Genomes and Genes
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
Publications140 found, 100 shown here
- Up-regulation of G-protein-coupled receptors for endothelin and thromboxane by lipid-soluble smoke particles in renal artery of ratYan hua Xie
Institute of Materia Medica, School of Pharmacy, Fourth Military Medical University, Xi an, Shaanxi, China
Basic Clin Pharmacol Toxicol 107:803-12. 2010Up-regulation of G-protein-coupled receptors (GPCR) plays key roles in renal hypertension and cardiovascular disease pathogenesis...
- Cloning and identification of an oxytocin/vasopressin-like receptor and its ligand from insectsElisabeth 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...
- A human gene encodes a putative G protein-coupled receptor highly expressed in the central nervous systemP 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 ..
- Promoting neurotrophic effects by GPCR ligandsFreddy 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...
- N-arachidonoyl glycine, an abundant endogenous lipid, potently drives directed cellular migration through GPR18, the putative abnormal cannabidiol receptorDouglas 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...
- A beta-arrestin binding determinant common to the second intracellular loops of rhodopsin family G protein-coupled receptorsSébastien 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)...
- Gene expression profiling for the identification of G-protein coupled receptors in human plateletsStefan 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...
- Involvement of OA1, an intracellular GPCR, and G alpha i3, its binding protein, in melanosomal biogenesis and optic pathway formationAlejandra 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...
- A review of neurohormone GPCRs present in the fruitfly Drosophila melanogaster and the honey bee Apis melliferaFrank 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. 2006G protein-coupled receptor (GPCR) genes are large gene families in every animal, sometimes making up to 1-2% of the animal's genome...
- Signal transduction pathways of G protein-coupled receptors and their cross-talk with receptor tyrosine kinases: lessons from bradykinin signalingC 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. 2000G 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 ..
- Confocal fluorescence microscopy for high-throughput screening of G-protein coupled receptorsRalf 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...
- Halothane binding to a G protein coupled receptor in retinal membranes by photoaffinity labelingY Ishizawa
Departments of Anesthesia, Physiology, and Biochemistry and Biophysics, University of Pennsylvania Medical Center, Philadelphia 19104 4283, USA
Biochemistry 39:8497-502. 2000General anesthetics have been reported to alter the functions of G protein coupled receptor (GPCR) signaling systems...
- S-nitrosoglutathione inhibits alpha1-adrenergic receptor-mediated vasoconstriction and ligand binding in pulmonary arteryEva 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...
- 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 parametersMilena 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 ..
- Control of PDGF-induced reactive oxygen species (ROS) generation and signal transduction in human lens epithelial cellsKate 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...
- The stability of the G protein-coupled receptor-beta-arrestin interaction determines the mechanism and functional consequence of ERK activationAkira 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...
- Expression of terminally glycosylated calcitonin receptor-like receptor in uterine leiomyoma: endothelial phenotype and association with microvascular densityLeonid 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 ..
- Compartmentation of G-protein-coupled receptors and their signalling components in lipid rafts and caveolaeP A Insel
Department of Anesthesiology Graduate Program, University of California, San Diego, La Jolla, CA 92093, USA
Biochem Soc Trans 33:1131-4. 2005G-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...
- A homogeneous enzyme fragment complementation cyclic AMP screen for GPCR agonistsRajasree 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...
- Coupling mechanism of a GPCR and a heterotrimeric G protein during chemoattractant gradient sensing in DictyosteliumXuehua 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...
- 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 activityJerzy 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. 2010Finding small non-peptide molecules for G protein-coupled receptors (GPCR) whose endogenous ligands are peptides, is a very important task for medicinal chemists...
- Fine tuning of blood pressure by the regulator of G protein signaling (RGS) 2Andrey 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-..
- Evolving concepts in G protein-coupled receptor endocytosis: the role in receptor desensitization and signalingS 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 ..
- Fusion proteins as model systems for the analysis of constitutive GPCR activityErich 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-..
- Drug design strategies for targeting G-protein-coupled receptorsThomas 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 ..
- Arrestin orchestrates crosstalk between G protein-coupled receptors to modulate the spatiotemporal activation of ERK MAPKDavid 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 ..
- 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. 2004HHV-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...
- Beta-arrestin1 and beta-arrestin2 are differentially required for phosphorylation-dependent and -independent internalization of delta-opioid receptorsXiaoqing Zhang
Pharmacology Research Center, Shanghai Medical College, Shanghai, China
J Neurochem 95:169-78. 2005Beta-arrestins are key negative regulators and scaffolds of G protein-coupled receptor (GPCR) signalling...
- 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) phosphorylationRodrigo Jacamo
Department of Medicine, David Geffen School of Medicine, UCLA, Los Angeles, California 90095, USA
J Biol Chem 283:12877-87. 2008Protein 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...
- Constitutive activity of G-protein coupled receptors: emphasis on serotonin receptorsMilt 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. 2002Several 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)...
- Regulated expression of G protein-coupled receptor kinases (GRK's) and beta-arrestins in osteoblastsR 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. 2003Desensitization of G-protein coupled receptors (GPCR's) is largely mediated by a family of enzymes and protein co-factors termed GRKs and arrestins, respectively...
- 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-..
- Modeling molecular mechanisms of binding of the anaphylatoxin C5a to the C5a receptorGregory 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 ..
- Formation of new genes explains lower intron density in mammalian Rhodopsin G protein-coupled receptorsDavids Fridmanis
Biomedical Research and Study Centre, University of Latvia, Ratsupites 1, Riga, Latvia
Mol Phylogenet Evol 43:864-80. 2007Mammalian 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...
- RNA interference screen for RGS protein specificity at muscarinic and protease-activated receptors reveals bidirectional modulation of signalingGeneviève Laroche
Department of Pharmacology, Univ of North Carolina at Chapel Hill, Chapel Hill, NC, USA
Am J Physiol Cell Physiol 299:C654-64. 2010Regulator of G protein signaling (RGS) proteins are considered key modulators of G protein-coupled receptor (GPCR)-mediated signal transduction...
- Ca2+/calmodulin-dependent protein kinase IIdelta orchestrates G-protein-coupled receptor and electric field stimulation-induced cardiomyocyte hypertrophyWei Zhang
Department of Pharmacology, Nantong University Medical College, Nantong, China
Clin Exp Pharmacol Physiol 37:795-802. 20101. G-Protein-coupled receptors (GPCR) and electrical field stimulation (EFS) regulate cardiac function and pathological remodelling, including cardiac hypertrophy...
- c-Cbl mediates ubiquitination, degradation, and down-regulation of human protease-activated receptor 2Claire Jacob
Departments of Surgery and Physiology, University of California, San Francisco, California 94143 0660, USA
J Biol Chem 280:16076-87. 2005Mechanisms that arrest G-protein-coupled receptor (GPCR) signaling prevent uncontrolled stimulation that could cause disease...
- The human formyl peptide receptor as model system for constitutively active G-protein-coupled receptorsRoland 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. 2003According 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...
- P-selectin cross-links PSGL-1 and enhances neutrophil adhesion to fibrinogen and ICAM-1 in a Src kinase-dependent, but GPCR-independent mechanismTao 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...
- Activation of calcitonin receptor and calcitonin receptor-like receptor by membrane-anchored ligandsChia 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...
- Quantification of dynamic protein complexes using Renilla luciferase fragment complementation applied to protein kinase A activities in vivoE 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. 2007The 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...
- Delayed internalization and lack of recycling in a beta2-adrenergic receptor fused to the G protein alpha-subunitMaria 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. 2008Chimeric 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...
- GPCR-induced dissociation of G-protein subunits in early stage signal transductionWayne 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...
- G-protein-coupled receptor (GPCR) kinase phosphorylation and beta-arrestin recruitment regulate the constitutive signaling activity of the human cytomegalovirus US28 GPCRWilliam 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 ..
- Phospholipids are needed for the proper formation, stability, and function of the photoactivated rhodopsin-transducin complexBeata 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...
- 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. 2007Chemoperception 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...
- A beta-arrestin/green fluorescent protein biosensor for detecting G protein-coupled receptor activationL 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. 1997G 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...
- Galphaq-coupled receptor internalization specifically induced by Galphaq signaling. Regulation by EBP50Moulay 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...
- Mechanisms of desensitization of the adrenocorticotropin response to arginine vasopressin in ovine anterior pituitary cellsA Hassan
School of Biological Sciences, University of Canterbury, Christchurch, New Zealand
J Endocrinol 184:29-40. 2005..the anterior pituitary via activation of the V1b vasopressin receptor, a member of the G protein-coupled receptor (GPCR) family...
- Proteome-wide classification and identification of mammalian-type GPCRs by binary topology patternYasuhito Inoue
Department of Electronic and Information System Engineering, Faculty of Science and Technology, Hirosaki University, Hirosaki 036 8550, Japan
Comput Biol Chem 28:39-49. 2004..Here, we developed a stepwise binary topology pattern (BTP) method for GPCR classification and identification and used it to identify and classify mammalian-type GPCRs in the genomes of 10 ..
- Visual arrestin interaction with clathrin adaptor AP-2 regulates photoreceptor survival in the vertebrate retinaHormoz Moaven
Neuroscience Graduate Program, Zilkha Neurogenetic Institute, Keck School of Medicine, University of Southern California, Los Angeles, CA 90033, USA
Proc Natl Acad Sci U S A 110:9463-8. 2013..Additionally, nonvisual arrestin/GPCR complex can initiate G protein-independent intracellular signals through their ability to act as scaffolds that ..
- The role of GPCR dimerisation/oligomerisation in receptor signallingG Milligan
Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, G12 8QQ Glasgow, Scotland, UK
Ernst Schering Found Symp Proc . 2006..approaches, including co-immunoprecipitation of differentially epitope-tagged but co-expressed forms of the same GPCR, co-operativity in ligand binding and a variety of resonance energy transfer techniques (Milligan and Bouvier 2005)...
- How the dynamic properties and functional mechanisms of GPCRs are modulated by their coupling to the membrane environmentSayan Mondal
Department of Physiology and Biophysics, Weill Cornell Medical College, Cornell University, Room E 509, 1300 York Avenue, 10065, New York City, NY, USA
Adv Exp Med Biol 796:55-74. 2014..Here we review findings that offer insight into how membrane-GPCR coupling is connected to the structural characteristics of the GPCR, from sequence to 3D structural detail, and how ..
- T cell homeostasis requires G protein-coupled receptor-mediated access to trophic signals that promote growth and inhibit chemotaxisRyan M Cinalli
Abramson Family Cancer Research Institute, Departments of Cancer Biology and Medicine, University of Pennsylvania, Philadelphia, USA
Eur J Immunol 35:786-95. 2005Signals that regulate T cell homeostasis are not fully understood. G protein-coupled receptors (GPCR), such as the chemokine receptors, may affect homeostasis by direct signaling or by guiding T cell migration to distinct location-..
- GRIFFIN: a system for predicting GPCR-G-protein coupling selectivity using a support vector machine and a hidden Markov modelYukimitsu Yabuki
Computational Biology Research Center, National Institute of Advanced Industrial Science and Technology AIST, 2 42 Aomi, Koto ku, Tokyo 135 0064, Japan
Nucleic Acids Res 33:W148-53. 2005..GRIFFIN (G-protein and Receptor Interaction Feature Finding INstrument), that predicts G-protein coupled receptor (GPCR) and G-protein coupling selectivity based on a support vector machine (SVM) and a hidden Markov model (HMM) with ..
- Identification of endogenous surrogate ligands for human P2Y receptors through an in silico searchTakeshi Hiramoto
Laboratory of Pharmcoinformatics, Department of Bioscience and Biotechnology, College of Science and Engineering, Ritsumeikan University, Kusatsu, Shiga, Japan
J Pharmacol Sci 95:81-93. 2004..receptors (GPCRs) are distributed widely throughout the human body, and nearly 50% of current medicines act on a GPCR. GPCRs are considered to consist of seven transmembrane alpha-helices that form an alpha-helical bundle in which ..
- Quantitative and dynamic analyses of G protein-coupled receptor signaling in yeast using Fus1, enhanced green fluorescence protein (EGFP), and His3 fusion proteinJun Ishii
Department of Molecular Science and Material Engineering, Graduate School of Science and Technology, Kobe University, Nada Ku, Japan
Biotechnol Prog 22:954-60. 2006The mechanism of G protein-coupled receptor (GPCR) signaling in yeasts is similar to that in mammalian cells...
- Implication of Gbetagamma proteins and c-SRC tyrosine kinase in parathyroid hormone-induced signal transduction in rat enterocytesClaudia Gentili
Departamento de Biologia, Bioquimica y Farmacia, Universidad Nacional del Sur, San Juan 670, 8000 Bahia Blanca, Argentina
J Endocrinol 188:69-78. 2006Parathyroid hormone (PTH) interacts in target tissues with a G protein-coupled receptor (GPCR) localized in the plasma membrane...
- Detection of G protein-selective G protein-coupled receptor (GPCR) conformations in live cellsRabia U Malik
Department of Cell and Developmental Biology, University of Michigan, Ann Arbor, Michigan 48109, USA
J Biol Chem 288:17167-78. 2013..this study, we report on a novel class of FRET-based sensors that can detect the ligand/mutagenic stabilization of GPCR conformations that promote interactions with G proteins in live cells...
- A perspective on more effective GPCR-targeted drug discovery effortsAnnette Gilchrist
CSO, Caden Biosciences, 5500 Nobel Drive, Suite 220, Madison, WI 53711, USA 1 608 278 8646 1 608 278 8669
Expert Opin Drug Discov 3:375-89. 2008..The activation of a GPCR (usually by ligand binding) results in conformational changes that lead to G-protein coupling with subsequent ..
- Towards improved quality of GPCR models by usage of multiple templates and profile-profile comparisonDorota Latek
International Institute of Molecular and Cell Biology, Warsaw, Poland
PLoS ONE 8:e56742. 2013..Nevertheless, low sequence similarity between the GPCR family members is still a serious obstacle not only in template selection but also in providing theoretical models ..
- Similarity between class A and class B G-protein-coupled receptors exemplified through calcitonin gene-related peptide receptor modelling and mutagenesis studiesShabana Vohra
School of Biological Sciences, University of Essex, Wivenhoe Park, Colchester, UK
J R Soc Interface 10:20120846. 2013Modelling class B G-protein-coupled receptors (GPCRs) using class A GPCR structural templates is difficult due to lack of homology. The plant GPCR, GCR1, has homology to both class A and class B GPCRs...
- Direct molecular evolution of detergent-stable G protein-coupled receptors using polymer encapsulated cellsDaniel J Scott
Department of Biochemistry, University of Zurich, Winterthurerstrasse 190, 8057 Zurich, Switzerland
J Mol Biol 425:662-77. 2013..studies as well as in vitro drug screening with purified receptors require detergent solubilization of the GPCR, but typically, these proteins exhibit only low stability in detergent micelles...
- Identification of GPCR-interacting cytosolic proteins using HDL particles and mass spectrometry-based proteomic approachKa Young Chung
Department of Molecular and Cellular Physiology, Stanford University, Medical School, Beckman Center, Stanford, California, United States of America
PLoS ONE 8:e54942. 2013..Although the canonical downstream target of an agonist-activated GPCR is a G protein heterotrimer; there is a growing body of evidence suggesting that other signaling molecules interact,..
- Why GPCRs behave differently in cubic and lamellar lipidic mesophasesGeorge Khelashvili
Department of Physiology and Biophysics, Weill Cornell Medical College of Cornell University, New York, New York 10065, United States
J Am Chem Soc 134:15858-68. 2012..in the crystallographic determination of structures of transmembrane proteins in the G protein-coupled receptor (GPCR) family have established the lipidic cubic phase (LCP) environment as the medium of choice for growing structure-..
- Stimulus bias provides evidence for conformational constraints in the structure of a G protein-coupled receptorKaren J Gregory
Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, and Department of Pharmacology, Monash University, Victoria 3800, Australia
J Biol Chem 287:37066-77. 2012..It is now clear that a GPCR coupling to these pathways can be regulated selectively by ligands that differentially drive signaling down one ..
- The anterograde transport of the human neuropeptide Y2 receptor is regulated by a subtype specific mechanism mediated by the C-terminusCornelia Walther
Institute of Biochemistry, Faculty of Biosciences, Pharmacy and Psychology, Universitat Leipzig, Germany
Neuropeptides 46:335-43. 2012The export of newly synthesized proteins, including G protein-coupled receptors (GPCR), from the endoplasmic reticulum (ER) and further transport to the plasma membrane is a tightly regulated process...
- High content screening for G protein-coupled receptors using cell-based protein translocation assaysCharlotta Granas
BioImage A S, Copenhagen, Denmark
Comb Chem High Throughput Screen 8:301-9. 2005..GPCRs) have been one of the most productive classes of drug targets for several decades, and new technologies for GPCR-based discovery promise to keep this field active for years to come...
- 76 deciphering g-protein coupled receptor network during bovine conceptus development and maternal recognition of pregnancyS Mamo
School of Agriculture, Food Science and Veterinary Medicine, University College Dublin, Belfield, Dublin, Ireland
Reprod Fertil Dev 24:150. 2011G-protein coupled receptors (GPCR) comprise a large protein family of transmembrane receptors that sense molecules outside the cell to activate the signal transduction pathways inside and, ultimately, the cellular responses...
- Minireview: G protein-coupled estrogen receptor-1, GPER-1: its mechanism of action and role in female reproductive cancer, renal and vascular physiologyEdward J Filardo
Department of Medicine, Rhode Island Hospital and Brown University Medical School, 593 Eddy Street, Aldrich Building Room 708, Providence, Rhode Island 02903, USA
Endocrinology 153:2953-62. 2012Using cDNA cloning strategies commonly employed for G protein-coupled receptors (GPCR), GPCR-30 (GPR30), was isolated from mammalian cells before knowledge of its cognate ligand...
- Adaptor protein-2 interaction with arrestin regulates GPCR recycling and apoptosisBrant M Wagener
Department of Cell Biology and Physiology and UNM Cancer Research and Treatment Center, University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA
Traffic 10:1286-300. 2009..b>GPCR signaling represents an intricate balance between receptor activation, inactivation (desensitization, ..
- 5-HT receptor-associated protein networks: new targets for drug discovery in psychiatric disorders?Philippe Marin
Institut de Genomique Fonctionnelle, 141 rue de la Cardonille, Montpellier F 34094 Montpellier Cedex 5, France
Curr Drug Targets 13:28-52. 2012..Except for 5-HT3 receptors, which are cationic channels, 5-HT receptors belong to the G protein-coupled receptor (GPCR) superfamily and allow an extraordinarily diverse and complex pattern of cellular signalling...
- Prenylation-deficient G protein gamma subunits disrupt GPCR signaling in the zebrafishTimothy Mulligan
Carnegie Institution, Department of Embryology, Johns Hopkins University, Baltimore, MD 21218, United States
Cell Signal 22:221-33. 2010..membrane localization of heterotrimeric G proteins and for functional heterotrimeric G protein coupled receptor (GPCR) signaling...
- TRPC channels in pheromone sensingKirill Kiselyov
Department of Biological Sciences, University of Pittsburgh, Pittsburgh, Pennsylvania, USA
Vitam Horm 83:197-213. 2010..relies on an amplification cascade that is triggered by pheromone binding to G protein-coupled receptors (GPCR)...
- Metformin disrupts crosstalk between G protein-coupled receptor and insulin receptor signaling systems and inhibits pancreatic cancer growthKrisztina Kisfalvi
Departments of Medicine, CURE, Digestive Diseases Research Center, Molecular Biology Institute, University of California at Los Angeles, 90095 1786, USA
Cancer Res 69:6539-45. 2009Recently, we identified a novel crosstalk between insulin and G protein-coupled receptor (GPCR) signaling pathways in human pancreatic cancer cells. Insulin enhanced GPCR signaling through a rapamycin-sensitive mTOR-dependent pathway...
- Determination of adenosine A1 receptor agonist and antagonist pharmacology using Saccharomyces cerevisiae: implications for ligand screening and functional selectivityGregory D Stewart
Monash Institute of Pharmaceutical Sciences, Parkville, Victoria, Australia
J Pharmacol Exp Ther 331:277-86. 2009..protein-coupled receptors (GPCRs) to the pheromone response pathway to facilitate empirical ligand screening and/or GPCR mutagenesis studies...
- A preformed signaling complex mediates GnRH-activated ERK phosphorylation of paxillin and FAK at focal adhesions in L beta T2 gonadotrope cellsMasha Dobkin-Bekman
Department of Biochemistry, George S Wise Faculty of Life Sciences, Tel Aviv University, Tel Aviv 69978, Israel
Mol Endocrinol 23:1850-64. 2009..Also, most GPCR ligands utilize families of receptors for mediation of diverse biological actions; however, the mammalian type I ..
- Targeting platelet G-protein coupled receptors (GPCRs): looking beyond conventional GPCR antagonismLouisa Dowal
Division of Hemostasis and Thrombosis, Department of Medicine, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA 02215, USA
Curr Vasc Pharmacol 8:140-54. 2010..A more detailed understanding of GPCR function is leading to the development of pharmacophores with novel mechanisms of drug action...
- Study of GPCR-protein interactions by BRETMartina Kocan
Drug Discovery Biology Laboratory, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Melbourne, Royal Parade, Parkvile, Victoria, Australia
Methods Mol Biol 746:357-71. 2011..This technique is highly amenable to the monitoring of G protein-coupled receptor (GPCR)-protein interactions, especially involving scaffolding, regulatory and signaling proteins, such as β-arrestins, ..
- Human cannabinoid 1 GPCR C-terminal domain interacts with bilayer phospholipids to modulate the structure of its membrane environmentElvis K Tiburu
Center for Drug Discovery and Department of Chemistry and Chemical Biology, Northeastern University, 360 Huntington Avenue, 116 Mugar Hall, Boston, Massachusetts 02115 5000, United States of America
AAPS J 13:92-8. 2011G protein-coupled receptors (GPCRs) play critical physiological and therapeutic roles. The human cannabinoid 1 GPCR (hCB1) is a prime pharmacotherapeutic target for addiction and cardiometabolic disease...
- Mechanism and function of Drosophila capa GPCR: a desiccation stress-responsive receptor with functional homology to human neuromedinU receptorSelim Terhzaz
Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, United Kingdom
PLoS ONE 7:e29897. 2012The capa peptide receptor, capaR (CG14575), is a G-protein coupled receptor (GPCR) for the D. melanogaster capa neuropeptides, Drm-capa-1 and -2 (capa-1 and -2)...
- Separation and reformation of cell surface dopamine receptor oligomers visualized in cellsBrian F O'Dowd
Centre for Addiction and Mental Health, University of Toronto, Toronto, Ontario, Canada
Eur J Pharmacol 658:74-83. 2011..We developed a method designed to study the formation and regulation of G protein coupled receptor (GPCR) oligomers in cells, using a GPCR into which a nuclear localization sequence (NLS) had been inserted...
- Mass spectrometry-based GPCR proteomics: comprehensive characterization of the human cannabinoid 1 receptorNikolai Zvonok
Northeastern University, Center for Drug Discovery, 116 Mugar Life Sciences Building, Boston, Massachusetts 02115, USA
J Proteome Res 9:1746-53. 2010The human cannabinoid 1 receptor (hCB1), a ubiquitous G protein-coupled receptor (GPCR), transmits cannabinergic signals that participate in diverse (patho)physiological processes...
- Thymoquinone from nutraceutical black cumin oil activates Neu4 sialidase in live macrophage, dendritic, and normal and type I sialidosis human fibroblast cells via GPCR Galphai proteins and matrix metalloproteinase-9Trisha M Finlay
Department of Microbiology and Immunology, Queen s University, Kingston, ON, K7L3N6, Canada
Glycoconj J 27:329-48. 2010..Pertussis toxin (PTX), a specific inhibitor of Galphai proteins of G-protein coupled receptor (GPCR) and the broad range inhibitors of matrix metalloproteinase (MMP) galardin and piperazine applied to live BMC-2, ..
- Exploring a role for heteromerization in GPCR signalling specificityRaphael Rozenfeld
Department of Pharmacology and Systems Therapeutics, Mount Sinai School of Medicine, New York, NY 10029, USA
Biochem J 433:11-8. 2011..Recent advances in GPCR pharmacology have demonstrated that different ligands binding to the same receptor can activate discrete sets of ..
- The year in G protein-coupled receptor researchRobert P Millar
Medical Research Council MRC Human Reproductive Sciences Unit, The Queen s Medical Research Institute, Edinburgh, Scotland, United Kingdom
Mol Endocrinol 24:261-74. 2010..From these recent technical advances, we can anticipate that many more GPCR structures will emerge, which will afford us greater insight into their common and unique structural features and, ..
- GRIPDB - G protein coupled Receptor Interaction Partners DataBaseWataru Nemoto
Computational Biology Research Center CBRC, Advanced Industrial Science and Technology AIST, AIST Tokyo, Japan
J Recept Signal Transduct Res 31:199-205. 2011The G protein Coupled Receptor (GPCR) superfamily is one of the most important pharmaceutical targets. Studies of GPCRs have long been performed under the assumption that GPCRs function as monomers...
- G protein-coupled receptor kinases in normal and failing myocardiumZheng Maggie Huang
Center for Translational Medicine and George Zallie and Family Laboratory for Cardiovascular Gene Therapy, Department of Medicine, Thomas Jefferson University, Philadelphia, PA, USA
Front Biosci (Landmark Ed) 16:3047-60. 2011..One of the striking characteristics of HF is the desensitization of G protein-coupled receptor (GPCR) signaling, particularly the beta-adrenergic receptor (betaAR) system...
- Extracellular osmolarity modulates G protein-coupled receptor-dependent ATP release from 1321N1 astrocytoma cellsAndrew E Blum
Department of Physiology and Biophysics, Case Western Reserve University School of Medicine, Cleveland, OH 44120, USA
Am J Physiol Cell Physiol 298:C386-96. 2010..from 1321N1 human astrocytoma cells could be stimulated either by activation of G protein-coupled receptors (GPCR) or by hypotonic stress. Cheema et al. (Cheema TA, Ward CE, Fisher SK...
- GPCR-2L: predicting G protein-coupled receptors and their types by hybridizing two different modes of pseudo amino acid compositionsXuan Xiao
Computer Department, Jing De Zhen Ceramic Institute, Jing De Zhen 333403, China
Mol Biosyst 7:911-9. 2011..The new predictor is called GPCR-2L, where "2L" means that it is a two-layer predictor: the 1st layer prediction engine is to identify a query ..
- Functional diversity of signaling pathways through G protein-coupled receptor heterodimerization with a species-specific orphan receptor subtypeTsubasa Sakai
Division of Biomolecular Research, Suntory Institute for Bioorganic Research, Osaka, Japan
Mol Biol Evol 27:1097-106. 2010..several signal transduction cascades via GnRH receptors (GnRHRs), members of the G protein-coupled receptor (GPCR) family...
- GPCR-CA: A cellular automaton image approach for predicting G-protein-coupled receptor functional classesXuan Xiao
Computer Department, Jing De Zhen Ceramic Institute, Jing De Zhen 33300, China
J Comput Chem 30:1414-23. 2009Given an uncharacterized protein sequence, how can we identify whether it is a G-protein-coupled receptor (GPCR) or not? If it is, which functional family class does it belong to? It is important to address these questions because GPCRs ..
- Multiple activation steps of the N-formyl peptide receptorE R Prossnitz
Department of Cell Biology and Physiology, University of New Mexico Health Science Center, Albuquerque 87131, USA
Biochemistry 38:2240-7. 1999The human N-formyl peptide receptor (FPR) is representative of a growing family of G protein-coupled receptors (GPCR) that respond to chemokines and chemoattractants...
- Large-scale analysis of gene structure in rhodopsin-like GPCRs: evidence for widespread loss of an ancient intronRobert J Bryson-Richardson
MRC Human Genetics Unit, Western General Hospital, Edinburgh, EH4 2XU, UK
Gene 338:15-23. 2004..Mammalian GPCR genes are reputed to be largely intron-deficient, but there have been no reports of using genome-wide analyses of ..
- Lower rate of genomic variation identified in the trans-membrane domain of monoamine sub-class of Human G-Protein Coupled Receptors: the Human GPCR-DB DatabaseClaes Wahlestedt
Center for Genomics and Bioinformatics, Karolinska Institutet, Berzelius vag 35, 17177 Stockholm, Sweden
BMC Genomics 5:91. 2004..b>GPCR receptors of physiological and clinical importance were prioritized for statistical analysis...
- Ventricular zone gene-1 (vzg-1) encodes a lysophosphatidic acid receptor expressed in neurogenic regions of the developing cerebral cortexJ H Hecht
Department of Biology, University of California, San Diego, La Jolla 92093 0636, USA
J Cell Biol 135:1071-83. 1996Neocortical neuroblast cell lines were used to clone G-protein-coupled receptor (GPCR) genes to study signaling mechanisms regulating cortical neurogenesis...
- KSHV-GPCR and CXCR2 transforming capacity and angiogenic responses are mediated through a JAK2-STAT3-dependent pathwayMeike Burger
Department of Internal Medicine, Freiburg University Hospital, Freiburg, Germany
Oncogene 24:2067-75. 2005The Kaposi's sarcoma herpesvirus encodes a G-protein-coupled chemokine receptor termed KSHV-GPCR. Expression of this constitutively active GPCR leads to cell transformation and vascular overgrowth characteristic of Kaposi's sarcoma...
- Probing the beta2 adrenoceptor binding site with catechol reveals differences in binding and activation by agonists and partial agonistsGayathri Swaminath
Department of Molecular and Cellular Physiology, Stanford University School of Medicine, 157 Beckman Circle, Stanford, CA 94305, USA
J Biol Chem 280:22165-71. 2005The beta(2) adrenergic receptor (beta(2)AR) is a prototypical family A G protein-coupled receptor (GPCR) and an excellent model system for studying the mechanism of GPCR activation...
- S-nitrosothiols modulate G protein-coupled receptor signaling in a reversible and highly receptor-specific mannerTarja Kokkola
Department of Physiology, University of Kuopio, POB 1627, FIN 70211, Kuopio, Finland
BMC Cell Biol 6:21. 2005Recent studies indicate that the G protein-coupled receptor (GPCR) signaling machinery can serve as a direct target of reactive oxygen species, including nitric oxide (NO) and S-nitrosothiols (RSNOs)...
- Vascular smooth muscle overexpression of G protein-coupled receptor kinase 5 elevates blood pressure, which segregates with sex and is dependent on Gi-mediated signalingJanelle R Keys
Department of Surgery, Duke University Medical Center, Durham, NC, USA
Circulation 112:1145-53. 2005..In addition, increased levels of G protein-coupled receptor (GPCR) kinases (GRKs), which regulate GPCR signaling, are associated with increased blood pressure (BP).
- Emerging concepts in GPCR function--the influence of cell phenotype on GPCR pharmacologyRichard M Eglen
DiscoveRx Corp, 42501 Albrae St, Fremont, CA 94538, USA
Proc West Pharmacol Soc 48:31-4. 2005..It is now appears that GPCR function is highly dependent upon the cellular environment in which it is expressed...
- Selective modulation of GPCR signal transduction with biased ligandsMICHAEL 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 ..
- 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...
- Neurokinin 3 Receptor: Nuclear Localization in Supraoptic NeuronsCELIA 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 ..
- Developing Methods for Crystallizing Class B GPCRsHO LEUNG NG; Fiscal Year: 2009..At present, only a handful of GPCR structures have been solved, and none within the Class B GPCR subfamily...
- Efficient and Sensitive Mining System for G-Protein Coupled ReceptorsEtsuko 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...
- Desensitization of neuronal G-protein coupled receptorsJonathon Wetherington; Fiscal Year: 2002..In many cases GPCR desensitization is mediated by a well- conserved mechanism involving receptor phosphorylation, internalization, and ..
- G Protein-Coupled Receptors - Kobilka, ChairAndrew 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 ..
- ARRESTINS IN G PROTEIN-COUPLE RECEPTOR REGULATIONJEFFREY 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 ..
- G PROTEINS AND SIGNAL TRANSDUCTION IN NEUROSPORA CRASSAKATHERINE 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...
- Novel GPCR Kinase Interactions in Macrophages and Role in ArthritisNarayanan 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...
- Targeting crosstalk between insulin and Gq signaling systems in pancreatic cancerJUAN 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 ..
- Screening Method for GPCRs Related to AppetiteMARIA 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...
- Screening Method for GPCRs Related to AppetiteCAMILLE 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...
- MECHANISMS FOR GPCR TRAFFICKING IN POLARIZED CELLSLEE 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...