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

Detail Information

Publications201 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. 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...
  14. 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...
  15. 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 ..
  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. 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 ..
  26. 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 ..
  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 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...
  29. 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-..
  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. 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...
  32. 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...
  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. 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...
  35. 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...
  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. 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...
  38. 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...
  39. 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...
  40. 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...
  41. 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...
  42. 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...
  43. 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...
  44. 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...
  45. 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...
  46. 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 ..
  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. doi Expressions and purification of a mature form of recombinant human Chemerin in Escherichia coli
    Di Xiang
    Laboratory of Regeneromics, School of Pharmacy, Shanghai Jiaotong University, Shanghai 200240, PR China
    Protein Expr Purif 69:153-8. 2010
    Chemerin is a novel chemokine that binds to the G protein-coupled receptor (GPCR) ChemR23, also known as chemokine-like receptor 1 (CMKLR1)...
  50. doi GRIP: a server for predicting interfaces for GPCR oligomerization
    Wataru Nemoto
    Computational Biology Research Center CBRC, Advanced Industrial Science and Technology AIST, Koto ku, Tokyo, Japan
    J Recept Signal Transduct Res 29:312-7. 2009
    ..The molecular mechanisms of oligomerization are not fully understood yet, due to the lack of structural data for GPCR complexes...
  51. doi A time-resolved fluorescent lanthanide (Eu)-GTP binding assay for chemokine receptors as targets in drug discovery
    Jean Labrecque
    AnorMED Corp, Langley, BC, Canada
    Methods Mol Biol 552:153-69. 2009
    ..Chemokine receptors are members of the seven-transmembrane, G protein-coupled receptor (GPCR) family...
  52. pmc 7TMRmine: a Web server for hierarchical mining of 7TMR proteins
    Guoqing Lu
    Department of Computer Science, University of Nebraska at Omaha, Omaha, NE 68182, USA
    BMC Genomics 10:275. 2009
    ..The need for new and accurate 7TMR/GPCR prediction tools is paramount with the accelerated rate of acquisition of diverse sequence information...
  53. doi The crystallographic structure of the human adenosine A2A receptor in a high-affinity antagonist-bound state: implications for GPCR drug screening and design
    Veli Pekka Jaakola
    Oulu Biocenter and Department of Biochemistry, University of Oulu, Post Office Box 3000, FIN 90014 Oulu, Finland
    Curr Opin Struct Biol 20:401-14. 2010
    ..state rhodopsin with covalently linked cis-retinal as an inverse agonist provided the first near-atomic view of the GPCR architecture...
  54. doi Analysis of the histamine H2-receptor in human monocytes
    Kristin Werner
    Institute of Pharmacology, Hannover Medical School, Carl Neuberg Strase 1, D 30625 Hannover, Germany Electronic address
    Biochem Pharmacol 92:369-79. 2014
    ..Recently, the classic two-state model describing GPCR activation has been extended to a multiple-state model implying that any ligand stabilizes a ligand-specific ..
  55. pmc Neural regulation of immunity: role of NPR-1 in pathogen avoidance and regulation of innate immunity
    Alejandro Aballay
    Department of Molecular Genetics and Microbiology, Duke University Medical Center, Durham, NC 27710, USA
    Cell Cycle 8:966-9. 2009
    ..of different pathogens, different modes of infection and genome-wide microarrays highlighted the importance of the GPCR NPR-1 in avoidance to certain pathogens and in the regulation of innate immunity...
  56. doi Chapter 6. Plasmon resonance methods in membrane protein biology applications to GPCR signaling
    Zdzislaw Salamon
    Department of Biochemistry and Molecular Biophysics, University of Arizona, Tucson, Arizona, USA
    Methods Enzymol 461:123-46. 2009
    ..In this chapter we outline the instrumentation used for these studies, the experimental methods that allow determination of the structural changes, and thermodynamic and kinetic parameters that can be obtained from these studies...
  57. pmc FTIR analysis of GPCR activation using azido probes
    Shixin Ye
    Laboratory of Molecular Biology and Biochemistry, The Rockefeller University, New York, New York, USA
    Nat Chem Biol 5:397-9. 2009
    ..We used FTIR difference spectroscopy to monitor the azido probe and show that the electrostatic environments of specific interhelical networks change during receptor activation...
  58. doi Detection of physiological activities of G protein-coupled receptor-acting pharmaceuticals in wastewater
    Masaru Ihara
    Research Center for Environmental Quality Management, Graduate School of Engineering, Kyoto University, Otsu, Shiga 520 0811, Japan
    Environ Sci Technol 49:1903-11. 2015
    ..applied the in vitro transforming growth factor-α (TGFα) shedding assay, which accurately and sensitively detect GPCR activation, to investigate the agonistic/antagonistic activities of wastewater extracts against receptors for ..
  59. pmc Identification and functional comparison of seven-transmembrane G-protein-coupled BILF1 receptors in recently discovered nonhuman primate lymphocryptoviruses
    Katja Spiess
    Laboratory for Molecular Pharmacology, Department of Neuroscience and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark Division 12, Measles, Mumps, Rubella, and Viruses Affecting Immunocompromised Patients, Robert Koch Institute, Berlin, Germany
    J Virol 89:2253-67. 2015
    ..BILF1 encoded by human Epstein-Barr virus (EBV) is a 7-transmembrane (7TM) G-protein-coupled receptor (GPCR) with multiple immunomodulatory functions, including attenuation of PKR phosphorylation, activation of G-protein ..
  60. doi A 1,536-well [(35)S]GTPgammaS scintillation proximity binding assay for ultra-high-throughput screening of an orphan galphai-coupled GPCR
    Eric N Johnson
    Department of Automated Biotechnology, Merck Research Laboratories, North Wales, PA 19454, USA
    Assay Drug Dev Technol 6:327-37. 2008
    ..35)S]GTPgammaS) scintillation proximity assay (SPA) binding assay targeting a Galphai-coupled GPCR recombinantly expressed in membranes of Chinese hamster ovary (CHO) cells was developed and miniaturized into 1,536-..
  61. doi Expression of G protein-coupled receptor kinase 4 is associated with breast cancer tumourigenesis
    J Matsubayashi
    Department of Diagnostic Pathology, Tokyo Medical University, Tokyo, Japan
    J Pathol 216:317-27. 2008
    ..GRKs and beta-arrestins are key participants in the canonical pathways leading to phosphorylation-dependent GPCR desensitization, endocytosis, intracellular trafficking and resensitization...
  62. pmc Molecular insights into the dynamics of pharmacogenetically important N-terminal variants of the human β2-adrenergic receptor
    Ganesh Shahane
    CSIR National Chemical Laboratory, Pune, India
    PLoS Comput Biol 10:e1004006. 2014
    The human β2-adrenergic receptor (β2AR), a member of the G-protein coupled receptor (GPCR) family, is expressed in bronchial smooth muscle cells. Upon activation by agonists, β2AR causes bronchodilation and relief in asthma patients...
  63. pmc Intestinal signaling to GABAergic neurons regulates a rhythmic behavior in Caenorhabditis elegans
    Timothy R Mahoney
    Department of Anatomy and Neurobiology, Washington University School of Medicine, St Louis, MO 63110, USA
    Proc Natl Acad Sci U S A 105:16350-5. 2008
    ..Here, we demonstrate that aex-2 encodes a G-protein-coupled receptor (GPCR) and aex-4 encodes an exocytic SNAP25 homologue...
  64. pmc GIT1 mediates VEGF-induced podosome formation in endothelial cells: critical role for PLCgamma
    Jing Wang
    Aab Cardiovascular Research Institute, University of Rochester School of Medicine and Dentistry, Rochester, NY 14642, USA
    Arterioscler Thromb Vasc Biol 29:202-8. 2009
    ..tyrosine kinase receptors (TKRs) such as the epidermal growth factor receptor stimulate G protein-coupled receptor (GPCR) kinase-interacting protein 1 (GIT1) phosphorylation via c-Src, which is required for phospholipase C-gamma (..
  65. doi The expansion of GPCR transactivation-dependent signalling to include serine/threonine kinase receptors represents a new cell signalling frontier
    Danielle Kamato
    Diabetes Complications Laboratory, Discipline of Pharmacy, School of Medical Sciences and Diabetes Complications Group, RMIT University, Bundoora, Vic, 3083, Australia
    Cell Mol Life Sci 72:799-808. 2015
    G protein-coupled receptor (GPCR) signalling is mediated through transactivation-independent signalling pathways or the transactivation of protein tyrosine kinase receptors and the recently reported activation of the serine/threonine ..
  66. pmc Omega-3 fatty acids and other FFA4 agonists inhibit growth factor signaling in human prostate cancer cells
    Ze Liu
    Department of Pharmaceutical Sciences, College of Pharmacy, Washington State University, Spokane, Washington
    J Pharmacol Exp Ther 352:380-94. 2015
    ..The rapid onset of the inhibitory action of EPA suggested involvement of a GPCR. Further studies showed that DU145 and PC-3 cells express mRNA and protein for both FFA4 and FFA1...
  67. pmc Cannabinoid receptor interacting protein (CRIP1a) attenuates CB1R signaling in neuronal cells
    Lawrence C Blume
    Department of Physiology and Pharmacology, Wake Forest University Health Sciences, Winston Salem, NC 27157, USA
    Cell Signal 27:716-26. 2015
    CB1 cannabinoid receptors (CB1R) are one of the most abundantly expressed G protein coupled receptors (GPCR) in the CNS and regulate diverse neuronal functions...
  68. pmc High-resolution modeling of transmembrane helical protein structures from distant homologues
    Kuang Yui M Chen
    Verna and Marrs McLean Department of Biochemistry and Molecular Biology, Baylor College of Medicine, Houston, Texas, United States of America
    PLoS Comput Biol 10:e1003636. 2014
    ..Models of the adenosine A2AR and chemokine CXCR4 receptors were first ranked in GPCR-DOCK blind prediction contests in the receptor structure accuracy category...
  69. pmc Electronic sculpting of ligand-GPCR subtype selectivity: the case of angiotensin II
    Francesca Magnani
    Laboratory of Molecular Biology, Medical Research Council, Cambridge CB2 0QH, United Kingdom
    ACS Chem Biol 9:1420-5. 2014
    b>GPCR subtypes possess distinct functional and pharmacological profiles, and thus development of subtype-selective ligands has immense therapeutic potential...
  70. pmc Adenosine receptors: expression, function and regulation
    Sandeep Sheth
    Department of Pharmacology and Neuroscience, Southern Illinois University School of Medicine, Springfield, IL 62702, USA
    Int J Mol Sci 15:2024-52. 2014
    Adenosine receptors (ARs) comprise a group of G protein-coupled receptors (GPCR) which mediate the physiological actions of adenosine. To date, four AR subtypes have been cloned and identified in different tissues...
  71. pmc Protease-activated receptor-1 modulates hippocampal memory formation and synaptic plasticity
    Antoine G Almonte
    Department of Neurobiology and Evelyn F McKnight Brain Institute, University of Alabama at Birmingham, Birmingham, AL 35294, USA
    J Neurochem 124:109-22. 2013
    Protease-activated receptor-1 (PAR1) is an unusual G-protein coupled receptor (GPCR) that is activated through proteolytic cleavage by extracellular serine proteases...
  72. pmc Engineering a GPCR-ligand pair that simulates the activation of D(2L) by Dopamine
    Nuska Tschammer
    Department of Chemistry and Pharmacy, Emil Fischer Center, Friedrich Alexander University, Schuhstrasse 19, D 91052 Erlangen, Germany
    ACS Chem Neurosci 1:25-35. 2010
    ..The engineered dopamine receptor D(2L) F390(6.52)W in combination with FAUC 185 (5b) provides a new tool to probe GPCR functions selectively in specific cell populations in vitro and in vivo.
  73. pmc The formyl peptide receptor like-1 and scavenger receptor MARCO are involved in glial cell activation in bacterial meningitis
    Benedikt J Braun
    Department of Anatomy and Cell Biology, RWTH Aachen University, Germany
    J Neuroinflammation 8:11. 2011
    ..The chemotactic G-protein-coupled receptor (GPCR) formyl-peptide-receptor like-1 (FPRL1) plays an essential role in the inflammatory responses of host defence ..
  74. pmc Probing the regulation of TASK potassium channels by PI4,5P₂ with switchable phosphoinositide phosphatases
    Moritz Lindner
    Institute of Physiology and Pathophysiology, Department of Neurophysiology, Philipps University, Deutschhausstrasse 1 2, 35037 Marburg, Germany
    J Physiol 589:3149-62. 2011
    ..Here, we address the role of PI(4,5)P2 for G-protein-coupled receptor (GPCR)-mediated TASK inhibition by using recently developed genetically encoded tools to alter phosphoinositide (PI) ..
  75. pmc The extreme C-terminal region of Gαs differentially couples to the luteinizing hormone and beta2-adrenergic receptors
    Geneva Demars
    Department of Biochemistry and Molecular Biology, University of Georgia, Athens, Georgia 30602 7229, USA
    Mol Endocrinol 25:1416-30. 2011
    The mechanisms of G protein coupling to G protein-coupled receptors (GPCR) share general characteristics but may exhibit specific interactions unique for each GPCR/G protein partnership...
  76. pmc RIC8 is a guanine-nucleotide exchange factor for Galpha subunits that regulates growth and development in Neurospora crassa
    Sara J Wright
    Program in Biochemistry and Molecular Biology, Department of Plant Pathology and Microbiology, University of California, Riverside, CA 92521, USA
    Genetics 189:165-76. 2011
    ..Recently, facilitated GDP/GTP exchange by non-GPCR GEFs, such as RIC8, has emerged as an important mechanism for Gα regulation in animals...
  77. doi BacMam system for FRET-based cAMP sensor expression in studies of melanocortin MC1 receptor activation
    Olga Mazina
    University of Tartu, Institute of Chemistry, Tartu, Estonia
    J Biomol Screen 17:1096-101. 2012
    ..G-protein-coupled receptors (GPCRs) and a useful readout molecule to estimate the biological activity of various GPCR-specific agents...
  78. pmc CODA-RET reveals functional selectivity as a result of GPCR heteromerization
    Eneko Urizar
    Center for Molecular Recognition and Departments of Psychiatry and Pharmacology, College of Physicians and Surgeons, Columbia University, New York, New York, USA
    Nat Chem Biol 7:624-30. 2011
    ..a molecular mechanism for functional selectivity in which a drug acts differently at a G protein-coupled receptor (GPCR) protomer depending on the identity of the second protomer participating in the formation of the signaling unit--..
  79. doi Heterocomplex formation of 5-HT2A-mGlu2 and its relevance for cellular signaling cascades
    Hannah K Delille
    Abbott GmbH and Co KG, Neuroscience Research, Global Pharmaceutical Research and Development, Knollstrasse 50, 67061 Ludwigshafen, Germany
    Neuropharmacology 62:2184-91. 2012
    ..Taken together, the formation of GPCR heterocomplexes does not necessarily translate into second messenger effects...
  80. doi Insights into the activation mechanism of the visual receptor rhodopsin
    Steven O Smith
    Department of Biochemistry and Cell Biology, Center for Structural Biology, Stony Brook University, Stony Brook, NY 11794 5215, USA
    Biochem Soc Trans 40:389-93. 2012
    ..dim-light photoreceptor in vertebrates, as well as the common elements that it shares with the large class A GPCR family. However, despite progress, a number of questions remain unanswered about how these receptors are activated.
  81. doi GPCR oligomerization: contribution to receptor biogenesis
    Kathleen Van Craenenbroeck
    Laboratory of Eukaryotic Gene Expression and Signal Transduction LEGEST, Ghent University Ugent, K L Ledeganckstraat 35, 9000, Ghent, Belgium
    Subcell Biochem 63:43-65. 2012
    G protein-coupled receptor (GPCR) export to the plasma membrane is considered to follow the default secretory pathway...
  82. ncbi Progress in the developement of positive allosteric modulators of the metabotropic glutamate receptor 2
    A A Trabanco
    Neuroscience Medicinal Chemistry, Johnson and Johnson, Pharmaceutical Research and Development, Janssen Cilag S A, Calle Jarama 75, Poligono Industrial, Toledo 45007, Spain
    Curr Med Chem 18:47-68. 2011
    The metabotropic glutamate type 2 (mGlu2) receptor is a G-protein coupled receptor (GPCR) expressed on presynaptic nerve terminals where it negatively modulates glutamate and GABA release...
  83. pmc Structure-function studies with G protein-coupled receptors as a paradigm for improving drug discovery and development of therapeutics
    Patrick M McNeely
    Department of Chemical and Biomolecular Engineering, University of Delaware, Newark, DE, USA
    Biotechnol J 7:1451-61. 2012
    ..We also review experimental evidence that suggests there may be multiple ways to target a GPCR - and by extension, membrane proteins - to more effectively target unhealthy phenotypes while reducing the ..
  84. doi Non-raft adenylyl cyclase 2 defines a cAMP signaling compartment that selectively regulates IL-6 expression in airway smooth muscle cells: differential regulation of gene expression by AC isoforms
    Amy S Bogard
    Department of Pharmacology, University of Tennessee Health Science Center, 874 Union Ave, Crowe 115, Memphis, TN, 38163, USA
    Naunyn Schmiedebergs Arch Pharmacol 387:329-39. 2014
    ..IL-6 production by BSMC was induced by Fsk and select G protein-coupled receptor (GPCR) agonists, though IL-6 levels did not directly correlate with global cAMP levels...
  85. pmc Normal autophagic activity in macrophages from mice lacking Gαi3, AGS3, or RGS19
    Ali Vural
    B Cell Molecular Immunology Section, Laboratory of Immunoregulation, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, Maryland, United States of America
    PLoS ONE 8:e81886. 2013
    ..In similar assays we compared macrophages treated or not with pertussis toxin, an inhibitor of GPCR (G-protein couple receptor) triggered Gαi nucleotide exchange...
  86. pmc Reactive oxygen species are required for 5-HT-induced transactivation of neuronal platelet-derived growth factor and TrkB receptors, but not for ERK1/2 activation
    Jeff S Kruk
    Department of Biology, University of Waterloo, Waterloo, Ontario, Canada
    PLoS ONE 8:e77027. 2013
    ..to induce the production of ROS resulting in transactivation of both PDGFβ and TrkB receptors may suggest that instead of a single GPCR to single RTK pathway, a less selective, more global RTK response to GPCR activation is occurring.
  87. pmc Activation of the Cl- channel ANO1 by localized calcium signals in nociceptive sensory neurons requires coupling with the IP3 receptor
    Xin Jin
    Faculty of Biological Sciences, School of Biomedical Sciences, University of Leeds, Leeds LS2 9JT, UK
    Sci Signal 6:ra73. 2013
    ..These ANO1 channels can be selectively activated by the G protein-coupled receptor (GPCR)-induced release of Ca(2+) from intracellular stores but not by Ca(2+) influx through voltage-gated Ca(2+) channels...
  88. doi Role of ßarrestins in bradykinin B2 receptor-mediated signalling
    Brandon Zimmerman
    McGill University Health Center Research Institute, Department of Medicine, Royal Victoria Hospital, 687 Pine Avenue West, Montreal, Quebec, Canada
    Cell Signal 23:648-59. 2011
    ..Receptor recruitment of ßarrestin is also important for GPCR desensitization, internalization and resensitization...
  89. pmc Allosteric modulation of metabotropic glutamate receptors: structural insights and therapeutic potential
    Karen J Gregory
    Department of Pharmacology, Vanderbilt Program in Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232 0697, USA
    Neuropharmacology 60:66-81. 2011
    ..In the absence of a class C GPCR crystal structure, this approach has shown promise with respect to the interpretation of mutagenesis data and ..
  90. pmc A novel experimental strategy to assess the metabolic effects of selective activation of a G(q)-coupled receptor in hepatocytes in vivo
    Jian Hua Li
    PhD, Chief, Molecular Signaling Section, Laboratory of Bioorganic Chemistry, National Institutes of Health, National Institute of Diabetes and Digestive and Kidney Diseases, Building 8A, Room B1A 05, 8 Center Drive MSC 0810, Bethesda, Maryland 20892 0810 or Jianhua Li, PhD, Center for Molecular Medicine, National Institutes of Health, National Heart, Lung, and Blood Institute, Building 10 CRC, Room 5 3216, 10 Center Drive MSC 1454, Bethesda, Maryland 20892 1454 E mail
    Endocrinology 154:3539-51. 2013
    ..of Hep-Rq mice enabled us to determine the metabolic consequences caused by selective activation of a G(q)-coupled GPCR in hepatocytes in vivo...
  91. doi Arrestins and protein ubiquitination
    Reddy Peera Kommaddi
    Department of Medicine, Duke University Medical Center, Durham, North Carolina, USA
    Prog Mol Biol Transl Sci 118:175-204. 2013
    ..7TMR activation leads not only to the recruitment of arrestin proteins upon phosphorylation by GPCR kinases but also to β-arrestin ubiquitination...
  92. pmc The downstream regulation of chemokine receptor signalling: implications for atherosclerosis
    Jyoti Patel
    Division of Cardiovascular Medicine, Radcliffe Department of Medicine, University of Oxford, John Radcliffe Hospital, Oxford, UK
    Mediators Inflamm 2013:459520. 2013
    ..Regulation of GPCR signalling is critical in limiting vascular inflammation and involves interaction with downstream proteins such as ..
  93. pmc Conformational biosensors reveal GPCR signalling from endosomes
    Roshanak Irannejad
    Department of Psychiatry, University of California, San Francisco, California 94158, USA
    Nature 495:534-8. 2013
    ..tenet of molecular pharmacology is that canonical signal transduction mediated by G-protein-coupled receptor (GPCR) coupling to heterotrimeric G proteins is confined to the plasma membrane...
  94. pmc Critical features for biosynthesis, stability, and functionality of a G protein-coupled receptor uncovered by all-versus-all mutations
    Karola M Schlinkmann
    Department of Biochemistry, University of Zurich, 8057 Zurich, Switzerland
    Proc Natl Acad Sci U S A 109:9810-5. 2012
    ..Starting from the rat neurotensin receptor 1, a class A GPCR, we generated a separate library comprising all 64 codons for each amino acid position...
  95. pmc Molecular mechanisms that control initiation and termination of physiological depolarization-evoked transmitter release
    Yonatan M Kupchik
    Department of Neurobiology, Hebrew University, Jerusalem 91904, Israel
    Proc Natl Acad Sci U S A 105:4435-40. 2008
    ..The time course of ACh release is controlled by a presynaptic inhibitory G protein-coupled autoreceptor (GPCR), whose agonist-binding affinity is voltage-sensitive...
  96. ncbi Structure-based analysis of GPCR function: conformational adaptation of both agonist and receptor upon leukotriene B4 binding to recombinant BLT1
    Jean Louis Baneres
    UMR 5074 CNRS, Chimie Biomoléculaire et Interactions Biologiques, Faculte de Pharmacie, 15 Avenue Ch Flahault, BP 14491, 34093, Cedex 05, Montpellier, France
    J Mol Biol 329:801-14. 2003
    ....
  97. pmc Noise-induced cochlear F-actin depolymerization is mediated via ROCK2/p-ERM signaling
    Yu Han
    Department of Pathology and Laboratory Medicine, Medical University of South Carolina, Charleston, South Carolina, USA
    J Neurochem 133:617-28. 2015
    ..Lysophosphatidic acid (LPA), an agonist of RhoA, binds to the G-protein-coupled receptor (GPCR) leading to activation of RhoA through Gα12/13 and RhoGEF...
  98. pmc LIM homeobox gene-dependent expression of biogenic amine receptors in restricted regions of the C. elegans nervous system
    Ephraim L Tsalik
    Department of Biochemistry and Molecular Biophysics, Center for Neurobiology and Behavior, Columbia University, College of Physicians and Surgeons, New York, NY 10032, USA
    Dev Biol 263:81-102. 2003
    ..Their functions are predominantly mediated through G-protein-coupled 7-transmembrane domain receptors (GPCR), 16 of which are predicted to exist in the genome sequence of the nematode Caenorhabditis elegans...
  99. ncbi Enhanced rewarding properties of morphine, but not cocaine, in beta(arrestin)-2 knock-out mice
    Laura M Bohn
    Department of Pharmacology, The Ohio State University College of Medicine and Public Health, Columbus, Ohio 43210, USA
    J Neurosci 23:10265-73. 2003
    ..Both mu-opioid and dopamine receptors are members of the G-protein-coupled receptor (GPCR) family of proteins...
  100. ncbi A network of control mediated by regulator of calcium/calmodulin-dependent signaling
    S V Rakhilin
    Laboratory of Molecular and Cellular Neuroscience, Rockefeller University, New York, NY 10021, USA
    Science 306:698-701. 2004
    ..G protein-coupled receptor (GPCR)-dependent activation of protein kinase A (PKA) led to phosphorylation of RCS at Ser55 and increased its binding to ..
  101. pmc Ras is an indispensable coregulator of the class IB phosphoinositide 3-kinase p87/p110gamma
    Barbara Kurig
    Department of Pharmacology and Experimental Therapy, Institute of Experimental and Clinical Pharmacology and Toxicology, Eberhard Karls University Hospitals and Clinics, and Interfaculty Center of Pharmacogenomics and Pharmaceutical Research, University of Tubingen, 72074 Tubingen, Germany
    Proc Natl Acad Sci U S A 106:20312-7. 2009
    ..reconstituted to lipid vesicles, we elucidated a novel pathway of p87-dependent, G protein-coupled receptor (GPCR)-induced PI3Kgamma activation...

Research Grants72

  1. BIOPHYSICS OF RECEPTOR/G-PROTEIN INTERACTIONS
    Oleg G Kisselev; Fiscal Year: 2011
    ..We will test this hypothesis using the prototypical GPCR rhodopsin (R) and the G-protein transducin (Gt) responsible for phototransduction in retinal rod cells as a model ..
  2. Methods for the Development of Arrestin2 Inhibitors.
    Spiro Pavlopoulos; Fiscal Year: 2010
    ..is a cytosolic protein that serves to control G-protein Coupled Receptors (GPCRs) by mediating downregulation of GPCR function upon prolonged exposure to a ligand...
  3. CARMA3-mediated NF-kappaB activation in GPCR signaling pathways
    Xin Lin; Fiscal Year: 2010
    ..Binding LPA to its receptor, a GPCR family member, initiates multiple signaling pathways, leading to induction of pro-inflammatory and pro-angiogenic ..
  4. Regulation and function of the YAP transcription co-activator oncoprotein
    Kun Liang Guan; Fiscal Year: 2013
    ..We recently discovered that G-protein coupled receptors (GPCR) and their cognate ligands regulate the Hippo pathway...
  5. TYROSINE KINASES IN G PROTEIN MEDIATED SIGNALING
    Louis M Luttrell; Fiscal Year: 2013
    ..receptors (GPCRs) control cell growth, proliferation and differentiation has fundamentally changed our view of GPCR signal transduction...
  6. GPCR Network
    Raymond C Stevens; Fiscal Year: 2013
    ..modeling of close homolog's and functional studies by external collaborators thereby establishing The PSI GPCR Network...
  7. Beta2 Adrenoceptor Structure and Mechanism of Activation
    Brian K Kobilka; Fiscal Year: 2013
    ..GPCRs exhibit complex and diverse signaling behaviors. A single GPCR can activate more than one G protein subtype as well as G protein independent signaling pathways such as arrestins...
  8. Drug abuse: Discovering ligands for pertinent GPCRs
    Marc G Caron; Fiscal Year: 2013
    ..GPCRs, and more importantly an expanding repository of off-the shelf cell-based assays for over half of the GPCR targets of interest to NIDA funded scientists, with a goal of quickly progressing to the remaining cell assays...
  9. Modulation of insulin and glucagon secretion by GPCR ligands
    TARA ASHLEY SCHWETZ; Fiscal Year: 2011
    ..This is especially significant considering GPCR ligands (i.e. GLP-1 analogs) have emerged as a promising treatment of Type-2 diabetes...
  10. Physiological Regulation of MLCK in Intact Arteries
    Withrow Gil Wier; Fiscal Year: 2013
    ..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...
  11. Rho- and GPCR-mediated signaling through novel cellular effectors
    Joan Heller Brown; Fiscal Year: 2012
    ..second specific aim is to elucidate the role played by increased CCN1/Cyr61 expression in Rho-mediated responses to GPCR agonists...
  12. Endogenous G-Protein Coupled Receptor Antagonists
    Carrie Haskell-Luevano; Fiscal Year: 2012
    ..To achieve these objectives, we will use peptide design, combinatorial libraries, and GPCR mutagenesis strategies...
  13. Synthetic Fabs for Crystallization of Chemokine:Receptor Complexes
    Tracy M Handel; Fiscal Year: 2013
    ..Nevertheless, since 2007 there has been a virtual explosion in the field of GPCR structural biology with the determination of many new structures including one chemokine receptor, CXCR4, in ..
  14. Neuronal-Astrocytic Communication In Vivo
    KEN DOUGLAS MCCARTHY; Fiscal Year: 2013
    ..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 ..
  15. Exploring the Role of the Prokineticin System in Human Reproduction
    ANA PAULA DE ABREU E SILVA METZGER; Fiscal Year: 2013
    ..and will provide insights into the structure-activity relationships of the PROKR2, with potential implications for GPCR biology in general...
  16. Structural Biology of G-Protein Coupled Receptors
    Wayne A Hendrickson; Fiscal Year: 2011
    ..This project emphasizes continued efforts on three GPCR systems;mammalian neurotransmitter receptors for serotonin (5-hydroxytryptamine (5HT) notably receptor 5HT2c;the ..
  17. Deorphanizing the Peptidome
    Bryan L Roth; Fiscal Year: 2012
    ..comprehensive 'de-orphanization'(and thereby annotation) of the universe of peptides involved in neuronal GPCR signaling...
  18. Ligand Directed Functional Selectivity of G-Protein Coupled Receptor Signalling
    Gerry S Oxford; Fiscal Year: 2012
    ..Classical receptor theory suggests that any agonist of a specific GPCR will induce the same conformational changes, and that differences in efficacy and potency among agonists reflect ..
  19. The Role of RGS Proteins in the Regulation of Taste Transduction
    Staci P Cohen; Fiscal Year: 2013
    ..proteins) that act as G[unreadable]-directed GTPase-accelerating proteins (GAPs), regulate G-protein activity and GPCR-initiated signaling;however, taste-specific modulators of G-proteins have not been definitively established...
  20. Developing GalR 1/2 Agonists to Treat Nerve Gas Induced Seizure
    Tamas Bartfai; Fiscal Year: 2010
    ..This will be achieved by targeting two G-protein coupled receptors (GPCR) in the central nervous system, Gal-R1 and Gal-R2...
  21. Adapter molecules on C3a receptor signaling in mast cells
    Hydar Ali; Fiscal Year: 2009
    ..Surprisingly, however, regulation of GPCR function in mast cells remains largely unexplored...
  22. Crystallization and structure determination of the mu-opioid receptor
    Roger K Sunahara; Fiscal Year: 2012
    ..A major breakthrough in GPCR structural biology was the incorporation of a stable protein, T4 lysozyme (T4L), into a structurally unstable ..
  23. Structural Biology of Class B G-Protein Coupled Receptors
    H Eric Xu; Fiscal Year: 2010
    ..The Class B GPCR contains an N-terminal extracellular domain (ECD) that is responsible for specific hormone recognition...
  24. GPCR regulation of progenitor cells in pancreatic cancer
    Thomas M Wilkie; Fiscal Year: 2013
    ..To achieve these advances, focused libraries of putative GPCR ligands will be screened to identify small synthetic molecules that regulate Rgs16 expression in PDAC cell culture...
  25. GPCR Signaling Through a Novel NF-kB Pathway
    Linda M McAllister-Lucas; Fiscal Year: 2013
    ..We have uncovered a signal transduction pathway that mediates NF-kB activation in response to the GPCR agonists, Angiotensin II and thrombin...
  26. Mu opioid agonists with reduced side effects for the treatment of pain
    Chad E Groer; Fiscal Year: 2011
    ..Opioid ligands activate G protein coupled receptors (GPCR) to mediate diverse physiological functions...
  27. Screening Method for GPCRs Related to Appetite
    MARIA MORANO; Fiscal Year: 2009
    ..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...
  28. Targeting Pancreatic Cancer with Aptamers to the CCK-B Receptor
    Gail L Matters; Fiscal Year: 2013
    ..that gastrin stimulates growth of pancreatic cancer by mediating its effects in an autocrine fashion through this GPCR. We have shown that if gastrin's interaction at the receptor can be blocked, pancreatic cancer is inhibited...
  29. Relating GPCRs by biased ligands for enhanced therapeutic efficacy
    MICHAEL JAMES KEISER; Fiscal Year: 2013
    ..Aim 2: To relate GPCR pharmacology by biased ligands. We will extend our maps of all GPCRs to reflect biased ligand classes...
  30. Biosensors of GPCR Activation & Inhibition for Drug Discovery
    RICHARD SCOTT STRUTHERS; Fiscal Year: 2010
    ..Cellular functional assays measuring the production of GPCR second messengers such as cAMP and inositol phosphates, are used routinely and remain conceptually unchanged since ..
  31. Structural Basis of Opioid Receptor Function
    Brian K Kobilka; Fiscal Year: 2013
    ..Aim 2. Conformational dynamics of OR structure and activation. OR activation and more generally GPCR activation involves a complex allosteric coupling between ligand binding and G protein coupling domains that is ..
  32. HTS Assays for Modulators of GPCR Signaling
    Robert G Lowery; Fiscal Year: 2010
    ..relatively recent discovery of a family of proteins called "regulator of G protein signaling" (RGS), that attenuate GPCR signals by increasing the GTPase activity of associated G proteins, has opened up a new avenue for modulating the ..
  33. Luminal factors affecting duodenal protection and chemosensing
    Jonathan D Kaunitz; Fiscal Year: 2013
    ..GPCRs will be immunolocalized to the gut. We will also determine if taste GPCR ligands increase mucosal defense mechanism such as mucosal blood flow, mucus secretion, enterocyte alkalinization, ..
  34. G protein-coupled receptor kinase 3 regulation of leukocyte function in inflammat
    TERESA KATHLEEN TARRANT; Fiscal Year: 2013
    ..GPCRs) phosphorylated by G-protein receptor kinases (GRKs), which serve as negative regulators to turn off GPCR signaling...
  35. G PROTEIN COUPLED RECEPTOR ACTIVATION STUDIED IN YEAST
    Mark Dumont; Fiscal Year: 2009
    ..The yeast pheromone response pathway provides an example of GPCR signaling that can be genetically manipulated in ways that would be impossible in other types of cells, yet ..
  36. Metalloproteinase regulation of ErbB signaling in skin
    Stefan W Stoll; Fiscal Year: 2010
    ..ADAM10 was recently shown to mediate the basal as well as G protein-coupled receptors (GPCR)- stimulated activation of ErbB1 in epithelial cells...
  37. Parathyroid Hormone Receptor Type 1: Dynamics, Traffic and Recycling
    Guillermo G Romero; Fiscal Year: 2010
    The traffic and fate of internalized G protein coupled receptors (GPCR) play a central role in the regulation of their function...
  38. Sensitive Deuterium Exchange MS for Membrane Proteins
    Terry D Lee; Fiscal Year: 2012
    ..Structural information on the GPCR-chemokine complexes is of great importance, but such information is difficult to obtain because of the challenges ..
  39. Mapping the Ligand-Modulated Conformational Landscape of GPCRs
    MORGAN ELIZABETH LAWRENZ; Fiscal Year: 2013
    ..Recent GPCR structures give opportunity for computational study of receptor dynamics...
  40. Bivalent ligands as molecular probes for CB1/OX1 receptor heterodimers
    Yanan Zhang; Fiscal Year: 2010
    ..Interestingly, the importance of GPCR heteromers in vivo remains to be exploited and appreciated, largely due to a lack of selective pharmacological ..
  41. Functions of Chemokine GCPRs in Zebrafish Embryogenesis
    Lilianna Solnica-Krezel; Fiscal Year: 2013
    ..In Aim 2, we will test the hypothesis that Ccr7 chemokine GPCR regulates axis formation by inhibiting [unreadable]-catenin in a GSK3[unreadable] independent and a G[unreadable]q/..
  42. Crosstalk among Growth Factors, ADAMs and Integrins
    Monika Gooz; Fiscal Year: 2010
    ..Further, we wish to study how extracellular matrix (ECM) receptors (called integrins) influence GPCR-RTK cross-talk in cultured mesangial cells. The specific aims of this proposal are: 1...
  43. Universal High Throughput GPCR Screening Assay
    John Bergmann; Fiscal Year: 2010
    G-protein coupled receptors (GPCR) are a family of cell surface proteins involved in mediating many of the biological actions of neurotransmitters in the brain...
  44. 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...
  45. Selective modulation of GPCR signal transduction with biased ligands
    MICHAEL WILLIAM LARK; Fiscal Year: 2010
    ..It is now proposed that GPCR ligands that are biased towards induction or blockade of specific signaling pathways will have differentiated ..
  46. Optimizing analgesia by exploiting CB2 agonist functional selectivity
    KENNETH P MACKIE; Fiscal Year: 2013
    ..Thus, functional selectivity adds another dimension beyond potency, subtype selectivity and intrinsic efficacy to GPCR agonists-a dimension that may be exploited for therapeutic benefit...
  47. Structure-based discovery of allosteric ligands for G Protein Coupled Receptors
    Brian K Kobilka; Fiscal Year: 2013
    ..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...
  48. Investigating G Protein Coupling of Nanodisc-solubilized Beta Adrenergic Receptor
    Courtney Sloan; Fiscal Year: 2013
    ..By combining the nanodisc and microring resonator technologies, bioassays will be developed to characterize the effects of various ligands on GPCR binding and off-target effects in a highly multiplexable platform.
  49. Cell Type Specific Control of Neuronal Signaling
    MARTILIAS STEPHEN FARRELL; Fiscal Year: 2012
    ..In order to determine how receptors might modulate neuronal circuits, it is necessary to selectively activate GPCR signaling in a specific neuronal population in vivo...
  50. Cell-free Detection of GPCR Signaling in a Nanoscale System
    BENJAMIN JACOB DORANZ; Fiscal Year: 2010
    ..However, some of the most desirable types of GPCR drugs have also been some of the most difficult to discover...
  51. Structural Studies in Rhodopsin and G Protein Activation
    DAVID THOMAS LODOWSKI; Fiscal Year: 2011
    ..Upon binding of agonist, structural changes activate the GPCR, and allow the GPCR to bind and induce nucleotide exchange upon the alpha subunit of the heterotrimeric G protein ..
  52. Multiscale modeling of G protein-coupled receptors
    Alan Grossfield; Fiscal Year: 2013
    ..Specifically, we will investigate the role of ligand binding in modulating GPCR function, via two separate all-atom molecular dynamics calculations...
  53. Structural Studies in Rhodopsin and G Protein Activation
    DAVID THOMAS LODOWSKI; Fiscal Year: 2013
    ..Upon binding of agonist, structural changes activate the GPCR, and allow the GPCR to bind and induce nucleotide exchange upon the alpha subunit of the heterotrimeric G protein ..
  54. Role of Arrestins in G Protein-Coupled Receptor Regulation
    Jeffrey L Benovic; Fiscal Year: 2013
    ..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 ..
  55. H1R Signaling and Immune Deviation in EAE
    Cory Teuscher; Fiscal Year: 2013
    ..GPCRs in vitro, and knowledge gained from the proposed in vivo experiments may have broad implications for GPCR-diseases...
  56. SIGNALING THROUGH RHO GTP/GDP EXCHANGE FACTORS
    Philip B Wedegaertner; Fiscal Year: 2013
    ..The RGS-RhoGEFs thus mediate signaling from several important G protein-coupled receptors (GPCR) to activation of Rho and changes in a cell's actin cytoskeleton...
  57. Functional analysis of the CAMTA Transcription Factors
    Hong Sheng Li; Fiscal Year: 2013
    ..neurons, to maintain the intracellular Ca2+ homeostasis, these cells need to fortify the regulatory machinery of GPCR/ROC by expressing more regulatory molecules...
  58. Molecular basis for the regulation of G protein-coupled receptor kinases
    John J G Tesmer; Fiscal Year: 2012
    ..A family of GPCR kinases (GRKs) modulates the activity of these GPCRs by phosphorylating sites in their cytoplasmic loops and C-..
  59. G Protein Coupled Receptor Modulation of Synaptic Transmission
    EDAENI YISHAK HAMID; Fiscal Year: 2010
    ..Furthermore, the presynaptic mechanism most commonly attributed to GPCR mediated inhibition is presynaptic attenuation of Ca2+ entry...
  60. Discovery of antibodies that bind G protein-coupled receptors
    Matthew P DeLisa; Fiscal Year: 2012
    ..As a result, only four unique GPCR structures have been reported...
  61. Characterization of a GPCR-blocking antibody for the treatment of breast cancer.
    GARRET GUENTHER; Fiscal Year: 2011
    ..Evidence suggests that these actions are largely the result of the stimulation of a cognate GPCR for S1P called S1P3...
  62. Assaying the Anthelmintic Potential of a Novel Flatworm-Specific GPCR Family
    Timothy A Day; Fiscal Year: 2013
    ..We have labeled these platyhelminth Rhodopsin orphan family 1 (PROF1) receptors, and they are and entirely novel GPCR subfamily that is present only in flatworms...
  63. Neurokinin 3 Receptor: Nuclear Localization in Supraoptic Neurons
    CELIA SLADEK; Fiscal Year: 2009
    ..Since NK3-Rs are G-protein coupled receptors (GPCR), this suggests the intriguing possibility that extracellular NK3-R ligand induces translocation of NK3-R from the ..
  64. Developing Methods for Crystallizing Class B GPCRs
    HO LEUNG NG; Fiscal Year: 2009
    ..At present, only a handful of GPCR structures have been solved, and none within the Class B GPCR subfamily...
  65. G Protein-Coupled Receptors - Kobilka, Chair
    Andrew D Robertson; Fiscal Year: 2010
    ..Successful development of new drugs for GPCRs has been disappointing in spite of having access to all GPCR sequences in the genome, as well as physiologic insights from gene modification technology, larger more diverse ..
  66. 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 ..
  67. 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 ..
  68. 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...
  69. Novel GPCR Kinase Interactions in Macrophages and Role in Arthritis
    Narayanan Parameswaran; Fiscal Year: 2009
    ..We demonstrate in preliminary data that G-protein coupled receptor kinases (GPCR kinases or GRKs) -2 and -5 play novel and crucial roles in the signaling of TNF receptors in macrophages...
  70. Targeting crosstalk between insulin and Gq signaling systems in pancreatic cancer
    JUAN ENRIQUE ROZENGURT; Fiscal Year: 2010
    ..Crosstalk between the insulin receptor and G protein-coupled receptor (GPCR) signaling systems plays a critical role in the regulation of many physiological functions and in the pathogenesis ..
  71. Screening Method for GPCRs Related to Appetite
    CAMILLE NORTON; Fiscal Year: 2004
    ..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...
  72. 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...