OXER1

Summary

Gene Symbol: OXER1
Description: oxoeicosanoid receptor 1
Alias: GPCR, GPR170, TG1019, oxoeicosanoid receptor 1, 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, OXE receptor, oxoeicosanoid (OXE) receptor 1
Species: human

Top Publications

  1. 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
  2. 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
  3. 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
  4. 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
  5. 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
  6. 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
  7. 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
  8. 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
  9. 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
  10. 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

Research Grants

  1. BIOPHYSICS OF RECEPTOR/G-PROTEIN INTERACTIONS
    Oleg G Kisselev; Fiscal Year: 2011
  2. Methods for the Development of Arrestin2 Inhibitors.
    Spiro Pavlopoulos; Fiscal Year: 2010
  3. CARMA3-mediated NF-kappaB activation in GPCR signaling pathways
    Xin Lin; Fiscal Year: 2010
  4. Kun Liang Guan; Fiscal Year: 2015
  5. Louis M Luttrell; Fiscal Year: 2016
  6. Raymond C Stevens; Fiscal Year: 2014
  7. Brian K Kobilka; Fiscal Year: 2016
  8. Marc G Caron; Fiscal Year: 2016
  9. Modulation of insulin and glucagon secretion by GPCR ligands
    TARA ASHLEY SCHWETZ; Fiscal Year: 2011
  10. Physiological Regulation of MLCK in Intact Arteries
    Withrow Gil Wier; Fiscal Year: 2013

Detail Information

Publications596 found, 100 shown here

  1. 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...
  2. 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 ..
  3. 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...
  4. 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...
  5. 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)...
  6. 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...
  7. 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...
  8. 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...
  9. 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 ..
  10. 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...
  11. 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...
  12. 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...
  13. 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 ..
  14. 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...
  15. 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 ..
  16. 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...
  17. 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...
  18. 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...
  19. 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-..
  20. 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 ..
  21. 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 ..
  22. 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-..
  23. 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)...
  24. 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...
  25. 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...
  26. 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...
  27. 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-..
  28. 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 ..
  29. 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...
  30. 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...
  31. 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...
  32. 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...
  33. 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...
  34. 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...
  35. 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...
  36. 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 ..
  37. 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...
  38. 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...
  39. 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...
  40. 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...
  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 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...
  43. ncbi GTP-binding-protein-coupled receptor kinases--two mechanistic models
    K Palczewski
    Department of Ophthalmology, University of Washington, School of Medicine, Seattle 98195 6485, USA
    Eur J Biochem 248:261-9. 1997
    ..It appears that GRKs bind GPCR* through two separate sites: a high-affinity site, which involves intracellular loops of the activated receptor, ..
  44. ncbi G-protein-mediated signaling and its control in macrophages and mammalian cells
    P Chakraborty
    Biomembrane Division, Indian Institute of Chemical Biology, Calcutta
    Crit Rev Microbiol 27:1-8. 2001
    G-protein coupled receptor (GPCR) in various cell types exert its effects through heterotrimetic GTP-binding proteins (G-proteins)...
  45. ncbi Activator of G-protein signaling 1 blocks GIRK channel activation by a G-protein-coupled receptor: apparent disruption of receptor signaling complexes
    Aya Takesono
    Department of Pharmacology, Medical University of South Carolina, Charleston, South Carolina 29425, USA
    J Biol Chem 277:13827-30. 2002
    ..and activates heterotrimeric G-protein signaling systems independent of a G-protein-coupled receptor (GPCR)...
  46. ncbi Gastrointestinal peptide signalling in health and disease
    Enrique Rozengurt
    Department of Medicine, School of Medicine and Molecular Biology Institute, University of California, Los Angeles 90095 1786, USA
    Eur J Surg Suppl . 2002
    ..b>GPCR agonists including bombesin/GRP induce a rapid and striking activation of PKD by PKC...
  47. ncbi Recent advances in mammalian RFamide peptides: the discovery and functional analyses of PrRP, RFRPs and QRFP
    Shoji Fukusumi
    Frontier Research Laboratories, Pharmaceutical Research Division, Takeda Pharmaceutical Company Ltd, Wadai 10, Tsukuba shi, Ibaraki 300 4293, Japan
    Peptides 27:1073-86. 2006
    ..RFamide peptides was made possible by reverse pharmacology on the basis of orphan G protein-coupled receptor (GPCR) research...
  48. ncbi A boolean network modelling of receptor mosaics relevance of topology and cooperativity
    L F Agnati
    Department of Biomedical Sciences, University of Modena and Reggio Emilia and IRCCS, Ospedale San Camillo, Venezia, Italy
    J Neural Transm (Vienna) 114:77-92. 2007
    ..the last five years data have been obtained showing that a functional cross-talk among G Protein Coupled receptors (GPCR) exists at the plasma membrane level where they can dimerise and are able to generate high order oligomers...
  49. ncbi DEP-domain-mediated regulation of GPCR signaling responses
    Daniel R Ballon
    Department of Molecular and Cell Biology, Division of Biochemistry and Molecular Biology, University of California, Berkeley, CA 94720, USA
    Cell 126:1079-93. 2006
    ..G protein signaling (RGS) protein Sst2 and demonstrate that the DEP domains in Sst2 mediate binding to its cognate GPCR (Ste2)...
  50. ncbi The cell biology of Smo signalling and its relationships with GPCRs
    Ana Ruiz-Gomez
    Departamento de Biologia Molecular, Universidad Autonoma de Madrid, Cantoblanco, Madrid, Spain
    Biochim Biophys Acta 1768:901-12. 2007
    ..and cellular aspects of Smo signalling, with particular focus in the similarities in the mechanism of signal transduction between Smo and other transmembrane proteins belonging to the G-Protein coupled receptors superfamily (GPCR).
  51. ncbi Diverse pathways for nuclear signaling by G protein-coupled receptors and their ligands
    Edward J Goetzl
    Department of Medicine, University of California, San Francisco, California, USA
    FASEB J 21:638-42. 2007
    ..The first consists of GPCR-complex activation of messengers that enter the nucleus and there initiate cell-modifying processes without the ..
  52. doi Raf kinase inhibitory protein: a signal transduction modulator and metastasis suppressor
    Alexey E Granovsky
    Ben May Department for Cancer Research, University of Chicago, 929 East 57th Street, Chicago, IL 60637, USA
    Cell Res 18:452-7. 2008
    ..RKIP inhibits MAP kinase (Raf-MEK-ERK), G protein-coupled receptor (GPCR) kinase and NFkappaB signaling cascades...
  53. doi Is the adrenal cortex a target for gonadotropins?
    Sophie Bernichtein
    Department of Reproductive Biology, Imperial College London, Hammersmith Campus, Du Cane Road, London W12 0NN, UK
    Trends Endocrinol Metab 19:231-8. 2008
    ..hormone/chorionic gonadotropin receptors (LHCGR), a characteristic gonad-specific G-protein coupled receptor (GPCR). LHCGR levels increase in the adrenal cortex after exposure to chronically elevated gonadotropins (e.g...
  54. pmc Selectivity of agonists for the active state of M1 to M4 muscarinic receptor subtypes
    Katherine W Figueroa
    Department of Pharmacology, University of California, Irvine, California 92697 4625, USA
    J Pharmacol Exp Ther 328:331-42. 2009
    ..RA(i) is a relative measure of the microscopic affinity constant of an agonist for the active state of a GPCR expressed relative to that of a standard agonist...
  55. doi Staphylococcal SSL5 inhibits leukocyte activation by chemokines and anaphylatoxins
    Jovanka Bestebroer
    Medical Microbiology, University Medical Center Utrecht, Utrecht, The Netherlands
    Blood 113:328-37. 2009
    ..Importance of glycans was shown for both GPCR and chemokine binding...
  56. pmc A surface of the kinase domain critical for the allosteric activation of G protein-coupled receptor kinases
    Chih Chin Huang
    Life Sciences Institute, Department of Pharmacology, University of Michigan, Ann Arbor, Michigan 48109 2216, USA
    J Biol Chem 284:17206-15. 2009
    G protein-coupled receptor (GPCR) kinases (GRKs) phosphorylate activated GPCRs and initiate their desensitization...
  57. doi Expression, solubilization and purification of a human olfactory receptor from Escherichia coli
    Hyun Seok Song
    School of Chemical and Biological Engineering, Seoul National University, Gwanak Gu Sillim Dong San 56 1, Seoul, 151 744, Korea
    Curr Microbiol 59:309-14. 2009
    Olfactory receptors pertaining to G protein-coupled receptor (GPCR) are integral membrane proteins composed of seven transmembrane spanning domains...
  58. doi Impact of the DRY motif and the missing "ionic lock" on constitutive activity and G-protein coupling of the human histamine H4 receptor
    Erich H Schneider
    Department of Pharmacology and Toxicology, University of Regensburg, Regensburg, Germany
    J Pharmacol Exp Ther 333:382-92. 2010
    ..69-R6.31 rather than by the missing ionic lock, 2) Y3.60 may form alternative locks in active and inactive GPCR states, 3) R3.50 is crucial for hH4R-G protein coupling, and 4) hH4R-R3...
  59. pmc Rational design of dualsteric GPCR ligands: quests and promise
    Klaus Mohr
    Institute of Pharmacy, Rheinische Friedrich Wilhelms University, Bonn, Germany
    Br J Pharmacol 159:997-1008. 2010
    ..As allosteric interactions are increasingly described for GPCRs and as insight into the spatial geometry of ligand/GPCR-complexes is growing impressively, the rational design of dualsteric drugs is a promising new approach to achieve ..
  60. doi Stability study of the human G-protein coupled receptor, Smoothened
    Rony Nehmé
    Universite de Nice Sophia Antipolis, CNRS UMR 6543, Parc Valrose, F 06108 Nice Cedex 2, France
    Biochim Biophys Acta 1798:1100-10. 2010
    Smoothened is a member of the G-protein coupled receptor (GPCR) family responsible for the transduction of the Hedgehog signal to the intracellular effectors of the Hedgehog signaling pathway...
  61. doi Functionally selective cannabinoid receptor signalling: therapeutic implications and opportunities
    Barbara Bosier
    Unité de Chimie Pharmaceutique et de Radiopharmacie CMFA 7340, Louvain Drug Research Institute, Brussels, Belgium
    Biochem Pharmacol 80:1-12. 2010
    ..At variance with the classical concept that all agonists at a given GPCR induce a similar repertoire of downstream events in all tissues, we also summarize the experimental evidence ..
  62. pmc Kinetics of G-protein-coupled receptor endosomal trafficking pathways revealed by single quantum dots
    Katye M Fichter
    Department of Biomedical Engineering, Oregon Health and Science University, Portland, OR 97239, USA
    Proc Natl Acad Sci U S A 107:18658-63. 2010
    ..The role of endosomal trafficking in GPCR signaling regulation is gaining substantial consideration...
  63. doi Constitutively active μ-opioid receptors
    Mark Connor
    Australian School of Advanced Medicine, Macquarie University, New South Wales, Australia
    Methods Enzymol 484:445-69. 2010
    The μ-opioid receptor is the G protein coupled receptor (GPCR) responsible for the analgesic, rewarding and unwanted effects of morphine and similar drugs...
  64. pmc CK2 phosphorylation of an acidic Ser/Thr di-isoleucine motif in the Na+/H+ exchanger NHE5 isoform promotes association with beta-arrestin2 and endocytosis
    Viktoria Lukashova
    Department of Physiology, McGill University, Montreal, Quebec, Canada
    J Biol Chem 286:11456-68. 2011
    ..site was robustly phosphorylated by the acidotropic protein kinase CK2, whereas other kinases, such as CK1 or the GPCR kinase GRK2, were considerably less potent...
  65. doi Design and use of fluorescent ligands to study ligand-receptor interactions in single living cells
    Stephen J Briddon
    Institute of Cell Signalling, School of Biomedical Sciences, University of Nottingham, Nottingham, UK
    Methods Mol Biol 746:211-36. 2011
    ..Here, we describe some basic considerations in the design of fluorescent GPCR ligands, including choice of pharmacological template, linker, and fluorophore...
  66. pmc Allosteric modulation of metabotropic glutamate receptors
    Douglas J Sheffler
    Department of Pharmacology, Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, Tennessee, USA
    Adv Pharmacol 62:37-77. 2011
    ..One GPCR family that has greatly benefited from this approach is the metabotropic glutamate receptors (mGlus)...
  67. pmc Novel role for proteinase-activated receptor 2 (PAR2) in membrane trafficking of proteinase-activated receptor 4 (PAR4)
    Margaret R Cunningham
    Department of Physiology and Pharmacology, Strathclyde Institute for Biomedical Sciences, Univesity of Strathclyde, 27 Taylor Street, Glasgow G4 0NR, Scotland, United Kingdom
    J Biol Chem 287:16656-69. 2012
    Proteinase-activated receptors 4 (PAR(4)) is a class A G protein-coupled receptor (GPCR) recognized through the ability of serine proteases such as thrombin and trypsin to mediate receptor activation...
  68. pmc Targeted inactivation of GPR26 leads to hyperphagia and adiposity by activating AMPK in the hypothalamus
    Daohong Chen
    Department of Cellular and Molecular Physiology, Pennsylvania State University College of Medicine, Hershey, Pennsylvania, United States of America
    PLoS ONE 7:e40764. 2012
    G-protein coupled receptor 26 (GPR26) is a brain-specific orphan GPCR with high expression in the brain region that controls satiety. Depletion of GPR26 has been shown to increase fat storage in C...
  69. ncbi Recent advances in the rationale design of GPER ligands
    C Rosano
    U O S Biopolimeri e Proteomica IRCCS A O U San Martino IST, Istituto Nazionale per la Ricerca sul Cancro, Largo R Benzi 10, 16132 Genova Italy
    Curr Med Chem 19:6199-206. 2012
    G-Protein Coupled Receptor (GPCR) superfamily, which comprises approximately 900 members, is the largest family of protein targets with proven therapeutic value...
  70. doi Approaches towards structures of Y receptors, examples of human G-protein coupled receptors, by solution NMR
    Reto Walser
    University of Zurich Institute of Organic Chemistry, Winterthurerstrasse 190, CH 8057 Zurich, Switzerland
    Chimia (Aarau) 66:781-6. 2012
    Despite recent advances no solution structure for a true G-protein coupled receptor (GPCR) is available today due to biochemical and spectroscopic problems...
  71. doi Bimolecular fluorescence complementation analysis of G protein-coupled receptor dimerization in living cells
    Karin F K Ejendal
    Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, West Lafayette, Indiana, USA
    Methods Enzymol 521:259-79. 2013
    Emerging evidence indicates that G protein-coupled receptor (GPCR) signaling is mediated by receptor-receptor interactions at multiple levels...
  72. doi Fluorescent ligands to investigate GPCR binding properties and oligomerization
    Martin Cottet
    Institute de Ge nomique Fonctionnelle CNRS, UMR 5203, Montpellier, France
    Biochem Soc Trans 41:148-53. 2013
    ..time-resolved)-FRET (fluorescence resonance energy transfer) approaches exhibit an interesting potential to study GPCR interactions with various partners...
  73. doi The second extracellular loop of GPCRs determines subtype-selectivity and controls efficacy as evidenced by loop exchange study at A2 adenosine receptors
    Benjamin F Seibt
    PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, 53121 Bonn, Germany
    Biochem Pharmacol 85:1317-29. 2013
    ..This role of the EL2 is likely to extend to other members of the GPCR family, and the EL2 of GPCRs appears to be an attractive target structure for drugs.
  74. ncbi Recent trends and future prospects in computational GPCR drug discovery: from virtual screening to polypharmacology
    Antonio Carrieri
    Dipartimento di Farmacia Scienze del Farmaco, Università degli Studi di Bari Aldo Moro Via Orabona 4, 70125 Bari, Italy
    Curr Top Med Chem 13:1069-97. 2013
    ..Here, we discuss some of the advantages of multi-target approaches, and we review some significant examples of their application in the last decade to that well known class of pharmaceutical targets, the G-protein coupled receptors...
  75. pmc IKK epsilon kinase is crucial for viral G protein-coupled receptor tumorigenesis
    Yi Wang
    Department of Molecular Microbiology and Immunology, University of Southern California, Los Angeles, CA 90033, USA
    Proc Natl Acad Sci U S A 110:11139-44. 2013
    ..Herpesvirus genomes encode multiple GPCRs implicated in viral pathogenesis. Kaposi sarcoma-associated herpesvirus GPCR (kGPCR) activates proliferative pathways and, when expressed in endothelium in mice, sufficiently induces ..
  76. pmc TLR4 Signaling augments monocyte chemotaxis by regulating G protein-coupled receptor kinase 2 translocation
    Zheng Liu
    Department of Pathophysiology, Southern Medical University, Guangzhou 510515, China
    J Immunol 191:857-64. 2013
    ..function of MCP-1 is mediated by binding to the CCR2 receptor, a member of the G protein-coupled receptor (GPCR) family...
  77. pmc Defective homocysteine metabolism: potential implications for skeletal muscle malfunction
    Sudhakar Veeranki
    Department of Physiology and Biophysics, University of Louisville School of Medicine, Louisville, KY 40202, USA
    Int J Mol Sci 14:15074-91. 2013
    ..potential and imbalances in Hcy production and/or catabolism impacts gene expression and cell signaling including GPCR signaling...
  78. doi Gastrin-releasing peptide receptor signaling in the integration of stress and memory
    Rafael Roesler
    Laboratory of Neuropharmacology and Neural Tumor Biology, Department of Pharmacology, Institute for Basic Health Sciences, Federal University of Rio Grande do Sul, 90050 170 Porto Alegre, RS, Brazil Cancer Research Laboratory, University Hospital Research Center CPE HCPA, Federal University of Rio Grande do Sul, 90035 003 Porto Alegre, RS, Brazil National Institute for Translational Medicine INCT TM, 90035 003 Porto Alegre, RS, Brazil Electronic address
    Neurobiol Learn Mem 112:44-52. 2014
    ..GRP acts by binding to the GRP receptor (GRPR, also called BB2), a member of the G-protein coupled receptor (GPCR) superfamily...
  79. doi [G protein-coupled receptors in the spot light]
    Abla Benleulmi-Chaachoua
    INSERM, U1016, Institut Cochin, 22 rue Mechain, 75014 Paris, France CNRS UMR 8104, Institut Cochin, 22 rue Mechain, 75014 Paris, France Université Paris Descartes, 12 rue de l Ecole de medecine, 75006 Paris, France
    Biol Aujourdhui 207:191-200. 2013
    ..Research efforts in the GPCR field have been rewarded in 2012 by the Nobel Price in Chemistry...
  80. pmc A PET study comparing receptor occupancy by five selective cannabinoid 1 receptor antagonists in non-human primates
    Stephan Hjorth
    Biosciences, CVMD Innovative Medicines, AstraZeneca R and D, Molndal, Sweden
    Neuropharmacology 101:519-30. 2016
    ..typically around ∼20-30%, thus much lower than what would be expected for classical G-protein coupled receptor (GPCR) antagonists in other therapeutic contexts...
  81. pmc Biochemical Large-Scale Interaction Analysis of Murine Olfactory Receptors and Associated Signaling Proteins with Post-Synaptic Density 95, Drosophila Discs Large, Zona-Occludens 1 (PDZ) Domains
    Fabian Jansen
    From the Department of Cell Physiology, Faculty for Biology and Biotechnology
    Mol Cell Proteomics 14:2072-84. 2015
    ..Various GPCR-mediated pathways are organized into protein microdomains that can be orchestrated and regulated through ..
  82. doi An insight into antagonist binding and induced conformational dynamics of class B GPCR corticotropin-releasing factor receptor 1
    Junli Xu
    State Key Laboratory of Medicinal Chemical Biology and College of Pharmacy, Nankai University, Tianjin 300071, China
    Mol Biosyst 11:2042-50. 2015
    The human corticotropin-releasing factor receptor type 1 (CRF1R) is a class B G-protein-coupled receptor (GPCR), which mediates the response to stress and has been considered as a drug target for depression and anxiety...
  83. pmc The Dynamic Process of Drug-GPCR Binding at Either Orthosteric or Allosteric Sites Evaluated by Metadynamics
    Sebastian Schneider
    Department of Structural and Chemical Biology, Icahn School of Medicine at Mount Sinai, One Gustave L Levy Place, P O Box 1677, New York, NY, 10029 6574, USA
    Methods Mol Biol 1335:277-94. 2015
    Major advances in G Protein-Coupled Receptor (GPCR) structural biology over the past few years have yielded a significant number of high-resolution crystal structures for several different receptor subtypes...
  84. doi The power of mass spectrometry in structural characterization of GPCR signaling
    Kunhong Xiao
    a Department of Pharmacology and Chemical Biology, University of Pittsburgh, Pittsburgh, PA, USA and
    J Recept Signal Transduct Res 35:213-9. 2015
    ..this mini-review, we will highlight several examples demonstrating the power of MS in structural analysis to better elucidate the structural basis of GPCR signaling, particularly through the β-arrestin-mediated GPCR signaling pathway.
  85. pmc Mass spectrometry-based ligand binding assays on adenosine A1 and A2A receptors
    A Massink
    Division of Medicinal Chemistry, LACDR, Leiden University, Leiden, The Netherlands
    Purinergic Signal 11:581-94. 2015
    ..receptors (A(1)AR and A(2A)AR), which are well-characterized members of the class A G protein-coupled receptor (GPCR) family...
  86. pmc Integrating the GPCR transactivation-dependent and biased signalling paradigms in the context of PAR1 signalling
    P J Little
    School of Pharmacy, The University of Queensland, Pharmacy Australia Centre of Excellence, Woolloongabba, QLD, Australia
    Br J Pharmacol 173:2992-3000. 2016
    ..This overview, with a focus on the GPCR, protease-activated receptor-1, integrates both of these processes to predict the complex array of responses that ..
  87. pmc RGS proteins as targets in the treatment of intestinal inflammation and visceral pain: New insights and future perspectives
    Maciej Salaga
    Faculty of Medicine, Department of Biochemistry, Medical University of Lodz, Lodz, Poland
    Bioessays 38:344-54. 2016
    Regulators of G protein signaling (RGS) proteins provide timely termination of G protein-coupled receptor (GPCR) responses...
  88. doi Biased signalling from the glucocorticoid receptor: Renewed opportunity for tailoring glucocorticoid activity
    Christine R Keenan
    Department of Pharmacology and Therapeutics, The University of Melbourne, Parkville, Victoria 3010, Australia
    Biochem Pharmacol 112:6-12. 2016
    ..Drawing on concepts of signalling bias from the field of G protein-coupled receptor (GPCR) biology, we speculate that ligand-dependent differences in GR signalling can be considered analogous to GPCR ..
  89. doi CARMA3 Is a Host Factor Regulating the Balance of Inflammatory and Antiviral Responses against Viral Infection
    Changying Jiang
    Department of Molecular and Cellular Oncology, The University of Texas, MD Anderson Cancer Center, Houston, TX 77030, USA
    Cell Rep 14:2389-401. 2016
    ..Here, we have found that CARMA3, a scaffold protein previously shown to mediate NF-κB activation induced by GPCR and EGFR, positively regulates MAVS-induced NF-κB activation...
  90. doi Evidence that the Rhodopsin Kinase (GRK1) N-Terminus and the Transducin Gα C-Terminus Interact with the Same "Hydrophobic Patch" on Rhodopsin TM5
    Amber M Jones Brunette
    Department of Biochemistry and Molecular Biology, Oregon Health and Science University, Portland, Oregon 97239 3098, United States
    Biochemistry 55:3123-35. 2016
    ..Here, we purified fully functional GPCR kinase 1 (GRK1) using a rapid method and used it to gain insights into how this important kinase interacts with the ..
  91. pmc Recent advances in understanding the extracellular calcium-sensing receptor
    Matilde Colella
    Department of Biosciences, Biotechnology and Biopharmaceutics, University of Bari, Bari, Italy
    F1000Res 5:. 2016
    The extracellular calcium-sensing receptor (CaR), a ubiquitous class C G-protein-coupled receptor (GPCR), is responsible for the control of calcium homeostasis in body fluids...
  92. ncbi Adhesion GPCR Function in Pulmonary Development and Disease
    Marie Gabrielle Ludwig
    Novartis Institutes for BioMedical Research, Basel, 4056, Switzerland
    Handb Exp Pharmacol 234:309-327. 2016
    ..Emerging data demonstrate critical roles for members of the adhesion GPCR (aGPCR) family in pulmonary development, homeostasis, and disease...
  93. ncbi Development of displacement binding and GTPgammaS scintillation proximity assays for the identification of antagonists of the micro-opioid receptor
    George Rodgers
    Eli Lilly and Company Lilly RTP, Research Triangle Park, NC 27709, USA
    Assay Drug Dev Technol 1:627-36. 2003
    ..Opioid receptors are members of the seven-transmembrane G protein-coupled receptor (GPCR) family and are involved in the control of various aspects of human physiology, including pain, stress, reward, ..
  94. pmc Structure modeling of all identified G protein-coupled receptors in the human genome
    Yang Zhang
    Center of Excellence in Bioinformatics, University at Buffalo, Buffalo, New York, USA
    PLoS Comput Biol 2:e13. 2006
    ..structural information is crucial for function annotation and drug design, there are few experimentally determined GPCR structures...
  95. ncbi [Membrane-associated steroid hormone receptors: functional significance of nongenomic action]
    Mitsuhiro Kawata
    Department of Anatomy and Neurobiology, Kyoto Prefectural University of Medicine
    Nihon Rinsho 66:55-62. 2008
    ..in the nucleus for genomic actions, and also membrane-associated receptors which include nuclear receptor itself or GPCR(G protein-coupled receptor) followed by the activation of second messengers...
  96. pmc Non-traditional roles of G protein-coupled receptors in basic cell biology
    Xin Zhang
    High Magnetic Field Laboratory, Chinese Academy of Sciences, Hefei, PR China
    Mol Biosyst 9:586-95. 2013
    ..In this review, we give a basic introduction to GPCR signaling and highlight some less well described roles of GPCRs, including in cell division and membrane ..
  97. pmc Employing novel animal models in the design of clinically efficacious GPCR ligands
    Sophie J Bradley
    MRC Toxicology Unit, University of Leicester, Hodgkin Building, Leicester LE1 9HN, UK
    Curr Opin Cell Biol 27:117-25. 2014
    The headline success of targeting GPCRs in human diseases has masked the fact that many GPCR drug discovery programmes fail...
  98. pmc Functional characterization of five different PRXamide receptors of the red flour beetle Tribolium castaneum with peptidomimetics and identification of agonists and antagonists
    Hongbo Jiang
    Key Laboratory of Entomology and Pest Control Engineering, College of Plant Protection, Southwest University, Chongqing 400715, PR China Department of Entomology, Kansas State University, Manhattan, KS 66506, United States
    Peptides 68:246-52. 2015
    ..This observation suggests that a target GPCR with more promiscuity will provide better success for peptidomimetic approaches...
  99. doi Dynamics of G protein effector interactions and their impact on timing and sensitivity of G protein-mediated signal transduction
    Eva Lisa Bodmann
    Institute for Pharmacology and Clinical Pharmacy, Faculty of Pharmacy, Philipps University Marburg, Karl von Frisch Str 1, 35043 Marburg, Germany
    Eur J Cell Biol 94:415-9. 2015
    ..The introduction of Förster resonance energy transfer methods into the field of GPCR research led to interesting insights into the temporal patterns of interactions between G protein subunits and ..
  100. ncbi Molecular evolution of the human interleukin-8 receptor gene cluster
    S K Ahuja
    National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, Maryland 20892
    Nat Genet 2:31-6. 1992
    ..by the IL-8 ligand-receptor complex--ligand promiscuity for IL-8, receptor promiscuity for IL8RA, gene duplication for both ligands and receptors and gene extinction in the case of IL8RAP--is unprecedented for the GPCR superfamily.
  101. pmc A novel angiotensin II type 2 receptor signaling pathway: possible role in cardiac hypertrophy
    Takaaki Senbonmatsu
    Departments of Biochemistry, Pharmacology, Pathology and Medicine, Vanderbilt University School of Medicine, Nashville, TN 37232 0146, USA
    EMBO J 22:6471-82. 2003
    We describe a novel signaling mechanism mediated by the G-protein-coupled receptor (GPCR) angiotensin II (Ang II) type 2 receptor (AT(2))...

Research Grants74

  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. Kun Liang Guan; Fiscal Year: 2015
    ..We recently discovered that G-protein coupled receptors (GPCR) and their cognate ligands regulate the Hippo pathway...
  5. Louis M Luttrell; Fiscal Year: 2016
    ..receptors (GPCRs) control cell growth, proliferation and differentiation has fundamentally changed our view of GPCR signal transduction...
  6. Raymond C Stevens; Fiscal Year: 2014
    ..modeling of close homolog's and functional studies by external collaborators thereby establishing The PSI GPCR Network...
  7. Brian K Kobilka; Fiscal Year: 2016
    ..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. Marc G Caron; Fiscal Year: 2016
    ..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. ANA PAULA DE ABREU E SILVA METZGER; Fiscal Year: 2014
    ..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. 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 ..
  18. 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...
  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. Linda M McAllister-Lucas; Fiscal Year: 2016
    ..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. Gail L Matters; Fiscal Year: 2014
    ..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. Brian K Kobilka; Fiscal Year: 2016
    ..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. Jonathan D Kaunitz; Fiscal Year: 2015
    ..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. LILIANNA SOLNICAKREZEL; Fiscal Year: 2015
    ..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. KENNETH P MACKIE; Fiscal Year: 2014
    ..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. 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.
  48. Brian K Kobilka; Fiscal Year: 2016
    ..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...
  49. 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...
  50. 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...
  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. Alan Grossfield; Fiscal Year: 2015
    ..Specifically, we will investigate the role of ligand binding in modulating GPCR function, via two separate all-atom molecular dynamics calculations...
  53. DAVID THOMAS LODOWSKI; Fiscal Year: 2014
    ..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. Jeffrey L Benovic; Fiscal Year: 2015
    ..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. Cory Teuscher; Fiscal Year: 2014
    ..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. John J G Tesmer; Fiscal Year: 2016
    ..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. Physiological Implications of Serotonin Receptor Regulation
    Laura M Bohn; Fiscal Year: 2013
    ..Serotonin mediates its actions by binding to and activating G protein-coupled receptors (GPCR) on the surface of neurons and other cells...
  62. 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...
  63. 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...
  64. 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 ..
  65. 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...
  66. 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 ..
  67. 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 ..
  68. 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 ..
  69. 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...
  70. 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...
  71. 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 ..
  72. 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...
  73. 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...