Yi Chuan Xue Za Zhi 24:48-51. 2007
    ..To investigate whether two polymorphism sites of the G protein-coupled receptor 154 gene (GPR154) are associated with asthma in Han nationality of Hubei province in China...
  90. ncbi Identification of host genes involved in hepatitis C virus replication by small interfering RNA technology
    Teresa I Ng
    Global Pharmaceutical Research and Development, Antiviral Research, Abbott Laboratories, 200 Abbott Park Road, Abbott Park, IL 60064, USA
    Hepatology 45:1413-21. 2007
    ..Of interest, some of these genes are members of the tumor necrosis factor/lymphotoxin signaling pathway...
  91. pmc Type I gamma phosphatidylinositol phosphate kinase is required for EGF-stimulated directional cell migration
    Yue Sun
    Department of Pharmacology, School of Medicine and Public Health, University of Wisconsin Madison, Madison, WI 53706, USA
    J Cell Biol 178:297-308. 2007
    ..These interactions in turn define the spatial and temporal generation of PI4,5P(2) and derived messengers required for directional migration...
  92. pmc G protein-coupled receptor 83 is dispensable for the development and function of regulatory T cells
    Li Fan Lu
    Department of Immunology, University of Washington, Seattle, WA 98195 7650, USA
    Mol Cell Biol 27:8065-72. 2007
    ..Collectively, our results demonstrate that GPR83 is dispensable for Treg-cell development and function...
  93. doi A sexually dimorphic distribution pattern of the novel estrogen receptor G-protein-coupled receptor 30 in some brain areas of the hamster
    Marcello Canonaco
    Comparative Neuroanatomy and Cytology Laboratory and Pharmaco Biology Department, University of Calabria, 87030 Arcavacata di Rende, Cosenza, Italy
    J Endocrinol 196:131-8. 2008
    ....
  94. doi Expression and biophysical analysis of two double-transmembrane domain-containing fragments from a yeast G protein-coupled receptor
    Leah S Cohen
    Department of Chemistry, College of Staten Island, CUNY, NY 10314, USA
    Biopolymers 90:117-30. 2008
    ..These findings set the stage for the determination of the 3D structure of these large domains of a GPCR in micelles using high-resolution NMR...
  95. pmc GIT1 paxillin-binding domain is a four-helix bundle, and it binds to both paxillin LD2 and LD4 motifs
    Ziwei M Zhang
    Department of Structural Biology, St Jude Children s Research Hospital, Memphis, Tennessee 38105, USA
    J Biol Chem 283:18685-93. 2008
    ..These results are in agreement with the notion that phosphorylation of paxillin Ser(272) plays an essential role in regulating focal adhesion turnover...
  96. pmc A RAC/CDC-42-independent GIT/PIX/PAK signaling pathway mediates cell migration in C. elegans
    Mark Lucanic
    Center for Neuroscience, University of California Davis, Davis, California, United States of America
    PLoS Genet 4:e1000269. 2008
    P21 activated kinase (PAK), PAK interacting exchange factor (PIX), and G protein coupled receptor kinase interactor (GIT) compose a highly conserved signaling module controlling cell migrations, immune system signaling, and the formation ..
  97. ncbi Synaptic scaffolding molecule binds to and regulates vasoactive intestinal polypeptide type-1 receptor in epithelial cells
    Heon Yung Gee
    Department of Pharmacology and Brain Korea 21 Project for Medical Science, Institute of Gastroenterology, Yonsei University College of Medicine, Seoul, Korea
    Gastroenterology 137:607-17, 617.e1-4. 2009
    ..We analyzed the association between S-SCAM and VPAC1...
  98. pmc Kisspeptin-10, a KISS1-derived decapeptide, inhibits tumor angiogenesis by suppressing Sp1-mediated VEGF expression and FAK/Rho GTPase activation
    Sung Gook Cho
    Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology and Department of Molecular and Cellular Medicine, Texas A and M University Health Science Center, Houston, Texas 77030, USA
    Cancer Res 69:7062-70. 2009
    ....
  99. pmc Role of membrane integrity on G protein-coupled receptors: Rhodopsin stability and function
    Beata Jastrzebska
    Department of Pharmacology, School of Medicine, Case Western Reserve University, Cleveland, OH 44106 4965, USA
    Prog Lipid Res 50:267-77. 2011
    ..Thus, altering the lipid organization of ROS membranes can result in visual dysfunction and blindness...
  100. doi Role of GPER/GPR30 in tumoral testicular germ cells proliferation
    Nicolas Chevalier
    Institut National de la Santé et de la Recherche Médicale INSER M, Nice, France
    Cancer Biol Ther 12:2-3. 2011
    ..We are sure that this information we obtained by working for several years on a human seminoma cell line will be appreciated by the readers of Cancer Biology & Therapy...
  101. doi Characterization of adenosine receptor in its native environment: insights from molecular dynamics simulations of palmitoylated/glycosylated, membrane-integrated human A(2B) adenosine receptor
    Mahboubeh Mansourian
    Department of Medicinal Chemistry, School of Pharmacy and Isfahan Pharmaceutical Sciences Research Center, Isfahan University of Medical Sciences, Isfahan, Iran
    J Mol Model 18:4309-24. 2012
    ....

Research Grants76

  1. Jeffrey L Benovic; Fiscal Year: 2015
    ..Our proposed research will provide unique mechanistic insight into the biochemical, cellular and molecular function of arrestins and should prove important in understanding the biological function of arrestins and their role in disease...
  2. Endogenous G-Protein Coupled Receptor Antagonists
    Carrie Haskell-Luevano; Fiscal Year: 2012
    ..This research project proposes to generate knowledge for the rational design of molecules as potential therapeutic agents to prevent or treat the diseases associated with over or under eating. ..
  3. Ligand Directed Functional Selectivity of G-Protein Coupled Receptor Signalling
    Gerry S Oxford; Fiscal Year: 2012
    ..As the receptors are important targets for pharmaco-therapies, the outcome of our research will guide the development of more refined and specific drugs for these disorders with fewer side effects. ..
  4. 2010 Ligand Recognition and Molecular Gating Gordon Research Conference
    NANCY RYAN GRAY; Fiscal Year: 2010
    ....
  5. G protein-coupled receptor kinase 3 regulation of leukocyte function in inflammat
    TERESA KATHLEEN TARRANT; Fiscal Year: 2013
    ....
  6. G PROTEIN COUPLED RECEPTOR ACTIVATION STUDIED IN YEAST
    Mark Dumont; Fiscal Year: 2009
    ..The mutant receptors will then be used to determine the effects of oligomerization on signaling function. ..
  7. Brian K Kobilka; Fiscal Year: 2016
    ..The overall goal of this proposal it to develop structure-based approaches to discover new G protein coupled receptor (GPCR) ligands having new signaling properties and specificities...
  8. G Protein Coupled Receptor Modulation of Synaptic Transmission
    EDAENI YISHAK HAMID; Fiscal Year: 2010
    ....
  9. Qin Wang; Fiscal Year: 2016
    ....
  10. Basis of Variability of Lung GPCR Signaling
    Stephen B Liggett; Fiscal Year: 2013
    ..abstract_text> ..
  11. Beta Andrenergic Receptor Structure and Desensitization
    Richard B Clark; Fiscal Year: 2010
    ..modeling of the complex inhibitory feedback loops involving 132AR phosphorylation by PKA and multiple G protein coupled receptor kinase (GRK) subtypes, and their downstream sequelae such as arrestin binding, internalization, and ..
  12. Targeting adenylyl cyclase to prevent L-DOPA-induced dyskinesia
    Xiaoxi Zhuang; Fiscal Year: 2010
    ..Such a lack of CaCaM stimulation of cAMP production and its reliance on G protein coupled receptor activation makes corticostriatal neuroplasticity dependent on dopamine input...
  13. Signaling regulation in the striatum in Parkinson's disease
    Eugenia V Gurevich; Fiscal Year: 2013
    ..The studies will pave the way to development of novel therapeutic approaches to control motor deficits in Parkinsons'disease and complications of L-DOPA therapy. ..
  14. The role of receptor desensitization machinery in psychostimulant addiction
    Eugenia V Gurevich; Fiscal Year: 2012
    ....
  15. Structural Studies in Rhodopsin and G Protein Activation
    DAVID THOMAS LODOWSKI; Fiscal Year: 2011
    ..Furthermore, as rhodopsin is a member of the G protein coupled receptor superfamily, it will serve to explain how important physiological processes, such as sight, smell, taste;..
  16. MLP Assay for Arrestin-AP2 Inhibitors
    Eric R Prossnitz; Fiscal Year: 2012
    ..Such a molecule would be of great benefit for researchers in the field and could find therapeutic utility in its ability to induce apoptosis in hyper stimulated disease cells such as cancer cells. ..
  17. MICHAEL CHRISTIAN ANDRESEN; Fiscal Year: 2014
    ....
  18. Kelly R Monk; Fiscal Year: 2016
    ....
  19. John J G Tesmer; Fiscal Year: 2016
    ....
  20. In Vivo Neuronal Modulation via Engineered G Protein-Coupled Receptors
    SARAH CLAIRE ROGAN; Fiscal Year: 2012
    ..manipulating neuronal GPCR signaling in vivo. Additionally, the particular signaling pathways this proposal will investigate could reveal critical information regarding the etiology and treatment of mental illness. ..
  21. Johannes Reisert; Fiscal Year: 2014
    ....
  22. Jonathan A Javitch; Fiscal Year: 2016
    ....
  23. Raul M Torres; Fiscal Year: 2016
    ....
  24. G Protein Coupled Receptor Regulatory Mechanisms in Arthritis
    TERESA KATHLEEN TARRANT; Fiscal Year: 2010
    ..The effects of GRK inhibition in leukocyte migration and disease pathogenesis could lead to therapies that target GPCR signaling pathways in patients with RA. ..
  25. Towards a structural and temporal understanding of phototransduction
    PAUL S PARK; Fiscal Year: 2010
    ..Understanding the molecular mysteries of these systems will lead to the development of more effective therapeutic solutions. ..
  26. Lakshmi A Devi; Fiscal Year: 2016
    ....
  27. Jeffrey L Benovic; Fiscal Year: 2016
    ..These studies will provide important insight that is highly relevant to not only understanding GRKs in the worm but also to understanding how GRKs function in humans. ..
  28. Sudha K Shenoy; Fiscal Year: 2014
    ..The long-term goal of this project is to understand the molecular mechanisms that integrate G protein-coupled receptor trafficking and signaling, which could play a critical role in balancing physiological responsiveness. ..
  29. G-protein Signaling in Zebrafish Primordial Germ Cell Migration
    Fang Lin; Fiscal Year: 2010
    ..abstract_text> ..
  30. Radiolytic Footprinting Methods for Structural Mass Spectrometry
    Mark R Chance; Fiscal Year: 2013
    ..Advanced technologies to examine the structure and dynamics of all proteins are needed in biology and medicine to better correlate structure and function. ..
  31. Roger K Sunahara; Fiscal Year: 2016
    ..This subaim will further characterize the interactions between these two domains in the ?2AR-Gs complex as well as in GTP and GDP bound states. ..
  32. Olivier Lichtarge; Fiscal Year: 2016
    ..It will benefit human health by providing new approaches to rational drug design and by enhancing the diagnostic value of SNP analysis and human genotyping. ..
  33. Raymond B Penn; Fiscal Year: 2016
    ....
  34. PATRICK DANIEL BARTH; Fiscal Year: 2016
    ..The high-resolution information gained from these studies will set the stage for the rational design of GPCR variants with reprogrammed signaling properties for future structural and functional studies at the system level. ..
  35. Rongshi Li; Fiscal Year: 2015
    ..Finally, we will assess the in vivo efficacy of optimized compounds using animal models for CXCR4-directed metastatic cancer as described in our recent publication in PNAS. This is a key prerequisite for PAR-12-060. ..
  36. Multimeric Ligands for Targeting Melanoma
    David L Morse; Fiscal Year: 2012
    ..They also have advantages over other multifunctional agents in that they are produced via convergent synthesis and hence are relatively small with acceptable ADME characteristics. ..
  37. Jean Pierre Vilardaga; Fiscal Year: 2014
    ....
  38. Robert J Lefkowitz; Fiscal Year: 2016
    ..By understanding the functional signaling consequences and structural basis of [unreadable] arr-biased agonism we will lay the basis for the development of a novel class of therapeutic agents. ..
  39. Shuichi Takayama; Fiscal Year: 2014
    ..Use the experimental observations with mathematical models to delineate mechanisms of action. Aim 4. Disseminate self-regulating chips that make microfluidic phase-locking studies accessible to anyone. ..
  40. Marta Filizola; Fiscal Year: 2016
    ....
  41. Crystallization and structure determination of the angiotensin II type 1 receptor
    Brian K Kobilka; Fiscal Year: 2012
    ..The AT1R is a member of the Class A G protein coupled receptor (GPCR) superfamily that plays important roles in the regulation of cardiovascular function...
  42. Development of Protein Surface Binding, Low Entropy Oligomers
    Christian E Schafmeister; Fiscal Year: 2013
    ..The third target is the seven-transmembrane G-protein coupled receptor GLP-1R: we will develop bis-peptides that act as agonists and antagonists of GLP-1R which could be used to treat type 2 diabetes. ..
  43. Nicola C Partridge; Fiscal Year: 2016
    ..Moreover, it will define how HDACs contribute to this. In so doing, the data will also provide new perspectives into treatment of disorders of calcium metabolism, cancer-associated bone disease and other bone disorders. ..
  44. The mechanism of apelin-APJ mediated increased cardiac contractility
    DAVID NEIGHBOR CHARO; Fiscal Year: 2010
    ..This system warrants further investigation with the aim of developing new therapies to combat human disease. ..
  45. Calcineurin Phosphatase in Cell Signaling Pathways
    Chi Wing Chow; Fiscal Year: 2010
    ..Beta-adrenergic receptors are seven transmembrane receptors belong to the G protein coupled receptor (GPCR) superfamily...
  46. Timothy E McGraw; Fiscal Year: 2016
    ..The GRKs and [unreadable]-arrestins control the internalization/down regulation of activated GPCR's, and therefore control signaling of the GPCRs. ..
  47. Transgenic Targeting of Vascular G Protein Signaling
    Karsten Peppel; Fiscal Year: 2010
    ..Data from these experiments should also increase our understanding of 21AR signaling in the setting of high blood pressure and help in the development of novel antihypertensive therapeutic strategies. ..
  48. Walter J Koch; Fiscal Year: 2015
    ....
  49. TRPV1 regulation by B-arrestins
    ELAINE DARCEY POR; Fiscal Year: 2012
    ..2) Determine the effect of Beta-arrestin knockdown on TRPV1 activity. 3) Investigate Beta-arrestin-scaffolded PDE4D in the regulation of TRPV1. ..
  50. Howard A Rockman; Fiscal Year: 2016
    ..The results will be used to define novel strategies for manipulation of these recently discovered mechanisms for the therapy of patients with heart failure. ..
  51. Regulation of CXCR4 by cognate and non-cognate ligands
    Elias Lolis; Fiscal Year: 2013
    ..This application seeks to understand the mechanism by which proteins function as agonists or antagonists of CXCR4 and the effects that small molecules inhibitors of these proteins have on these functions and on CXCR4. ..
  52. C David Weaver; Fiscal Year: 2015
    ..Identification of small molecule allosteric modulators of Y4 will allow future development of pharmacological probes and can seed drug discovery programs in obesity. ..
  53. Analysis of Radiomitigative Cell Signaling
    Gabor J Tigyi; Fiscal Year: 2012
    ..The objective of this grant application is to elucidate the an- tiapoptotic mechanism of action unique to the LPA2 receptor subtype ..
  54. Louis M Luttrell; Fiscal Year: 2016
    ..This information will be critical to efforts to develop novel therapeutics that exploit ligand bias. ..
  55. FXR, nuclear receptors, and transcriptional regulation of liver homeostasis
    Grace L Guo; Fiscal Year: 2011
    ..The species similarities will provide a scientific basis for selection of relevant translational research of FXR in human liver physiology and diseases. ..
  56. Development of Second Messenger, Trafficking, and Functional Assays for GPR119
    PATRICIA HELEN MCDONALD; Fiscal Year: 2012
    DESCRIPTION (provided by applicant): The G protein coupled receptor GPR119 is a recently deophanized receptor that has emerged as an attractive target for the treatment of obesity and Type 2 Diabetes Mellitus...
  57. Laurence J Miller; Fiscal Year: 2014
    ....
  58. Erin Nevius; Fiscal Year: 2014
    ..Given that GPCRs are prime targets for therapeutic interventions, the proposed studies have the potential to elucidate new aspects of osteoclast biology that should have a translational impact in bone disease. ..
  59. Role of RAMPs in Intermedin Signaling
    Sheau Yu Teddy Hsu; Fiscal Year: 2010
    ....
  60. ROBERT NISSENSON; Fiscal Year: 2015
    ..osteoporosis is intermittent parathyroid hormone which activates two G proteins- Gs and Gq- through a G protein coupled receptor (GPCR) in osteoblasts...
  61. Toshihiro Kitamoto; Fiscal Year: 2014
    ....
  62. REYNOLD ALEXANDER PANETTIERI; Fiscal Year: 2016
    ..abstract_text> ..
  63. PSGR as a Molecular Target in Human Prostate Cancer
    Mingyao Liu; Fiscal Year: 2005
    ..abstract_text> ..
  64. STRUCTURAL STUDIES OF G-PROTEIN COUPLED RECEPTORS
    KEVIN RIDGE; Fiscal Year: 2004
    ....
  65. The Role of Phosphorylation in Photoreceptor Cell Biology
    ELLEN RUTH WEISS; Fiscal Year: 2010
    ..It is anticipated that these studies will lead to a better understanding of cone function advance our ability to prevent cone-related diseases. ..
  66. Transcription & Function of Adipocyte Beta3AR in Obesity
    Sheila Collins; Fiscal Year: 2006
    ..abstract_text> ..
  67. PROTEIN KINASE C AND PHOTORECEPTORS
    ALEXANDRA NEWTON; Fiscal Year: 2002
    ..Specifically, the effect of this phosphorylation on rhodopsin s macromolecular interactions (transducin coupling, arrestin binding) will be explored. ..
  68. SIGNALING PATHWAYS OF ARF GTPASES AND ARF GAPS
    Richard Premont; Fiscal Year: 2005
    ..of biochemical and cell biological techniques to define the functional significance of GIT proteins and GIT- associated proteins as regulators of heterotrimeric G protein coupled receptor signaling and function.
  69. Transition states in G-protein coupled receptor signaling
    T M Iverson; Fiscal Year: 2010
    ..This two year proposal develops a model system to stabilize the complex between the G protein coupled receptor rhodopsin and the G123 heterotrimer.
  70. BETA 3-ADRENOCEPTORS AND MAP KINASE IN ADIPOCYTES
    Sheila Collins; Fiscal Year: 2003
    ..abstract_text> ..
  71. Studies of a Novel CCK-B/Gastrin Receptor Splice Variant
    MARK HELLMICH; Fiscal Year: 2005
    ..Furthermore, these studies may, in the future, provide the basis for the development of innovative therapeutic strategies for the treatment of peptide hormone-sensitive cancers. ..
  72. Targeting crosstalk between insulin and Gq signaling systems in pancreatic cancer
    JUAN ENRIQUE ROZENGURT; Fiscal Year: 2010
    ....
  73. The Role of GPR54 Signaling in Pubertal Disorders
    SUZY DRUMOND CARVALHO BIANCO; Fiscal Year: 2010
    ..These insights, in turn, may contribute to future development of therapies designed to modulate the timing of puberty by manipulating the kisspeptin-GPR54 signaling system. ..
  74. STRUCTURE OF ADENOSINE RECEPTORS
    Jack Wells; Fiscal Year: 2002
    ..abstract_text> ..
  75. Stephen B Liggett; Fiscal Year: 2016
    ..The results of the this effort will help to define the role of beta2AR polymorphisms in determining the severity of the asthma, its response to beta-agonist therapy, and other phenotypic characteristics. ..
  76. SIGNAL TRANSDUCTION OF A G PROTEIN COUPLED RECEPTOR
    Athan Kuliopulos; Fiscal Year: 1999
    ..These studies should provide the basis for understanding how this receptor activates the downstream signaling pathway and will serve as a general model for other G protein/receptor mutant-related human diseases. ..