OXER1

Summary

Gene Symbol: OXER1
Description: oxoeicosanoid (OXE) receptor 1
Alias: GPCR, GPR170, TG1019, 5-oxo-ETE G-protein coupled receptor, 5-oxo-ETE acid G-protein-coupled receptor 1, G-protein coupled receptor 170, G-protein coupled receptor R527, G-protein coupled receptor TG1019, oxoeicosanoid receptor 1
Species: human

Top Publications

  1. doi Up-regulation of G-protein-coupled receptors for endothelin and thromboxane by lipid-soluble smoke particles in renal artery of rat
    Yan hua Xie
    Institute of Materia Medica, School of Pharmacy, Fourth Military Medical University, Xi an, Shaanxi, China
    Basic Clin Pharmacol Toxicol 107:803-12. 2010
  2. pmc Cloning and identification of an oxytocin/vasopressin-like receptor and its ligand from insects
    Elisabeth Stafflinger
    Center for Functional and Comparative Insect Genomics, Department of Biology, University of Copenhagen, Universitetsparken 15, DK 2100 Copenhagen, Denmark
    Proc Natl Acad Sci U S A 105:3262-7. 2008
  3. 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
  4. ncbi Promoting neurotrophic effects by GPCR ligands
    Freddy Jeanneteau
    Molecular Neurobiology Program, Skirball Institute of Biomolecular Medicine, Department of Cell Biology, New York University School of Medicine, NY 10016, USA
    Novartis Found Symp 276:181-9; discussion 189-92, 233-7, 275-81. 2006
  5. pmc N-arachidonoyl glycine, an abundant endogenous lipid, potently drives directed cellular migration through GPR18, the putative abnormal cannabidiol receptor
    Douglas McHugh
    The Department of Psychological and Brain Sciences, Indiana University, Bloomington, IN 47405, USA
    BMC Neurosci 11:44. 2010
  6. ncbi A beta-arrestin binding determinant common to the second intracellular loops of rhodopsin family G protein-coupled receptors
    Sébastien Marion
    Department of Cell Biology, Duke University Medical Center, Durham, North Carolina 27710, USA
    J Biol Chem 281:2932-8. 2006
  7. ncbi Gene expression profiling for the identification of G-protein coupled receptors in human platelets
    Stefan Amisten
    Department of Cardiology, Lund University Hospital, SE 221 85 Lund, Sweden
    Thromb Res 122:47-57. 2008
  8. pmc Involvement of OA1, an intracellular GPCR, and G alpha i3, its binding protein, in melanosomal biogenesis and optic pathway formation
    Alejandra Young
    Jules Stein Eye Institute, University of California, Los Angeles School of Medicine, Los Angeles, California 90095, USA
    Invest Ophthalmol Vis Sci 49:3245-52. 2008
  9. ncbi A review of neurohormone GPCRs present in the fruitfly Drosophila melanogaster and the honey bee Apis mellifera
    Frank Hauser
    Center for Functional and Comparative Insect Genomics, Department of Cell Biology and Comparative Zoology, Institute of Biology, University of Copenhagen, Universitetsparken 15, DK 2100 Copenhagen, Denmark
    Prog Neurobiol 80:1-19. 2006
  10. ncbi Signal transduction pathways of G protein-coupled receptors and their cross-talk with receptor tyrosine kinases: lessons from bradykinin signaling
    C Liebmann
    Institute of Biochemistry and Biophysics, Biological and Pharmaceutical Faculty and Research Group, Molecular Cell Biology, Friedrich Schiller University Jena, Germany
    Curr Med Chem 7:911-43. 2000

Research Grants

  1. Mechanisms Regulating GPCR Trafficking
    JoAnn Trejo; Fiscal Year: 2010
  2. Mechanisms Regulating GPCR Trafficking
    JoAnn Trejo; Fiscal Year: 2010
  3. TYROSINE KINASES IN G PROTEIN MEDIATED SIGNALING
    Louis M Luttrell; Fiscal Year: 2010
  4. TYROSINE KINASES IN G PROTEIN MEDIATED SIGNALING
    Louis M Luttrell; Fiscal Year: 2010
  5. Neuronal-Astrocytic Communication In Vivo
    KEN DOUGLAS MCCARTHY; Fiscal Year: 2010
  6. TYROSINE KINASES IN G PROTEIN MEDIATED SIGNALING
    Louis Luttrell; Fiscal Year: 2009
  7. Neuronal-Astrocytic Communication In Vivo
    Ken McCarthy; Fiscal Year: 2009
  8. G PROTEIN-COUPLED RECEPTOR KINASES
    JEFFREY BENOVIC; Fiscal Year: 2007
  9. G PROTEIN-COUPLED RECEPTOR KINASES
    Jeffrey L Benovic; Fiscal Year: 2010
  10. PKA targeting: A novel mechanism for GPCR resensitization
    SULEIMAN WAKIM BAHOUTH; Fiscal Year: 2010

Detail Information

Publications140 found, 100 shown here

  1. doi Up-regulation of G-protein-coupled receptors for endothelin and thromboxane by lipid-soluble smoke particles in renal artery of rat
    Yan hua Xie
    Institute of Materia Medica, School of Pharmacy, Fourth Military Medical University, Xi an, Shaanxi, China
    Basic Clin Pharmacol Toxicol 107:803-12. 2010
    Up-regulation of G-protein-coupled receptors (GPCR) plays key roles in renal hypertension and cardiovascular disease pathogenesis...
  2. pmc Cloning and identification of an oxytocin/vasopressin-like receptor and its ligand from insects
    Elisabeth Stafflinger
    Center for Functional and Comparative Insect Genomics, Department of Biology, University of Copenhagen, Universitetsparken 15, DK 2100 Copenhagen, Denmark
    Proc Natl Acad Sci U S A 105:3262-7. 2008
    ..for insect oxytocin/vasopressin-like peptide) and a gene coding for an inotocin G protein-coupled receptor (GPCR). We cloned the Tribolium inotocin preprohormone and the inotocin GPCR and expressed the GPCR in CHO cells...
  3. 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 have used reverse transcription-polymerase chain reaction (PCR) to isolate a cDNA from human brain mRNA, GPCR/CNS, that encodes a putative G protein-coupled receptor (GPCR) based upon the presence of the paradigmatic seven ..
  4. ncbi Promoting neurotrophic effects by GPCR ligands
    Freddy Jeanneteau
    Molecular Neurobiology Program, Skirball Institute of Biomolecular Medicine, Department of Cell Biology, New York University School of Medicine, NY 10016, USA
    Novartis Found Symp 276:181-9; discussion 189-92, 233-7, 275-81. 2006
    ..An alternative approach is to use ligands in the G protein-coupled receptor (GPCR) family to transactivate trophic activities...
  5. pmc N-arachidonoyl glycine, an abundant endogenous lipid, potently drives directed cellular migration through GPR18, the putative abnormal cannabidiol receptor
    Douglas McHugh
    The Department of Psychological and Brain Sciences, Indiana University, Bloomington, IN 47405, USA
    BMC Neurosci 11:44. 2010
    ..The endogenous cannabinoid system regulates microglial migration via CB2 receptors and an as yet unidentified GPCR termed the 'abnormal cannabidiol' (Abn-CBD) receptor...
  6. ncbi A beta-arrestin binding determinant common to the second intracellular loops of rhodopsin family G protein-coupled receptors
    Sébastien Marion
    Department of Cell Biology, Duke University Medical Center, Durham, North Carolina 27710, USA
    J Biol Chem 281:2932-8. 2006
    ..and to mediate endocytosis for many of the hundreds of nonvisual rhodopsin family G protein-coupled receptors (GPCR)...
  7. ncbi Gene expression profiling for the identification of G-protein coupled receptors in human platelets
    Stefan Amisten
    Department of Cardiology, Lund University Hospital, SE 221 85 Lund, Sweden
    Thromb Res 122:47-57. 2008
    ..To identify new platelet GPCRs, a platelet gene expression profile was generated and validated using quantitative real-time PCR...
  8. pmc Involvement of OA1, an intracellular GPCR, and G alpha i3, its binding protein, in melanosomal biogenesis and optic pathway formation
    Alejandra Young
    Jules Stein Eye Institute, University of California, Los Angeles School of Medicine, Los Angeles, California 90095, USA
    Invest Ophthalmol Vis Sci 49:3245-52. 2008
    ..The OA1 gene encodes a G-protein-coupled receptor (GPCR) that coimmunoprecipitates with the G alpha i-subunit of heterotrimeric G-proteins from human melanocyte extracts...
  9. ncbi A review of neurohormone GPCRs present in the fruitfly Drosophila melanogaster and the honey bee Apis mellifera
    Frank Hauser
    Center for Functional and Comparative Insect Genomics, Department of Cell Biology and Comparative Zoology, Institute of Biology, University of Copenhagen, Universitetsparken 15, DK 2100 Copenhagen, Denmark
    Prog Neurobiol 80:1-19. 2006
    G protein-coupled receptor (GPCR) genes are large gene families in every animal, sometimes making up to 1-2% of the animal's genome...
  10. ncbi Signal transduction pathways of G protein-coupled receptors and their cross-talk with receptor tyrosine kinases: lessons from bradykinin signaling
    C Liebmann
    Institute of Biochemistry and Biophysics, Biological and Pharmaceutical Faculty and Research Group, Molecular Cell Biology, Friedrich Schiller University Jena, Germany
    Curr Med Chem 7:911-43. 2000
    G protein-coupled receptors (GPCRs) represent a major class of drug targets. Recent investigation of GPCR signaling has revealed interesting novel features of their signal transduction pathways which may be of great relevance to drug ..
  11. ncbi Confocal fluorescence microscopy for high-throughput screening of G-protein coupled receptors
    Ralf Heilker
    Department of Integrated Lead Discovery, Boehringer Ingelheim Pharma GmbH and Co KG, D 88397 Biberach, Germany
    Curr Med Chem 12:2551-9. 2005
    ..Finding compounds that interfere with the ligand-GPCR interaction in a specific and selective way is a major focus of pharmaceutical research today...
  12. ncbi Halothane binding to a G protein coupled receptor in retinal membranes by photoaffinity labeling
    Y Ishizawa
    Departments of Anesthesia, Physiology, and Biochemistry and Biophysics, University of Pennsylvania Medical Center, Philadelphia 19104 4283, USA
    Biochemistry 39:8497-502. 2000
    General anesthetics have been reported to alter the functions of G protein coupled receptor (GPCR) signaling systems...
  13. ncbi S-nitrosoglutathione inhibits alpha1-adrenergic receptor-mediated vasoconstriction and ligand binding in pulmonary artery
    Eva Nozik-Grayck
    Department of Pediatrics, University of Colorado Health Science Center, Denver, CO 80262, USA
    Am J Physiol Lung Cell Mol Physiol 290:L136-43. 2006
    ..via a cGMP-independent mechanism likely involving S-nitrosylation of its G protein-coupled receptor (GPCR) system...
  14. doi Effects of substituents on the NMR features of basic bicyclic ring systems of fluoroquinolone antibiotics and the relationships between NMR chemical shifts, molecular descriptors and drug-likeness parameters
    Milena Jadrijević Mladar Takač
    Faculty of Pharmacy and Biochemistry, University of Zagreb, Zagreb, Croatia
    Acta Pharm 60:237-54. 2010
    ..the volume (V) of computed molecular descriptors (MDs), as well as the G protein-coupled receptor ligand-likeness (GPCR ligand-ls), the ion channel ligand-likeness (ICL-ls), the kinase inhibitor-likeness (KI-ls) and the nuclear ..
  15. pmc Control of PDGF-induced reactive oxygen species (ROS) generation and signal transduction in human lens epithelial cells
    Kate Chao Wei Chen
    Department of Biochemistry, University of Nebraska Lincoln, NE, USA
    Mol Vis 13:374-87. 2007
    ..We investigated the upstream membrane-bound target proteins involved in PDGF-stimulated signal transduction in human lens epithelial cell (HLE B3), using specific inhibitors and transfected cells...
  16. ncbi The stability of the G protein-coupled receptor-beta-arrestin interaction determines the mechanism and functional consequence of ERK activation
    Akira Tohgo
    Department of Medicine, Duke University Medical Center, Durham, North Carolina 27710, USA
    J Biol Chem 278:6258-67. 2003
    ..Recent data suggest that beta-arrestins also contribute to GPCR signaling by acting as scaffolds for components of the ERK mitogen-activated protein kinase cascade...
  17. ncbi Expression of terminally glycosylated calcitonin receptor-like receptor in uterine leiomyoma: endothelial phenotype and association with microvascular density
    Leonid L Nikitenko
    Nuffield Department of Obstetrics and Gynaecology, The University of Oxford, John Radcliffe Hospital, Oxford, United Kingdom
    Clin Cancer Res 12:5648-58. 2006
    ..Calcitonin receptor-like receptor (CL) is a G protein-coupled receptor (GPCR) that mediates effects of AM, but little information is available on its expression and functional state in human ..
  18. ncbi Compartmentation of G-protein-coupled receptors and their signalling components in lipid rafts and caveolae
    P A Insel
    Department of Anesthesiology Graduate Program, University of California, San Diego, La Jolla, CA 92093, USA
    Biochem Soc Trans 33:1131-4. 2005
    G-protein-coupled receptors (GPCRs) and post-GPCR signalling components are expressed at low overall abundance in plasma membranes, yet they evoke rapid, high-fidelity responses...
  19. ncbi A homogeneous enzyme fragment complementation cyclic AMP screen for GPCR agonists
    Rajasree Golla
    Drug Discovery, Pharmaceutical Research Institute, Bristol Myers Squibb, Princeton, NJ, USA
    J Biomol Screen 7:515-25. 2002
    ..An added advantage of this assay is that the cAMP is measured as a positive signal, thereby reducing the incidence of false positives...
  20. doi Coupling mechanism of a GPCR and a heterotrimeric G protein during chemoattractant gradient sensing in Dictyostelium
    Xuehua Xu
    Chemotaxis Signal Section, National Institutes of Health, Rockville, MD 20852, USA
    Sci Signal 3:ra71. 2010
    ..guanine nucleotide-binding protein (G protein)-coupled receptors (GPCRs) with G proteins is fundamental for GPCR signaling; however, the mechanism of coupling is still debated...
  21. doi A concise synthesis of 1,4-dihydro-[1,4]diazepine-5,7-dione, a novel 7-TM receptor ligand core structure with melanocortin receptor agonist activity
    Jerzy R Szewczyk
    Department of Medicinal Chemistry, Five Moore Drive, PO Box 13398, Research Triangle Park, NC 27709 3398, USA
    Bioorg Med Chem 18:1822-33. 2010
    Finding small non-peptide molecules for G protein-coupled receptors (GPCR) whose endogenous ligands are peptides, is a very important task for medicinal chemists...
  22. ncbi Fine tuning of blood pressure by the regulator of G protein signaling (RGS) 2
    Andrey Ch da Costa Goncalves
    Max Delbruck Center for Molecular Medicine, Berlin, Germany
    J Am Soc Hypertens 2:403-9. 2008
    ..One of the key steps in the GPCR signaling cascade is the phosphorylation of the Galpha-subunit that triggers its dissociation from the Gbetagamma-..
  23. ncbi Evolving concepts in G protein-coupled receptor endocytosis: the role in receptor desensitization and signaling
    S S Ferguson
    The John P Robarts Research Institute and Department of Physiology, University of Western Ontario, London, Ontario, Canada
    Pharmacol Rev 53:1-24. 2001
    ..Agonist activation of GPCRs also initiates processes that are involved in the feedback desensitization of GPCR responsiveness, the internalization of GPCRs, and the coupling of GPCRs to heterotrimeric G protein-independent ..
  24. doi Fusion proteins as model systems for the analysis of constitutive GPCR activity
    Erich H Schneider
    Laboratory of Molecular Immunology, NIAID NIH, Bethesda, Maryland, USA
    Methods Enzymol 485:459-80. 2010
    ..Moreover, for a detailed characterization of GPCR/G-protein interactions, it may be required to work with a defined GPCR/G-protein stoichiometry and to avoid cross-..
  25. ncbi Drug design strategies for targeting G-protein-coupled receptors
    Thomas Klabunde
    Aventis Pharma Deutschland GmbH, DI and A LG Chemistry, Computational Chemistry, Industriepark Hoechst, Building G878, 65926 Frankfurt am Main, Germany
    Chembiochem 3:928-44. 2002
    ..ligands (chemical ligand space) enables novel drug design strategies to accelerate the finding and optimization of GPCR leads: The crystal structure of rhodopsin provides the first three-dimensional GPCR information, which now supports ..
  26. pmc Arrestin orchestrates crosstalk between G protein-coupled receptors to modulate the spatiotemporal activation of ERK MAPK
    David Cervantes
    Department of Molecular and Integrative Physiology, University of Illinois at Urbana Champaign, Urbana, IL 61801, USA
    Circ Res 106:79-88. 2010
    ..Despite extensive studies investigating the regulation of single GPCR signaling cascades, the effects of concomitant GPCR activation on downstream signaling and cellular function remain ..
  27. ncbi Insights into the viral G protein-coupled receptor encoded by human herpesvirus type 8 (HHV-8)
    Jean Pierre Couty
    Institut Cochin, Departement de Biologie Cellulaire, 22 rue Mechain, 75014 Paris, France
    Biol Cell 96:349-54. 2004
    HHV-8-GPCR is a chemokine-like receptor encoded by KSHV, the etiologic agent of KS. HHV-8-GPCR is constitutively active. Although it is homologous to mammalian CXCR2, it binds CXC and CC chemokines...
  28. ncbi Beta-arrestin1 and beta-arrestin2 are differentially required for phosphorylation-dependent and -independent internalization of delta-opioid receptors
    Xiaoqing Zhang
    Pharmacology Research Center, Shanghai Medical College, Shanghai, China
    J Neurochem 95:169-78. 2005
    Beta-arrestins are key negative regulators and scaffolds of G protein-coupled receptor (GPCR) signalling...
  29. pmc Sequential protein kinase C (PKC)-dependent and PKC-independent protein kinase D catalytic activation via Gq-coupled receptors: differential regulation of activation loop Ser(744) and Ser(748) phosphorylation
    Rodrigo Jacamo
    Department of Medicine, David Geffen School of Medicine, UCLA, Los Angeles, California 90095, USA
    J Biol Chem 283:12877-87. 2008
    Protein kinase D (PKD) is a serine/threonine protein kinase rapidly activated by G protein-coupled receptor (GPCR) agonists via a protein kinase C (PKC)-dependent pathway...
  30. ncbi Constitutive activity of G-protein coupled receptors: emphasis on serotonin receptors
    Milt Teitler
    Center for Neuroscience and Neuropharmacology, Albany Medical College, 47 New Scotland Avenue, Albany, N Y 12208, USA
    Curr Top Med Chem 2:529-38. 2002
    Several lines of evidence indicate that G-protein coupled receptors (GPCR) may exist in a state that allows a tonic level of stimulation in vivo (constitutive activity)...
  31. ncbi Regulated expression of G protein-coupled receptor kinases (GRK's) and beta-arrestins in osteoblasts
    R F Spurney
    Division of Nephrology, Department of Medicine, Duke University and Durham VA Medical Centers, Durham, NC 27710, USA
    Calcif Tissue Int 73:153-60. 2003
    Desensitization of G-protein coupled receptors (GPCR's) is largely mediated by a family of enzymes and protein co-factors termed GRKs and arrestins, respectively...
  32. ncbi Criteria for confirming sequence periodicity identified by Fourier transform analysis: application to GCR2, a candidate plant GPCR?
    Christopher J R Illingworth
    Department of Biological Sciences, University of Essex, Wivenhoe Park, Colchester, CO4 3SQ, United Kingdom
    Biophys Chem 133:28-35. 2008
    ..The method has been applied to G-protein coupled receptor (GPCR) sequences, by Fourier transformation of hydrophobicity values, codon frequencies and the extent of over-..
  33. doi Modeling molecular mechanisms of binding of the anaphylatoxin C5a to the C5a receptor
    Gregory V Nikiforovich
    Center for Computational Biology, Department of Biochemistry and Molecular Biophysics, Washington University Medical School, St Louis, Missouri 63110, USA
    Biochemistry 47:3117-30. 2008
    ..This is the first 3D model of a G-protein-coupled receptor (GPCR) complex with a peptide ligand deduced by a molecular modeling procedure analyzing various conformational ..
  34. ncbi Formation of new genes explains lower intron density in mammalian Rhodopsin G protein-coupled receptors
    Davids Fridmanis
    Biomedical Research and Study Centre, University of Latvia, Ratsupites 1, Riga, Latvia
    Mol Phylogenet Evol 43:864-80. 2007
    Mammalian G protein-coupled receptor (GPCR) genes are characterised by a large proportion of intronless genes or a lower density of introns when compared with GPCRs of invertebrates...
  35. pmc RNA interference screen for RGS protein specificity at muscarinic and protease-activated receptors reveals bidirectional modulation of signaling
    Geneviève Laroche
    Department of Pharmacology, Univ of North Carolina at Chapel Hill, Chapel Hill, NC, USA
    Am J Physiol Cell Physiol 299:C654-64. 2010
    Regulator of G protein signaling (RGS) proteins are considered key modulators of G protein-coupled receptor (GPCR)-mediated signal transduction...
  36. doi Ca2+/calmodulin-dependent protein kinase IIdelta orchestrates G-protein-coupled receptor and electric field stimulation-induced cardiomyocyte hypertrophy
    Wei Zhang
    Department of Pharmacology, Nantong University Medical College, Nantong, China
    Clin Exp Pharmacol Physiol 37:795-802. 2010
    1. G-Protein-coupled receptors (GPCR) and electrical field stimulation (EFS) regulate cardiac function and pathological remodelling, including cardiac hypertrophy...
  37. ncbi c-Cbl mediates ubiquitination, degradation, and down-regulation of human protease-activated receptor 2
    Claire Jacob
    Departments of Surgery and Physiology, University of California, San Francisco, California 94143 0660, USA
    J Biol Chem 280:16076-87. 2005
    Mechanisms that arrest G-protein-coupled receptor (GPCR) signaling prevent uncontrolled stimulation that could cause disease...
  38. ncbi The human formyl peptide receptor as model system for constitutively active G-protein-coupled receptors
    Roland Seifert
    Department of Pharmacology and Toxicology, The University of Kansas, Malott Hall, Room 5064, 1251 Wescoe Hall Drive, Lawrence, KS 66045 7582, USA
    Life Sci 73:2263-80. 2003
    According to the two-state model of G-protein-coupled receptor (GPCR) activation, GPCRs isomerize from an inactive (R) state to an active (R*) state. In the R* state, GPCRs activate G-proteins...
  39. pmc P-selectin cross-links PSGL-1 and enhances neutrophil adhesion to fibrinogen and ICAM-1 in a Src kinase-dependent, but GPCR-independent mechanism
    Tao Xu
    Laboratory of Molecular Cell Biology, Institute of Biochemistry and Cell Biology, Shanghai Institutes for Biological Sciences, The Graduate School of Chinese Academy of Sciences, Shanghai, China
    Cell Adh Migr 1:115-23. 2007
    ..which integrins become activated by extracellular stimuli for their firm adhesion in a G-protein coupled receptor (GPCR)-dependent mechanism...
  40. pmc Activation of calcitonin receptor and calcitonin receptor-like receptor by membrane-anchored ligands
    Chia Lin Chang
    Reproductive Biology and Stem Cell Research Program, Department of Obstetrics and Gynecology, Stanford University School of Medicine, Stanford, California 94305 5317, USA
    J Biol Chem 285:1075-80. 2010
    ..receptors (GPCRs) are the most important pharmaceutical targets, and more than 40% of drugs in use today modulate GPCR signaling...
  41. pmc Quantification of dynamic protein complexes using Renilla luciferase fragment complementation applied to protein kinase A activities in vivo
    E Stefan
    Département de Biochimie and Institute for Research in Immunology and Cancer, Universite de Montreal, Succursale Centre Ville, Montreal, QC, Canada
    Proc Natl Acad Sci U S A 104:16916-21. 2007
    The G protein-coupled receptor (GPCR) superfamily represents the most important class of pharmaceutical targets. Therefore, the characterization of receptor cascades and their ligands is a prerequisite to discovering novel drugs...
  42. pmc Delayed internalization and lack of recycling in a beta2-adrenergic receptor fused to the G protein alpha-subunit
    Maria Grazia Di Certo
    Istituto di Neurobiologia e Medicina Molecolare, CNR, c o Fondazione Santa Lucia EBRI, via del Fosso di Fiorano 64 65, 00143 Rome, Italy
    BMC Cell Biol 9:56. 2008
    Chimeric proteins obtained by the fusion of a G protein-coupled receptor (GPCR) sequence to the N-terminus of the G protein alpha-subunit have been extensively used to investigate several aspects of GPCR signalling...
  43. ncbi GPCR-induced dissociation of G-protein subunits in early stage signal transduction
    Wayne R Leifert
    CSIRO Molecular and Health Technologies, Adelaide, SA, Australia
    Mol Membr Biol 22:507-17. 2005
    ..e., Galpha and Gbetagamma) following agonist-induced GPCR (alpha(2A)-adrenergic receptor; alpha(2A)-AR) activation in a cell-free assay system...
  44. ncbi G-protein-coupled receptor (GPCR) kinase phosphorylation and beta-arrestin recruitment regulate the constitutive signaling activity of the human cytomegalovirus US28 GPCR
    William E Miller
    Departments of Medicine and Biochemistry, Howard Hughes Medical Institute, Duke University Medical Center, Durham, NC 27710, USA
    J Biol Chem 278:21663-71. 2003
    ..Human cytomegalovirus encodes a GPCR termed US28 that is homologous to the human chemokine family of GPCRs but differs from the cellular receptors in ..
  45. pmc Phospholipids are needed for the proper formation, stability, and function of the photoactivated rhodopsin-transducin complex
    Beata Jastrzebska
    Department of Pharmacology, School of Medicine, Case Western Reserve University, Cleveland, Ohio 44106 4965, USA
    Biochemistry 48:5159-70. 2009
    ..This transient coupling can be stabilized by nucleotide depletion, resulting in an empty-nucleotide G protein-GPCR complex...
  46. pmc A family of chemoreceptors in Tribolium castaneum (Tenebrionidae: Coleoptera)
    Mohatmed Abdel-latief
    Department of Applied Zoology, Animal Ecology, Institute of Biology, Freie Universitat Berlin, Berlin, Germany
    PLoS ONE 2:e1319. 2007
    Chemoperception in invertebrates is mediated by a family of G-protein-coupled receptors (GPCR). To date nothing is known about the molecular mechanisms of chemoperception in coleopteran species...
  47. ncbi A beta-arrestin/green fluorescent protein biosensor for detecting G protein-coupled receptor activation
    L S Barak
    Howard Hughes Medical Institute Laboratories and Department of Cell Biology, Duke University Medical Center, Durham, North Carolina 27710, USA
    J Biol Chem 272:27497-500. 1997
    G protein-coupled receptors (GPCR) represent the single most important drug targets for medical therapy, and information from genome sequencing and genomic data bases has substantially accelerated their discovery...
  48. ncbi Galphaq-coupled receptor internalization specifically induced by Galphaq signaling. Regulation by EBP50
    Moulay Driss Rochdi
    Service de Rhumatologie, Faculté de Médecine and Centre de Recherche Clinique, Universite de Sherbrooke, Sherbrooke, Quebec J1H 5N4, Canada
    J Biol Chem 278:17827-37. 2003
    ..TPbeta receptor internalization, which could not be reversed by overexpression of G protein-coupled receptor (GPCR) kinases and arrestins...
  49. ncbi Mechanisms of desensitization of the adrenocorticotropin response to arginine vasopressin in ovine anterior pituitary cells
    A Hassan
    School of Biological Sciences, University of Canterbury, Christchurch, New Zealand
    J Endocrinol 184:29-40. 2005
    ..the anterior pituitary via activation of the V1b vasopressin receptor, a member of the G protein-coupled receptor (GPCR) family...
  50. ncbi Proteome-wide classification and identification of mammalian-type GPCRs by binary topology pattern
    Yasuhito Inoue
    Department of Electronic and Information System Engineering, Faculty of Science and Technology, Hirosaki University, Hirosaki 036 8550, Japan
    Comput Biol Chem 28:39-49. 2004
    ..Here, we developed a stepwise binary topology pattern (BTP) method for GPCR classification and identification and used it to identify and classify mammalian-type GPCRs in the genomes of 10 ..
  51. pmc Visual arrestin interaction with clathrin adaptor AP-2 regulates photoreceptor survival in the vertebrate retina
    Hormoz Moaven
    Neuroscience Graduate Program, Zilkha Neurogenetic Institute, Keck School of Medicine, University of Southern California, Los Angeles, CA 90033, USA
    Proc Natl Acad Sci U S A 110:9463-8. 2013
    ..Additionally, nonvisual arrestin/GPCR complex can initiate G protein-independent intracellular signals through their ability to act as scaffolds that ..
  52. ncbi The role of GPCR dimerisation/oligomerisation in receptor signalling
    G Milligan
    Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, G12 8QQ Glasgow, Scotland, UK
    Ernst Schering Found Symp Proc . 2006
    ..approaches, including co-immunoprecipitation of differentially epitope-tagged but co-expressed forms of the same GPCR, co-operativity in ligand binding and a variety of resonance energy transfer techniques (Milligan and Bouvier 2005)...
  53. doi How the Dynamic Properties and Functional Mechanisms of GPCRs Are Modulated by Their Coupling to the Membrane Environment
    Sayan Mondal
    Department of Physiology and Biophysics, Weill Cornell Medical College, Cornell University, Room E 509, 1300 York Avenue, 10065, New York City, NY, USA
    Adv Exp Med Biol 796:55-74. 2014
    ..Here we review findings that offer insight into how membrane-GPCR coupling is connected to the structural characteristics of the GPCR, from sequence to 3D structural detail, and how ..
  54. pmc T cell homeostasis requires G protein-coupled receptor-mediated access to trophic signals that promote growth and inhibit chemotaxis
    Ryan M Cinalli
    Abramson Family Cancer Research Institute, Departments of Cancer Biology and Medicine, University of Pennsylvania, Philadelphia, USA
    Eur J Immunol 35:786-95. 2005
    Signals that regulate T cell homeostasis are not fully understood. G protein-coupled receptors (GPCR), such as the chemokine receptors, may affect homeostasis by direct signaling or by guiding T cell migration to distinct location-..
  55. pmc GRIFFIN: a system for predicting GPCR-G-protein coupling selectivity using a support vector machine and a hidden Markov model
    Yukimitsu Yabuki
    Computational Biology Research Center, National Institute of Advanced Industrial Science and Technology AIST, 2 42 Aomi, Koto ku, Tokyo 135 0064, Japan
    Nucleic Acids Res 33:W148-53. 2005
    ..GRIFFIN (G-protein and Receptor Interaction Feature Finding INstrument), that predicts G-protein coupled receptor (GPCR) and G-protein coupling selectivity based on a support vector machine (SVM) and a hidden Markov model (HMM) with ..
  56. ncbi Identification of endogenous surrogate ligands for human P2Y receptors through an in silico search
    Takeshi Hiramoto
    Laboratory of Pharmcoinformatics, Department of Bioscience and Biotechnology, College of Science and Engineering, Ritsumeikan University, Kusatsu, Shiga, Japan
    J Pharmacol Sci 95:81-93. 2004
    ..receptors (GPCRs) are distributed widely throughout the human body, and nearly 50% of current medicines act on a GPCR. GPCRs are considered to consist of seven transmembrane alpha-helices that form an alpha-helical bundle in which ..
  57. ncbi Quantitative and dynamic analyses of G protein-coupled receptor signaling in yeast using Fus1, enhanced green fluorescence protein (EGFP), and His3 fusion protein
    Jun Ishii
    Department of Molecular Science and Material Engineering, Graduate School of Science and Technology, Kobe University, Nada Ku, Japan
    Biotechnol Prog 22:954-60. 2006
    The mechanism of G protein-coupled receptor (GPCR) signaling in yeasts is similar to that in mammalian cells...
  58. ncbi Implication of Gbetagamma proteins and c-SRC tyrosine kinase in parathyroid hormone-induced signal transduction in rat enterocytes
    Claudia Gentili
    Departamento de Biologia, Bioquimica y Farmacia, Universidad Nacional del Sur, San Juan 670, 8000 Bahia Blanca, Argentina
    J Endocrinol 188:69-78. 2006
    Parathyroid hormone (PTH) interacts in target tissues with a G protein-coupled receptor (GPCR) localized in the plasma membrane...
  59. pmc Detection of G protein-selective G protein-coupled receptor (GPCR) conformations in live cells
    Rabia U Malik
    Department of Cell and Developmental Biology, University of Michigan, Ann Arbor, Michigan 48109, USA
    J Biol Chem 288:17167-78. 2013
    ..this study, we report on a novel class of FRET-based sensors that can detect the ligand/mutagenic stabilization of GPCR conformations that promote interactions with G proteins in live cells...
  60. doi A perspective on more effective GPCR-targeted drug discovery efforts
    Annette Gilchrist
    CSO, Caden Biosciences, 5500 Nobel Drive, Suite 220, Madison, WI 53711, USA 1 608 278 8646 1 608 278 8669
    Expert Opin Drug Discov 3:375-89. 2008
    ..The activation of a GPCR (usually by ligand binding) results in conformational changes that lead to G-protein coupling with subsequent ..
  61. pmc Towards improved quality of GPCR models by usage of multiple templates and profile-profile comparison
    Dorota Latek
    International Institute of Molecular and Cell Biology, Warsaw, Poland
    PLoS ONE 8:e56742. 2013
    ..Nevertheless, low sequence similarity between the GPCR family members is still a serious obstacle not only in template selection but also in providing theoretical models ..
  62. pmc Similarity between class A and class B G-protein-coupled receptors exemplified through calcitonin gene-related peptide receptor modelling and mutagenesis studies
    Shabana Vohra
    School of Biological Sciences, University of Essex, Wivenhoe Park, Colchester, UK
    J R Soc Interface 10:20120846. 2013
    Modelling class B G-protein-coupled receptors (GPCRs) using class A GPCR structural templates is difficult due to lack of homology. The plant GPCR, GCR1, has homology to both class A and class B GPCRs...
  63. doi Direct molecular evolution of detergent-stable G protein-coupled receptors using polymer encapsulated cells
    Daniel J Scott
    Department of Biochemistry, University of Zurich, Winterthurerstrasse 190, 8057 Zurich, Switzerland
    J Mol Biol 425:662-77. 2013
    ..studies as well as in vitro drug screening with purified receptors require detergent solubilization of the GPCR, but typically, these proteins exhibit only low stability in detergent micelles...
  64. pmc Identification of GPCR-interacting cytosolic proteins using HDL particles and mass spectrometry-based proteomic approach
    Ka Young Chung
    Department of Molecular and Cellular Physiology, Stanford University, Medical School, Beckman Center, Stanford, California, United States of America
    PLoS ONE 8:e54942. 2013
    ..Although the canonical downstream target of an agonist-activated GPCR is a G protein heterotrimer; there is a growing body of evidence suggesting that other signaling molecules interact,..
  65. pmc Why GPCRs behave differently in cubic and lamellar lipidic mesophases
    George Khelashvili
    Department of Physiology and Biophysics, Weill Cornell Medical College of Cornell University, New York, New York 10065, United States
    J Am Chem Soc 134:15858-68. 2012
    ..in the crystallographic determination of structures of transmembrane proteins in the G protein-coupled receptor (GPCR) family have established the lipidic cubic phase (LCP) environment as the medium of choice for growing structure-..
  66. pmc Stimulus bias provides evidence for conformational constraints in the structure of a G protein-coupled receptor
    Karen J Gregory
    Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, and Department of Pharmacology, Monash University, Victoria 3800, Australia
    J Biol Chem 287:37066-77. 2012
    ..It is now clear that a GPCR coupling to these pathways can be regulated selectively by ligands that differentially drive signaling down one ..
  67. doi The anterograde transport of the human neuropeptide Y2 receptor is regulated by a subtype specific mechanism mediated by the C-terminus
    Cornelia Walther
    Institute of Biochemistry, Faculty of Biosciences, Pharmacy and Psychology, Universitat Leipzig, Germany
    Neuropeptides 46:335-43. 2012
    The export of newly synthesized proteins, including G protein-coupled receptors (GPCR), from the endoplasmic reticulum (ER) and further transport to the plasma membrane is a tightly regulated process...
  68. ncbi High content screening for G protein-coupled receptors using cell-based protein translocation assays
    Charlotta Granas
    BioImage A S, Copenhagen, Denmark
    Comb Chem High Throughput Screen 8:301-9. 2005
    ..GPCRs) have been one of the most productive classes of drug targets for several decades, and new technologies for GPCR-based discovery promise to keep this field active for years to come...
  69. ncbi 76 deciphering g-protein coupled receptor network during bovine conceptus development and maternal recognition of pregnancy
    S Mamo
    School of Agriculture, Food Science and Veterinary Medicine, University College Dublin, Belfield, Dublin, Ireland
    Reprod Fertil Dev 24:150. 2011
    G-protein coupled receptors (GPCR) comprise a large protein family of transmembrane receptors that sense molecules outside the cell to activate the signal transduction pathways inside and, ultimately, the cellular responses...
  70. pmc Minireview: G protein-coupled estrogen receptor-1, GPER-1: its mechanism of action and role in female reproductive cancer, renal and vascular physiology
    Edward J Filardo
    Department of Medicine, Rhode Island Hospital and Brown University Medical School, 593 Eddy Street, Aldrich Building Room 708, Providence, Rhode Island 02903, USA
    Endocrinology 153:2953-62. 2012
    Using cDNA cloning strategies commonly employed for G protein-coupled receptors (GPCR), GPCR-30 (GPR30), was isolated from mammalian cells before knowledge of its cognate ligand...
  71. pmc Adaptor protein-2 interaction with arrestin regulates GPCR recycling and apoptosis
    Brant M Wagener
    Department of Cell Biology and Physiology and UNM Cancer Research and Treatment Center, University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA
    Traffic 10:1286-300. 2009
    ..b>GPCR signaling represents an intricate balance between receptor activation, inactivation (desensitization, ..
  72. ncbi 5-HT receptor-associated protein networks: new targets for drug discovery in psychiatric disorders?
    Philippe Marin
    Institut de Genomique Fonctionnelle, 141 rue de la Cardonille, Montpellier F 34094 Montpellier Cedex 5, France
    Curr Drug Targets 13:28-52. 2012
    ..Except for 5-HT3 receptors, which are cationic channels, 5-HT receptors belong to the G protein-coupled receptor (GPCR) superfamily and allow an extraordinarily diverse and complex pattern of cellular signalling...
  73. pmc Prenylation-deficient G protein gamma subunits disrupt GPCR signaling in the zebrafish
    Timothy Mulligan
    Carnegie Institution, Department of Embryology, Johns Hopkins University, Baltimore, MD 21218, United States
    Cell Signal 22:221-33. 2010
    ..membrane localization of heterotrimeric G proteins and for functional heterotrimeric G protein coupled receptor (GPCR) signaling...
  74. doi TRPC channels in pheromone sensing
    Kirill Kiselyov
    Department of Biological Sciences, University of Pittsburgh, Pittsburgh, Pennsylvania, USA
    Vitam Horm 83:197-213. 2010
    ..relies on an amplification cascade that is triggered by pheromone binding to G protein-coupled receptors (GPCR)...
  75. pmc Metformin disrupts crosstalk between G protein-coupled receptor and insulin receptor signaling systems and inhibits pancreatic cancer growth
    Krisztina Kisfalvi
    Departments of Medicine, CURE, Digestive Diseases Research Center, Molecular Biology Institute, University of California at Los Angeles, 90095 1786, USA
    Cancer Res 69:6539-45. 2009
    Recently, we identified a novel crosstalk between insulin and G protein-coupled receptor (GPCR) signaling pathways in human pancreatic cancer cells. Insulin enhanced GPCR signaling through a rapamycin-sensitive mTOR-dependent pathway...
  76. pmc Determination of adenosine A1 receptor agonist and antagonist pharmacology using Saccharomyces cerevisiae: implications for ligand screening and functional selectivity
    Gregory D Stewart
    Monash Institute of Pharmaceutical Sciences, Parkville, Victoria, Australia
    J Pharmacol Exp Ther 331:277-86. 2009
    ..protein-coupled receptors (GPCRs) to the pheromone response pathway to facilitate empirical ligand screening and/or GPCR mutagenesis studies...
  77. doi A preformed signaling complex mediates GnRH-activated ERK phosphorylation of paxillin and FAK at focal adhesions in L beta T2 gonadotrope cells
    Masha Dobkin-Bekman
    Department of Biochemistry, George S Wise Faculty of Life Sciences, Tel Aviv University, Tel Aviv 69978, Israel
    Mol Endocrinol 23:1850-64. 2009
    ..Also, most GPCR ligands utilize families of receptors for mediation of diverse biological actions; however, the mammalian type I ..
  78. ncbi Targeting platelet G-protein coupled receptors (GPCRs): looking beyond conventional GPCR antagonism
    Louisa Dowal
    Division of Hemostasis and Thrombosis, Department of Medicine, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA 02215, USA
    Curr Vasc Pharmacol 8:140-54. 2010
    ..A more detailed understanding of GPCR function is leading to the development of pharmacophores with novel mechanisms of drug action...
  79. doi Study of GPCR-protein interactions by BRET
    Martina Kocan
    Drug Discovery Biology Laboratory, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Melbourne, Royal Parade, Parkvile, Victoria, Australia
    Methods Mol Biol 746:357-71. 2011
    ..This technique is highly amenable to the monitoring of G protein-coupled receptor (GPCR)-protein interactions, especially involving scaffolding, regulatory and signaling proteins, such as β-arrestins, ..
  80. pmc Human cannabinoid 1 GPCR C-terminal domain interacts with bilayer phospholipids to modulate the structure of its membrane environment
    Elvis K Tiburu
    Center for Drug Discovery and Department of Chemistry and Chemical Biology, Northeastern University, 360 Huntington Avenue, 116 Mugar Hall, Boston, Massachusetts 02115 5000, United States of America
    AAPS J 13:92-8. 2011
    G protein-coupled receptors (GPCRs) play critical physiological and therapeutic roles. The human cannabinoid 1 GPCR (hCB1) is a prime pharmacotherapeutic target for addiction and cardiometabolic disease...
  81. pmc Mechanism and function of Drosophila capa GPCR: a desiccation stress-responsive receptor with functional homology to human neuromedinU receptor
    Selim Terhzaz
    Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, United Kingdom
    PLoS ONE 7:e29897. 2012
    The capa peptide receptor, capaR (CG14575), is a G-protein coupled receptor (GPCR) for the D. melanogaster capa neuropeptides, Drm-capa-1 and -2 (capa-1 and -2)...
  82. doi Separation and reformation of cell surface dopamine receptor oligomers visualized in cells
    Brian F O'Dowd
    Centre for Addiction and Mental Health, University of Toronto, Toronto, Ontario, Canada
    Eur J Pharmacol 658:74-83. 2011
    ..We developed a method designed to study the formation and regulation of G protein coupled receptor (GPCR) oligomers in cells, using a GPCR into which a nuclear localization sequence (NLS) had been inserted...
  83. pmc Mass spectrometry-based GPCR proteomics: comprehensive characterization of the human cannabinoid 1 receptor
    Nikolai Zvonok
    Northeastern University, Center for Drug Discovery, 116 Mugar Life Sciences Building, Boston, Massachusetts 02115, USA
    J Proteome Res 9:1746-53. 2010
    The human cannabinoid 1 receptor (hCB1), a ubiquitous G protein-coupled receptor (GPCR), transmits cannabinergic signals that participate in diverse (patho)physiological processes...
  84. doi Thymoquinone from nutraceutical black cumin oil activates Neu4 sialidase in live macrophage, dendritic, and normal and type I sialidosis human fibroblast cells via GPCR Galphai proteins and matrix metalloproteinase-9
    Trisha M Finlay
    Department of Microbiology and Immunology, Queen s University, Kingston, ON, K7L3N6, Canada
    Glycoconj J 27:329-48. 2010
    ..Pertussis toxin (PTX), a specific inhibitor of Galphai proteins of G-protein coupled receptor (GPCR) and the broad range inhibitors of matrix metalloproteinase (MMP) galardin and piperazine applied to live BMC-2, ..
  85. pmc Exploring a role for heteromerization in GPCR signalling specificity
    Raphael Rozenfeld
    Department of Pharmacology and Systems Therapeutics, Mount Sinai School of Medicine, New York, NY 10029, USA
    Biochem J 433:11-8. 2011
    ..Recent advances in GPCR pharmacology have demonstrated that different ligands binding to the same receptor can activate discrete sets of ..
  86. doi The year in G protein-coupled receptor research
    Robert P Millar
    Medical Research Council MRC Human Reproductive Sciences Unit, The Queen s Medical Research Institute, Edinburgh, Scotland, United Kingdom
    Mol Endocrinol 24:261-74. 2010
    ..From these recent technical advances, we can anticipate that many more GPCR structures will emerge, which will afford us greater insight into their common and unique structural features and, ..
  87. doi GRIPDB - G protein coupled Receptor Interaction Partners DataBase
    Wataru Nemoto
    Computational Biology Research Center CBRC, Advanced Industrial Science and Technology AIST, AIST Tokyo, Japan
    J Recept Signal Transduct Res 31:199-205. 2011
    The G protein Coupled Receptor (GPCR) superfamily is one of the most important pharmaceutical targets. Studies of GPCRs have long been performed under the assumption that GPCRs function as monomers...
  88. ncbi G protein-coupled receptor kinases in normal and failing myocardium
    Zheng Maggie Huang
    Center for Translational Medicine and George Zallie and Family Laboratory for Cardiovascular Gene Therapy, Department of Medicine, Thomas Jefferson University, Philadelphia, PA, USA
    Front Biosci (Landmark Ed) 16:3047-60. 2011
    ..One of the striking characteristics of HF is the desensitization of G protein-coupled receptor (GPCR) signaling, particularly the beta-adrenergic receptor (betaAR) system...
  89. pmc Extracellular osmolarity modulates G protein-coupled receptor-dependent ATP release from 1321N1 astrocytoma cells
    Andrew E Blum
    Department of Physiology and Biophysics, Case Western Reserve University School of Medicine, Cleveland, OH 44120, USA
    Am J Physiol Cell Physiol 298:C386-96. 2010
    ..from 1321N1 human astrocytoma cells could be stimulated either by activation of G protein-coupled receptors (GPCR) or by hypotonic stress. Cheema et al. (Cheema TA, Ward CE, Fisher SK...
  90. doi GPCR-2L: predicting G protein-coupled receptors and their types by hybridizing two different modes of pseudo amino acid compositions
    Xuan Xiao
    Computer Department, Jing De Zhen Ceramic Institute, Jing De Zhen 333403, China
    Mol Biosyst 7:911-9. 2011
    ..The new predictor is called GPCR-2L, where "2L" means that it is a two-layer predictor: the 1st layer prediction engine is to identify a query ..
  91. doi Functional diversity of signaling pathways through G protein-coupled receptor heterodimerization with a species-specific orphan receptor subtype
    Tsubasa Sakai
    Division of Biomolecular Research, Suntory Institute for Bioorganic Research, Osaka, Japan
    Mol Biol Evol 27:1097-106. 2010
    ..several signal transduction cascades via GnRH receptors (GnRHRs), members of the G protein-coupled receptor (GPCR) family...
  92. doi GPCR-CA: A cellular automaton image approach for predicting G-protein-coupled receptor functional classes
    Xuan Xiao
    Computer Department, Jing De Zhen Ceramic Institute, Jing De Zhen 33300, China
    J Comput Chem 30:1414-23. 2009
    Given an uncharacterized protein sequence, how can we identify whether it is a G-protein-coupled receptor (GPCR) or not? If it is, which functional family class does it belong to? It is important to address these questions because GPCRs ..
  93. ncbi Multiple activation steps of the N-formyl peptide receptor
    E R Prossnitz
    Department of Cell Biology and Physiology, University of New Mexico Health Science Center, Albuquerque 87131, USA
    Biochemistry 38:2240-7. 1999
    The human N-formyl peptide receptor (FPR) is representative of a growing family of G protein-coupled receptors (GPCR) that respond to chemokines and chemoattractants...
  94. ncbi Large-scale analysis of gene structure in rhodopsin-like GPCRs: evidence for widespread loss of an ancient intron
    Robert J Bryson-Richardson
    MRC Human Genetics Unit, Western General Hospital, Edinburgh, EH4 2XU, UK
    Gene 338:15-23. 2004
    ..Mammalian GPCR genes are reputed to be largely intron-deficient, but there have been no reports of using genome-wide analyses of ..
  95. pmc Lower rate of genomic variation identified in the trans-membrane domain of monoamine sub-class of Human G-Protein Coupled Receptors: the Human GPCR-DB Database
    Claes Wahlestedt
    Center for Genomics and Bioinformatics, Karolinska Institutet, Berzelius vag 35, 17177 Stockholm, Sweden
    BMC Genomics 5:91. 2004
    ..b>GPCR receptors of physiological and clinical importance were prioritized for statistical analysis...
  96. pmc Ventricular zone gene-1 (vzg-1) encodes a lysophosphatidic acid receptor expressed in neurogenic regions of the developing cerebral cortex
    J H Hecht
    Department of Biology, University of California, San Diego, La Jolla 92093 0636, USA
    J Cell Biol 135:1071-83. 1996
    Neocortical neuroblast cell lines were used to clone G-protein-coupled receptor (GPCR) genes to study signaling mechanisms regulating cortical neurogenesis...
  97. ncbi KSHV-GPCR and CXCR2 transforming capacity and angiogenic responses are mediated through a JAK2-STAT3-dependent pathway
    Meike Burger
    Department of Internal Medicine, Freiburg University Hospital, Freiburg, Germany
    Oncogene 24:2067-75. 2005
    The Kaposi's sarcoma herpesvirus encodes a G-protein-coupled chemokine receptor termed KSHV-GPCR. Expression of this constitutively active GPCR leads to cell transformation and vascular overgrowth characteristic of Kaposi's sarcoma...
  98. ncbi Probing the beta2 adrenoceptor binding site with catechol reveals differences in binding and activation by agonists and partial agonists
    Gayathri Swaminath
    Department of Molecular and Cellular Physiology, Stanford University School of Medicine, 157 Beckman Circle, Stanford, CA 94305, USA
    J Biol Chem 280:22165-71. 2005
    The beta(2) adrenergic receptor (beta(2)AR) is a prototypical family A G protein-coupled receptor (GPCR) and an excellent model system for studying the mechanism of GPCR activation...
  99. pmc S-nitrosothiols modulate G protein-coupled receptor signaling in a reversible and highly receptor-specific manner
    Tarja Kokkola
    Department of Physiology, University of Kuopio, POB 1627, FIN 70211, Kuopio, Finland
    BMC Cell Biol 6:21. 2005
    Recent studies indicate that the G protein-coupled receptor (GPCR) signaling machinery can serve as a direct target of reactive oxygen species, including nitric oxide (NO) and S-nitrosothiols (RSNOs)...
  100. ncbi Vascular smooth muscle overexpression of G protein-coupled receptor kinase 5 elevates blood pressure, which segregates with sex and is dependent on Gi-mediated signaling
    Janelle R Keys
    Department of Surgery, Duke University Medical Center, Durham, NC, USA
    Circulation 112:1145-53. 2005
    ..In addition, increased levels of G protein-coupled receptor (GPCR) kinases (GRKs), which regulate GPCR signaling, are associated with increased blood pressure (BP).
  101. ncbi Emerging concepts in GPCR function--the influence of cell phenotype on GPCR pharmacology
    Richard M Eglen
    DiscoveRx Corp, 42501 Albrae St, Fremont, CA 94538, USA
    Proc West Pharmacol Soc 48:31-4. 2005
    ..It is now appears that GPCR function is highly dependent upon the cellular environment in which it is expressed...

Research Grants104 found, 100 shown here

  1. Mechanisms Regulating GPCR Trafficking
    JoAnn Trejo; Fiscal Year: 2010
    ..Dysregulated GPCR signaling has been implicated in multiple human pathological conditions, making this receptor class the target of ..
  2. Mechanisms Regulating GPCR Trafficking
    JoAnn Trejo; Fiscal Year: 2010
    ..Dysregulated GPCR signaling has been implicated in multiple human pathological conditions, making this receptor class the target of ..
  3. TYROSINE KINASES IN G PROTEIN MEDIATED SIGNALING
    Louis M Luttrell; Fiscal Year: 2010
    ..receptors (GPCRs) control cell growth, proliferation and differentiation has fundamentally changed our view of GPCR signal transduction...
  4. TYROSINE KINASES IN G PROTEIN MEDIATED SIGNALING
    Louis M Luttrell; Fiscal Year: 2010
    ..receptors (GPCRs) control cell growth, proliferation and differentiation has fundamentally changed our view of GPCR signal transduction...
  5. Neuronal-Astrocytic Communication In Vivo
    KEN DOUGLAS MCCARTHY; Fiscal Year: 2010
    ..We fully anticipated that activating a Gq-linked GPCR definitively localized to astrocytes would lead to effects similar to those reported by ourselves and others using ..
  6. TYROSINE KINASES IN G PROTEIN MEDIATED SIGNALING
    Louis Luttrell; Fiscal Year: 2009
    ..receptors (GPCRs) control cell growth, proliferation and differentiation has fundamentally changed our view of GPCR signal transduction...
  7. Neuronal-Astrocytic Communication In Vivo
    Ken McCarthy; Fiscal Year: 2009
    ..We fully anticipated that activating a Gq-linked GPCR definitively localized to astrocytes would lead to effects similar to those reported by ourselves and others using ..
  8. G PROTEIN-COUPLED RECEPTOR KINASES
    JEFFREY BENOVIC; Fiscal Year: 2007
    ..An important mechanism for controlling GPCR signaling involves stimulus-dependent phosphorylation of the receptor, a process primarily mediated by G protein-..
  9. G PROTEIN-COUPLED RECEPTOR KINASES
    Jeffrey L Benovic; Fiscal Year: 2010
    G protein-coupled receptors (GPCRs) mediate hormonal control of numerous intracellular effectors. GPCR signaling systems are tightly regulated and rapidly attenuate their hormonal responsiveness following activation...
  10. PKA targeting: A novel mechanism for GPCR resensitization
    SULEIMAN WAKIM BAHOUTH; Fiscal Year: 2010
    ..Increased sympathetic tone impinges on G protein-coupled receptors (GPCR) such as the 1- AR to promote their desensitization and internalization...
  11. PKA targeting: A novel mechanism for GPCR resensitization
    SULEIMAN BAHOUTH; Fiscal Year: 2009
    ..Increased sympathetic tone impinges on G protein-coupled receptors (GPCR) such as the 1- AR to promote their desensitization and internalization...
  12. Rho- and GPCR-mediated signaling through novel cellular effectors
    Joan Heller Brown; Fiscal Year: 2010
    ..second specific aim is to elucidate the role played by increased CCN1/Cyr61 expression in Rho-mediated responses to GPCR agonists...
  13. Molecular basis for the regulation of G protein-coupled receptor kinases
    John J G Tesmer; Fiscal Year: 2010
    ..A family of GPCR kinases (GRKs) modulates the activity of these GPCRs by phosphorylating sites in their cytoplasmic loops and C-..
  14. Tissue Engineering with a Modular RASSL Toolbox
    Bruce R Conklin; Fiscal Year: 2010
    ..helped to establish a growing community of researchers who have engineered new RASSLs to activate all the major GPCR pathways, including Gs, which increases cAMP formation, and Gq, which stimulates calcium mobilization...
  15. Tissue Engineering with a Modular RASSL Toolbox
    Bruce Conklin; Fiscal Year: 2009
    ..helped to establish a growing community of researchers who have engineered new RASSLs to activate all the major GPCR pathways, including Gs, which increases cAMP formation, and Gq, which stimulates calcium mobilization...
  16. Efficient and Sensitive Mining System for G-Protein Coupled Receptors
    Etsuko Moriyama; Fiscal Year: 2009
    ..so-called orphan GPCRs and searching not-yet-discovered GPCRs from genomic information both potentially lead to new GPCR drug discovery...
  17. Efficient and Sensitive Mining System for G-Protein Coupled Receptors
    Etsuko Moriyama; Fiscal Year: 2009
    ..so-called orphan GPCRs and searching not-yet-discovered GPCRs from genomic information both potentially lead to new GPCR drug discovery...
  18. Structure and Dynamics of Beta 2 Adrenoceptor Coupling to Gs
    Brian K Kobilka; Fiscal Year: 2010
    ..The 22 adrenoceptor (22AR) has been one of the most extensively characterized members of the GPCR family...
  19. Basis of Variability of Lung GPCR Signaling
    Stephen B Liggett; Fiscal Year: 2010
    ..During the past 5 years, polymorphisms of individual HASM GPCR genes were identified in a reference population and functionally characterized...
  20. Structure and Dynamics of Beta 2 Adrenoceptor Coupling to Gs
    Brian Kobilka; Fiscal Year: 2009
    ..The 22 adrenoceptor (22AR) has been one of the most extensively characterized members of the GPCR family...
  21. Structure and Dynamics of Beta 2 Adrenoceptor Coupling to Gs
    Brian K Kobilka; Fiscal Year: 2010
    ..The 22 adrenoceptor (22AR) has been one of the most extensively characterized members of the GPCR family...
  22. Atomic-level, large-scale structure prediction of G protein-coupled receptors
    Yang Zhang; Fiscal Year: 2010
    ..Building on the recent success of the threading assemble refinement (TASSER) algorithm for reduced-level GPCR modeling, this proposal seeks to develop new computational methodologies for the generation of experiment- ..
  23. Desensitization of neuronal G-protein coupled receptors
    Jonathon Wetherington; Fiscal Year: 2002
    ..In many cases GPCR desensitization is mediated by a well- conserved mechanism involving receptor phosphorylation, internalization, and ..
  24. ARRESTINS IN G PROTEIN-COUPLE RECEPTOR REGULATION
    JEFFREY BENOVIC; Fiscal Year: 2005
    ..At the level of the receptor, regulation can occur via inhibition of GPCR/G protein coupling (desensitization), redistribution of cell surface receptors (trafficking), or receptor ..
  25. Rho-Dependent COX-2 Expression in Intestinal Cells
    Lee Slice; Fiscal Year: 2007
    ..Therefore, we have proposed a model that envisages a novel Rho-dependent signaling cascade that is activated by GPCR agonists in their target intestinal epithelial cells...
  26. Role of Arrestins in G Protein-Coupled Receptor Regulation
    JEFFREY BENOVIC; Fiscal Year: 2007
    ..At the receptor level, regulation can occur via inhibition of GPCR/G protein coupling (desensitization), redistribution of cell surface receptors (trafficking), or receptor ..
  27. B-Arrestins and GPCR Kinases in Vascular Function/Growth
    Robert Lefkowitz; Fiscal Year: 2005
    ..Following GPCR activation, GPCRs are phosphorylated by one of seven GPCR kinases (GRKs) and then one of two isoforms of b-arrestin ..
  28. G PROTEINS AND SIGNAL TRANSDUCTION IN NEUROSPORA CRASSA
    KATHERINE BORKOVICH; Fiscal Year: 2003
    ..subunits, and also predicts the existence of cAMP, pheromone and glucose-sensing G protein coupled receptors (GPCR's). GNA-1 is required for apical growth, asexual sporulation and female fertility...
  29. G PROTEINS AND SIGNAL TRANSDUCTION IN NEUROSPORA CRASSA
    KATHERINE BORKOVICH; Fiscal Year: 2006
    ..subunits, and also predicts the existence of cAMP, pheromone and glucose-sensing G protein coupled receptors (GPCR's). GNA-1 is required for apical growth, asexual sporulation and female fertility...
  30. Melanocortin-4 Receptor Traffic and Signaling
    Giulia Baldini; Fiscal Year: 2010
    Melanocortin-4 receptor (MC4R) is a G-protein-Coupled Receptor (GPCR) expressed in many areas of the brain including the paraventricular nucleus of the hypothalamus...
  31. Screening Method for GPCRs Related to Appetite
    MARIA MORANO; Fiscal Year: 2007
    ..for high throughput testing of drug compounds from combinatorial libraries that target G-Protein-Coupled Receptors (GPCR's) associated with appetite control and eating behavior...
  32. Physiological Regulation of MLCK in Intact Arteries
    Withrow Gil Wier; Fiscal Year: 2010
    ..of MLCK and regulation of MLCP in relation to 1) myogenic tone and 2) certain G-protein coupled receptors (GPCR) that are known to be important in hypertension...
  33. Structural Basis for Chemokine Function
    Brian F Volkman; Fiscal Year: 2010
    ..least three distinct types of interactions: dimerization, extracellular matrix glycosaminoglycan (GAG) binding, and GPCR activation...
  34. Regulation of alpha2A-adrenergic receptor signaling and trafficking by spinophili
    Qin Wang; Fiscal Year: 2010
    The ?2A-adrenergic receptor (AR) belongs to the large G protein-coupled receptor (GPCR) superfamily...
  35. MECHANISMS OF VISUAL TRANSDUCTION
    EDWARD PUGH; Fiscal Year: 2005
    ..While the molecular mechanism underlying the responses of rods to light - the rod "G protein-coupled receptor (GPCR) phototransduction cascade" - is now largely understood, and cones are known to have a related mechanism, ..
  36. MECHANISMS FOR GPCR TRAFFICKING IN POLARIZED CELLS
    LEE LIMBIRD; Fiscal Year: 2004
    ..from the Applicant's Abstract): These studies address the mechanisms by which G protein-coupled receptors (GPCR) achieve their discrete localization in target cells...
  37. Signaling Pathways in Neuronal Cells
    Marsha Rosner; Fiscal Year: 2009
    ..protein that is expressed from bacteria to man, RKIP inhibits MAP kinase (Raf-MEK-ERK), G protein-coupled receptor (GPCR) kinase and NFkB signaling cascades...
  38. Signaling Pathways in Neuronal Cells
    Marsha R Rosner; Fiscal Year: 2010
    ..protein that is expressed from bacteria to man, RKIP inhibits MAP kinase (Raf-MEK-ERK), G protein-coupled receptor (GPCR) kinase and NFkB signaling cascades...
  39. Compartmentation of Myocyte Adenosine Receptor Signaling
    ROBERT LASLEY; Fiscal Year: 2004
    ..Although the adenosine A1 receptor is a typical G protein coupled receptor (GPCR), it appears to differ from other GPCR in that it exerts no direct effects in ventricular myocardium...