g protein coupled receptors

Summary

Summary: The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.

Top Publications

  1. ncbi The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints
    Robert Fredriksson
    Department of Neuroscience, Biomedical Center, Box 593, 75 124 Uppsala, Sweden
    Mol Pharmacol 63:1256-72. 2003
  2. ncbi Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior
    T Sakurai
    Howard Hughes Medical Institute, Department of Molecular Genetics, University of Texas Southwestern Medical Center at Dallas, 75235 9050, USA
    Cell 92:573-85. 1998
  3. ncbi Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40
    Yasuaki Itoh
    Discovery Research Laboratories I, Pharmaceutical Research Division, Takeda Chemical Industries, Ltd, Wadai 10, Tsukuba, Ibaraki 300 4293, Japan
    Nature 422:173-6. 2003
  4. ncbi A transmembrane intracellular estrogen receptor mediates rapid cell signaling
    Chetana M Revankar
    Department of Cell Biology and Physiology, University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA
    Science 307:1625-30. 2005
  5. ncbi The GPR54 gene as a regulator of puberty
    Stephanie B Seminara
    Reproductive Endocrine Unit, Massachusetts General Hospital, Boston, MA 02114, USA
    N Engl J Med 349:1614-27. 2003
  6. pmc Inhibition of Hedgehog signaling by direct binding of cyclopamine to Smoothened
    James K Chen
    Department of Molecular Biology and Genetics, Howard Hughes Medical Institute, Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA
    Genes Dev 16:2743-8. 2002
  7. ncbi Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120
    Akira Hirasawa
    Department of Molecular, Cell Pharmacology, National Research Institute for Child Health and Development, 3 35 31, Taishi do, Setagaya Ku, Tokyo 154 8567, Japan
    Nat Med 11:90-4. 2005
  8. ncbi Wnt signaling: a common theme in animal development
    K M Cadigan
    Howard Hughes Medical Institute, Department of Developmental Biology, Beckman Center, Stanford University Medical Center, Stanford, California 94305 5323, USA
    Genes Dev 11:3286-305. 1997
  9. ncbi Crystal structure of the ligand-free G-protein-coupled receptor opsin
    Jung Hee Park
    Institut für Medizinische Physik und Biophysik CC2, Charite Universitatsmedizin Berlin, Chariteplatz 1, D 10117 Berlin, Germany
    Nature 454:183-7. 2008
  10. pmc Small molecule modulation of Smoothened activity
    James K Chen
    Department of Molecular Biology and Genetics, Howard Hughes Medical Institute, Johns Hopkins University School of Medicine, Baltimore, MD 21205, USA
    Proc Natl Acad Sci U S A 99:14071-6. 2002

Detail Information

Publications373 found, 100 shown here

  1. ncbi The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints
    Robert Fredriksson
    Department of Neuroscience, Biomedical Center, Box 593, 75 124 Uppsala, Sweden
    Mol Pharmacol 63:1256-72. 2003
    ..Our novel approach of analyzing such large and diverse sequence sets may be useful for studies on GPCRs in other genomes and divergent protein families...
  2. ncbi Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior
    T Sakurai
    Howard Hughes Medical Institute, Department of Molecular Genetics, University of Texas Southwestern Medical Center at Dallas, 75235 9050, USA
    Cell 92:573-85. 1998
    ..prepro-orexin mRNA level is up-regulated upon fasting, suggesting a physiological role for the peptides as mediators in the central feedback mechanism that regulates feeding behavior...
  3. ncbi Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40
    Yasuaki Itoh
    Discovery Research Laboratories I, Pharmaceutical Research Division, Takeda Chemical Industries, Ltd, Wadai 10, Tsukuba, Ibaraki 300 4293, Japan
    Nature 422:173-6. 2003
    ..Our results indicate that GPR40 agonists and/or antagonists show potential for the development of new anti-diabetic drugs...
  4. ncbi A transmembrane intracellular estrogen receptor mediates rapid cell signaling
    Chetana M Revankar
    Department of Cell Biology and Physiology, University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA
    Science 307:1625-30. 2005
    ..Thus, GPR30 represents an intracellular transmembrane estrogen receptor that may contribute to normal estrogen physiology as well as pathophysiology...
  5. ncbi The GPR54 gene as a regulator of puberty
    Stephanie B Seminara
    Reproductive Endocrine Unit, Massachusetts General Hospital, Boston, MA 02114, USA
    N Engl J Med 349:1614-27. 2003
    ..We conducted studies in humans and mice to identify the genetic factors that determine the onset of puberty...
  6. pmc Inhibition of Hedgehog signaling by direct binding of cyclopamine to Smoothened
    James K Chen
    Department of Molecular Biology and Genetics, Howard Hughes Medical Institute, Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA
    Genes Dev 16:2743-8. 2002
    ..These observations reveal the mechanism of cyclopamine's teratogenic and antitumor activities and further suggest a role for small molecules in the physiological regulation of Smo...
  7. ncbi Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120
    Akira Hirasawa
    Department of Molecular, Cell Pharmacology, National Research Institute for Child Health and Development, 3 35 31, Taishi do, Setagaya Ku, Tokyo 154 8567, Japan
    Nat Med 11:90-4. 2005
    ..Because GLP-1 is the most potent insulinotropic incretin, our results indicate that GPR120-mediated GLP-1 secretion induced by dietary FFAs is important in the treatment of diabetes...
  8. ncbi Wnt signaling: a common theme in animal development
    K M Cadigan
    Howard Hughes Medical Institute, Department of Developmental Biology, Beckman Center, Stanford University Medical Center, Stanford, California 94305 5323, USA
    Genes Dev 11:3286-305. 1997
  9. ncbi Crystal structure of the ligand-free G-protein-coupled receptor opsin
    Jung Hee Park
    Institut für Medizinische Physik und Biophysik CC2, Charite Universitatsmedizin Berlin, Chariteplatz 1, D 10117 Berlin, Germany
    Nature 454:183-7. 2008
    ..The opsin structure sheds new light on ligand binding to GPCRs and on GPCR activation...
  10. pmc Small molecule modulation of Smoothened activity
    James K Chen
    Department of Molecular Biology and Genetics, Howard Hughes Medical Institute, Johns Hopkins University School of Medicine, Baltimore, MD 21205, USA
    Proc Natl Acad Sci U S A 99:14071-6. 2002
    ..The mechanistic differences between the Smo antagonists may be useful in the therapeutic manipulation of Hh signaling...
  11. pmc Kisspeptin directly stimulates gonadotropin-releasing hormone release via G protein-coupled receptor 54
    Sophie Messager
    Paradigm Therapeutics, 214 Cambridge Science Park, Milton Road, Cambridge CB4 0WA, United Kingdom
    Proc Natl Acad Sci U S A 102:1761-6. 2005
    ..The localization and GnRH release effects of kisspeptin thus define GPR54 as a major control point in the reproductive axis and suggest kisspeptin to be a neurohormonal effector...
  12. ncbi Activating Smoothened mutations in sporadic basal-cell carcinoma
    J Xie
    Department of Dermatology, San Francisco General Hospital, University of California, 94110, USA
    Nature 391:90-2. 1998
    ..These findings support the role of SMO as a signalling component of the SHH-receptor complex and provide direct evidence that mutated SMO can function as an oncogene in BCCs...
  13. ncbi Flamingo, a seven-pass transmembrane cadherin, regulates planar cell polarity under the control of Frizzled
    T Usui
    Department of Biophysics, Faculty of Science, Japan
    Cell 98:585-95. 1999
    ..These results, together with phenotypes caused by ectopic expression of fz and fmi, suggest that cells acquire the P-D polarity by way of the Fz-dependent boundary localization of Fmi...
  14. ncbi G-protein-coupled receptors and cancer
    Robert T Dorsam
    Oral and Pharyngeal Cancer Branch, National Institute of Dental and Craniofacial Research, National Institutes of Health, Bethesda, Maryland 20892 4330, USA
    Nat Rev Cancer 7:79-94. 2007
    ..We will also discuss how interfering with GPCRs might provide unique opportunities for cancer prevention and treatment...
  15. ncbi Structural diversity of G protein-coupled receptors and significance for drug discovery
    Malin C Lagerström
    Department of Neuroscience, Functional Pharmacology, Uppsala University, BMC, Box 593, 751 24, Uppsala, Sweden
    Nat Rev Drug Discov 7:339-57. 2008
    ....
  16. pmc Angiotensin-(1-7) is an endogenous ligand for the G protein-coupled receptor Mas
    Robson A S Santos
    Department of Physiology and Biophysics, Federal University of Minas Gerais, Belo Horizonte, 31270, Minas Gerais, Brazil
    Proc Natl Acad Sci U S A 100:8258-63. 2003
    ..Collectively, these findings identify Mas as a functional receptor for Ang-(1-7) and provide a clear molecular basis for the physiological actions of this biologically active peptide...
  17. ncbi A mutation in a case of early onset narcolepsy and a generalized absence of hypocretin peptides in human narcoleptic brains
    C Peyron
    Center for Narcolepsy, Stanford University Medical School 1201 Welch Road, Stanford, California 94305 5485, USA
    Nat Med 6:991-7. 2000
    ..Although hypocretin loci do not contribute significantly to genetic predisposition, most cases of human narcolepsy are associated with a deficient hypocretin system...
  18. ncbi The molecular receptive ranges of human TAS2R bitter taste receptors
    Wolfgang Meyerhof
    Department of Molecular Genetics, German Institute of Human Nutrition Potsdam Rehbruecke, Arthur Scheunert Allee 114 116, 14558 Nuthetal, Germany
    Chem Senses 35:157-70. 2010
    ..Conversely, though 63 bitter substances activated only 1-3 receptors, 19 compounds stimulated up to 15 hTAS2Rs. Our data suggest that the detection of the numerous bitter chemicals is related to the molecular receptive ranges of hTAS2Rs...
  19. ncbi The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54
    M Kotani
    Institut de Recherche Interdisciplinare en Biologie Humaine et Nucléaire I R I B H N, Brussels, Belgium
    J Biol Chem 276:34631-6. 2001
    ..Stimulation of oxytocin secretion after kisspeptin administration to rats confirmed this hypothesis...
  20. ncbi The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids
    Celia P Briscoe
    Department of Metabolic Diseases, GlaxoSmithKline, Research Triangle Park, North Carolina 27709, USA
    J Biol Chem 278:11303-11. 2003
    ..These data suggest that some of the physiological effects of fatty acids in pancreatic islets and brain may be mediated through a cell-surface receptor...
  21. ncbi Estrogen-induced activation of Erk-1 and Erk-2 requires the G protein-coupled receptor homolog, GPR30, and occurs via trans-activation of the epidermal growth factor receptor through release of HB-EGF
    E J Filardo
    Department of Medicine and Surgery, Rhode Island Hospital and Brown University, Providence 02903, USA
    Mol Endocrinol 14:1649-60. 2000
    ..Our data imply that ER-negative breast tumors that continue to express GPR30 may use estrogen to drive growth factor-dependent cellular responses...
  22. pmc Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules
    Celia P Briscoe
    Department of Metabolic Diseases, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA
    Br J Pharmacol 148:619-28. 2006
    ..5. These results add further evidence to a link between GPR40 and the ability of fatty acids to acutely potentiate insulin secretion and demonstrate that small-molecule GPR40 agonists are glucose-sensitive insulin secretagogues...
  23. ncbi Isolation and characterization of a novel endogenous peptide ligand for the human APJ receptor
    K Tatemoto
    Institute for Molecular and Cellular Regulation, Gunma University, Maebashi, 371 8512, Japan
    Biochem Biophys Res Commun 251:471-6. 1998
    ....
  24. ncbi Estrogen signaling through the transmembrane G protein-coupled receptor GPR30
    Eric R Prossnitz
    Department of Cell Biology and Physiology, University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA
    Annu Rev Physiol 70:165-90. 2008
    ..In this review, we provide an overview of the evidence for the cellular and physiological actions of GPR30 in estrogen-dependent processes and discuss the relationship of GPR30 with classical estrogen receptors...
  25. ncbi Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells
    P Thomas
    University of Texas Marine Science Institute, 750 Channel View Drive, Port Aransas, Texas 78373, USA
    Endocrinology 146:624-32. 2005
    ..The identification of a second distinct class of GPCR-like steroid membrane receptors suggests a widespread role for GPCRs in nonclassical steroid hormone actions...
  26. ncbi The tumour-suppressor gene patched encodes a candidate receptor for Sonic hedgehog
    D M Stone
    Department of Neuroscience, Genentech, Inc, South San Francisco, California 94080, USA
    Nature 384:129-34. 1996
    ..These findings, combined with available genetic evidence from Drosophila, support the hypothesis that Ptc is a receptor for Shh, and that vSmo could be a signalling component that is linked to Ptc...
  27. ncbi Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1
    Mehrdad Matloubian
    Howard Hughes Medical Institute and Department of Microbiology, University of California San Francisco, 513 Parnassus Avenue, San Francisco, California 94143 0414, USA
    Nature 427:355-60. 2004
    ..These findings establish that S1P1 is essential for lymphocyte recirculation and that it regulates egress from both thymus and peripheral lymphoid organs...
  28. ncbi Differential expression of orexin receptors 1 and 2 in the rat brain
    J N Marcus
    Department of Neurobiology, Harvard Medical School, Boston, Massachusetts 02215, USA
    J Comp Neurol 435:6-25. 2001
    ..The differential distribution of orexin receptors is consistent with the proposed multifaceted roles of orexin in regulating homeostasis and may explain the unique role of the OX(2)R receptor in regulating sleep state stability...
  29. ncbi Free fatty acid receptor 1 (FFA(1)R/GPR40) and its involvement in fatty-acid-stimulated insulin secretion
    A Salehi
    Section of Diabetes and Endocrinology, BMC B11, 22184 Lund, Sweden
    Cell Tissue Res 322:207-15. 2005
    ..The results demonstrate that FFA(1)R/GPR40 is inhibited by the CPT-1 inhibitor, 2BrP, and confirm that FFA(1)R/GPR40 is indeed necessary, at least in part, for fatty-acid-stimulated insulin release...
  30. ncbi A role for kisspeptins in the regulation of gonadotropin secretion in the mouse
    M L Gottsch
    Department of Physiology and Biophysics Health Sciences Building, G 424 School of Medicine University of Washington, Box 357290, 1959 Northeast Pacific Street, Seattle, Washington 98195 7290, USA
    Endocrinology 145:4073-7. 2004
    ..We conclude that kisspeptin-GPR54 signaling may be part of the hypothalamic circuitry that governs the hypothalamic secretion of GnRH...
  31. ncbi The tissue distribution of the mRNA of ghrelin and subtypes of its receptor, GHS-R, in humans
    Sharmilee Gnanapavan
    Department of Endocrinology, St Bartholomew s and The Royal London Hospital, London ECIA 7BE, UK
    J Clin Endocrinol Metab 87:2988. 2002
    ..These data suggest that ghrelin might have widespread physiological effects via different, partly unidentified, subtypes of the GHS-R in endocrine and non-endocrine tissues...
  32. ncbi Expression of G protein coupled receptors in a cell-free translational system using detergents and thioredoxin-fusion vectors
    Goshi Ishihara
    RIKEN Genomic Sciences Center, 1 7 22 Suehiro cho, Tsurumi, Yokohama 230 0045, Japan
    Protein Expr Purif 41:27-37. 2005
    ..coli S30 extract, with G protein coupled receptors (GPCRs) as the target integral membrane proteins...
  33. ncbi Binding and activation of the seven-transmembrane estrogen receptor GPR30 by environmental estrogens: a potential novel mechanism of endocrine disruption
    Peter Thomas
    Marine Science Institute, University of Texas at Austin, 750 Channel View Drive, Port Aransas, TX 78373, USA
    J Steroid Biochem Mol Biol 102:175-9. 2006
    ..The results indicate that nontraditional estrogen actions mediated through GPR30 are potentially susceptible to disruption by a variety of environmental estrogens...
  34. pmc Gpr40 is expressed in enteroendocrine cells and mediates free fatty acid stimulation of incretin secretion
    Sara Edfalk
    Umeå Center for Molecular Medicine, University of Umea, Umea, Sweden
    Diabetes 57:2280-7. 2008
    ..Here, we addressed whether 1) Gpr40 is expressed in the intestine and 2) Ipf1/Pdx1 function is required for Gpr40 expression...
  35. ncbi Vertebrate Smoothened functions at the primary cilium
    Kevin C Corbit
    Developmental and Stem Cell Biology Program, University of California, San Francisco, California 94143, USA
    Nature 437:1018-21. 2005
    ..Thus, Hh-dependent translocation to cilia is essential for Smo activity, suggesting that Smo acts at the primary cilium...
  36. ncbi Mammalian Ryk is a Wnt coreceptor required for stimulation of neurite outgrowth
    Wange Lu
    California Institute of Technology, Division of Biology, Pasadena, CA 91125, USA
    Cell 119:97-108. 2004
    ..Thus, Ryk appears to play a crucial role in Wnt-mediated signaling...
  37. pmc Hedgehog signaling is restricted to the stromal compartment during pancreatic carcinogenesis
    Hua Tian
    Department of Molecular Biology, Genentech, Incorporated, 1 DNA Way, South San Francisco, CA 94080, USA
    Proc Natl Acad Sci U S A 106:4254-9. 2009
    ..These data support a paracrine model of Hh-mediated tumorigenesis, in which tumor cells secrete Hh ligand to induce tumor-promoting Hh target genes in adjacent stroma...
  38. pmc The structural basis of arrestin-mediated regulation of G-protein-coupled receptors
    Vsevolod V Gurevich
    Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA
    Pharmacol Ther 110:465-502. 2006
    ....
  39. ncbi Positional cloning of the human quantitative trait locus underlying taste sensitivity to phenylthiocarbamide
    Un Kyung Kim
    National Institute on Deafness and Other Communication Disorders, National Institutes of Health, 5 Research Court, Rockville, MD 20850, USA
    Science 299:1221-5. 2003
    ....
  40. ncbi Interaction between the corticotropin-releasing factor system and hypocretins (orexins): a novel circuit mediating stress response
    Raphaelle Winsky-Sommerer
    Department of Molecular Biology, The Scripps Research Institute, La Jolla, California 92037, USA
    J Neurosci 24:11439-48. 2004
    ..We propose that, after stressor stimuli, CRF stimulates the release of hypocretins and that this circuit contributes to activation and maintenance of arousal associated with the stress response...
  41. ncbi A paracrine requirement for hedgehog signalling in cancer
    Robert L Yauch
    Genentech Inc, 1 DNA Way, South San Francisco, California 94080, USA
    Nature 455:406-10. 2008
    ..Taken together, these studies demonstrate a paracrine requirement for Hh ligand signalling in the tumorigenesis of Hh-expressing cancers and have important implications for the development of Hh pathway antagonists in cancer...
  42. pmc Generation of functional multipotent adult stem cells from GPR125+ germline progenitors
    Marco Seandel
    Howard Hughes Medical Institute, Department of Genetic Medicine, Weill Cornell Medical College, New York 10065, USA
    Nature 449:346-50. 2007
    ....
  43. ncbi Drosophila CRY is a deep brain circadian photoreceptor
    P Emery
    Department of Biology, National Science Foundation Center for Biological Timing, Waltham, Massachusetts 02454, USA
    Neuron 26:493-504. 2000
    ..These brain neurons therefore contain an identified deep brain photoreceptor, as well as the other circadian elements: a central pace-maker and a behavioral output system...
  44. ncbi G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth response to 17beta-estradiol and selective GPR30 ligand G-1 in ovarian cancer cells
    Lidia Albanito
    Departments of Pharmaco Biology and Cell Biology, University of Calabria, 87030 Rende Cosenza, Italy
    Cancer Res 67:1859-66. 2007
    ....
  45. ncbi Distribution of GPR30, a seven membrane-spanning estrogen receptor, in primary breast cancer and its association with clinicopathologic determinants of tumor progression
    Edward J Filardo
    Department of Medicine, Rhode Island Hospital, and Department of Pathology, Brown University School of Medicine, Providence, Rhode Island 02903, USA
    Clin Cancer Res 12:6359-66. 2006
    ..Here, the significance of GPR30 in human breast cancer was evaluated by comparing its relationship to steroid hormone receptor expression and tumor progression variables...
  46. ncbi Mutant frizzled-4 disrupts retinal angiogenesis in familial exudative vitreoretinopathy
    Johane Robitaille
    Department of Ophthalmology, Izaak Walton Killam IWK Health Centre, Dalhousie University, Halifax, Nova Scotia B3H 2Y9, Canada
    Nat Genet 32:326-30. 2002
    ..In one of the mutants, altered subcellular trafficking led to defective signaling. These findings support a function for frizzled-4 in retinal angiogenesis and establish the first association between a Wnt receptor and human disease...
  47. ncbi Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents
    Hilary A Overton
    OSI Prosidion, Windrush Court, Watlington Road, Oxford OX4 6LT, UK
    Cell Metab 3:167-75. 2006
    ..GPR119 therefore represents a novel and attractive potential target for the therapy of obesity and related metabolic disorders...
  48. ncbi A G protein-coupled receptor responsive to bile acids
    Yuji Kawamata
    Discovery Research Laboratories 1, Pharmaceutical Research Division, Takeda Chemical Industries, Ltd, Wadai 10, Tsukuba, Ibaraki 300 4293, Japan
    J Biol Chem 278:9435-40. 2003
    ....
  49. ncbi Expression and regulation of the prokineticins (endocrine gland-derived vascular endothelial growth factor and Bv8) and their receptors in the human endometrium across the menstrual cycle
    S Battersby
    Department of Reproductive and Developmental Sciences, Centre for Reproductive Biology, University of Edinburgh, Edinburgh EH16 4SB, United Kingdom
    J Clin Endocrinol Metab 89:2463-9. 2004
    ..91 +/- 0.75-fold elevation in PK1 expression, compared with controls (P < 0.05). These data identify a paracrine role for the PKs and their receptors in endometrial vascular function...
  50. ncbi Molecular mechanisms of ligand binding, signaling, and regulation within the superfamily of G-protein-coupled receptors: molecular modeling and mutagenesis approaches to receptor structure and function
    Kurt Kristiansen
    Department of Pharmacology, Institute of Medical Biology, University of Tromsø, N 9037 Tromsø, Norway
    Pharmacol Ther 103:21-80. 2004
    ..Constitutively activating mutations or agonist binding disrupts such constraining interactions leading to receptor conformations that associates with and activate G-proteins...
  51. ncbi Developmental and hormonally regulated messenger ribonucleic acid expression of KiSS-1 and its putative receptor, GPR54, in rat hypothalamus and potent luteinizing hormone-releasing activity of KiSS-1 peptide
    V M Navarro
    Physiology Section, Department of Cell Biology, Physiology, and Immunology, Faculty of Medicine, University of Cordoba, Avda Menendez Pidal s n, 14004 Cordoba, Spain
    Endocrinology 145:4565-74. 2004
    ..Our current data support the contention that the hypothalamic KiSS-1/GPR54 system is a pivotal factor in central regulation of the gonadotropic axis at puberty and in adulthood...
  52. ncbi Estrogen action via the G protein-coupled receptor, GPR30: stimulation of adenylyl cyclase and cAMP-mediated attenuation of the epidermal growth factor receptor-to-MAPK signaling axis
    Edward J Filardo
    Department of Surgery, Rhode Island Hospital, and Brown University, Providence, Rhode Island 02903, USA
    Mol Endocrinol 16:70-84. 2002
    ....
  53. ncbi A diverse family of GPCRs expressed in specific subsets of nociceptive sensory neurons
    X Dong
    Division of Biology 216-76, California Institute of Technology, Pasadena, CA 91125, USA
    Cell 106:619-32. 2001
    ..Thus, mrgs may regulate nociceptor function and/or development, including the sensation or modulation of pain...
  54. ncbi The human TAS2R16 receptor mediates bitter taste in response to beta-glucopyranosides
    Bernd Bufe
    Department of Molecular Genetics, German Institute of Human Nutrition, Arthur Scheunert Allee 114 116, 14558 Potsdam Rehbrücke, Germany
    Nat Genet 32:397-401. 2002
    ..If the ability of TAS2R16 to detect substances with common molecular properties is typical of the bitter receptor family, it may explain how a few receptors permit the perception of numerous bitter substances...
  55. ncbi International Union of Pharmacology. XLVI. G protein-coupled receptor list
    Steven M Foord
    GlaxoSmithKline Research and Development, Stevenage, Hertfordshire, UK
    Pharmacol Rev 57:279-88. 2005
    ..nlm.nih.gov/entrez/query.fcgi?db=gene). This list is a major new initiative of NC-IUPHAR that, through continuing curation, defines the target of our ongoing receptor classification and invites further input from the scientific community...
  56. ncbi Signaling from Smo to Ci/Gli: conservation and divergence of Hedgehog pathways from Drosophila to vertebrates
    Danwei Huangfu
    Developmental Biology Program, Sloan Kettering Institute, 1275 York Avenue, New York, NY 10021, USA
    Development 133:3-14. 2006
    ..These include intra-flagellar transport proteins, which link vertebrate Hh signaling to cilia. Because abnormal Hh signaling can cause birth defects and cancer, these vertebrate-specific components may have roles in human health...
  57. pmc Planar polarization in embryonic epidermis orchestrates global asymmetric morphogenesis of hair follicles
    Danelle Devenport
    Howard Hughes Medical Institute, Laboratory of Mammalian Cell Biology and Development, The Rockefeller University, New York, NY 10065, USA
    Nat Cell Biol 10:1257-68. 2008
    ..Finally, we provide in vitro evidence that homotypic intracellular interactions of Celsr1 are required to recruit Vangl2 and Fzd6 to sites of cell-cell contact...
  58. ncbi Trimeric G protein-dependent frizzled signaling in Drosophila
    Vladimir L Katanaev
    Department of Genetics and Development, Center for Neurobiology and Behavior, College of Physicians and Surgeons, Columbia University, 701 West 168 Street, New York, NY 10032, USA
    Cell 120:111-22. 2005
    ..Thus, Go is likely part of a trimeric G protein complex that directly transduces Fz signals from the membrane to downstream components...
  59. ncbi Asymmetric localization of frizzled and the establishment of cell polarity in the Drosophila wing
    D I Strutt
    Centre for Developmental Genetics, Department of Biomedical Science, University of Sheffield, Western Bank, S10 2TN, Sheffield, United Kingdom
    Mol Cell 7:367-75. 2001
    ..This differential receptor distribution may represent a novel mechanism for amplifying small differences in signaling activity across the axis of a cell...
  60. pmc Small-molecule modulators of Hedgehog signaling: identification and characterization of Smoothened agonists and antagonists
    Maria Frank-Kamenetsky
    Curis, Inc, 61 Moulton Street, Cambridge, MA 02138, USA
    J Biol 1:10. 2002
    ....
  61. pmc Cilia and Hedgehog responsiveness in the mouse
    Danwei Huangfu
    Developmental Biology Program, Sloan Kettering Institute, 1275 York Avenue, New York, NY 10021, USA
    Proc Natl Acad Sci U S A 102:11325-30. 2005
    ....
  62. ncbi Broad tuning of the human bitter taste receptor hTAS2R46 to various sesquiterpene lactones, clerodane and labdane diterpenoids, strychnine, and denatonium
    Anne Brockhoff
    Department of Molecular Genetics, German Institute of Human Nutrition Potsdam Rehbruecke, Arthur Scheunert Allee 114 116, 14558 Nuthetal, Germany
    J Agric Food Chem 55:6236-43. 2007
    ....
  63. ncbi AXOR12, a novel human G protein-coupled receptor, activated by the peptide KiSS-1
    A I Muir
    Department of Discovery Biology, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex CM19 5AW, United Kingdom
    J Biol Chem 276:28969-75. 2001
    ..The biological significance of these expression patterns and the nature of the putative cognate ligand for AXOR12 are discussed...
  64. ncbi Kisspeptin-54 stimulates the hypothalamic-pituitary gonadal axis in human males
    Waljit S Dhillo
    Department of Metabolic Medicine, Faculty of Medicine, Imperial College London, London W12 ONN, United Kingdom
    J Clin Endocrinol Metab 90:6609-15. 2005
    ..The endogenous neuropeptide agonist for G protein-coupled receptor 54, kisspeptin, potently stimulates the hypothalamic-pituitary-gonadal axis in rodents and primates...
  65. ncbi Desensitization of G protein-coupled receptors and neuronal functions
    Raul R Gainetdinov
    Howard Hughes Medical Institute Laboratories, Department of Cell Biology, Duke University Medical Center, Durham, North Carolina 27710, USA
    Annu Rev Neurosci 27:107-44. 2004
    ..Furthermore, the utility of a pharmacological strategy aimed at targeting this GPCR desensitization machinery to regulate brain functions can be envisaged...
  66. ncbi The G protein-coupled receptor GPR30 mediates c-fos up-regulation by 17beta-estradiol and phytoestrogens in breast cancer cells
    Marcello Maggiolini
    Department of Pharmaco Biology, University of Calabria, 87030 Rende CS, Italy
    J Biol Chem 279:27008-16. 2004
    ..The ability of E2 and phytoestrogens to regulate the expression of growth-related genes such as c-fos even in the absence of ER has interesting implications for understanding breast cancer progression...
  67. ncbi Hedgehog regulates smoothened activity by inducing a conformational switch
    Yun Zhao
    Department of Developmental Biology, University of Texas Southwestern Medical Center, Dallas, Texas 75390, USA
    Nature 450:252-8. 2007
    ..Hence, by employing multiple Arg clusters as inhibitory elements counteracted by differential phosphorylation, SMO acts as a rheostat to translate graded HH signals into distinct responses...
  68. pmc The decoupling of Smoothened from Galphai proteins has little effect on Gli3 protein processing and Hedgehog-regulated chick neural tube patterning
    Wee Chuang Low
    Department of Genetic Medicine, Weill Medical College of Cornell University, 1300 York Avenue, W404, New York, NY 10021, USA
    Dev Biol 321:188-96. 2008
    ..Thus, our results indicate that the Smo-induced Galpha(i) activity plays an insignificant role in the regulation of Gli3 processing and Shh-regulated neural tube patterning...
  69. ncbi The Drosophila smoothened gene encodes a seven-pass membrane protein, a putative receptor for the hedgehog signal
    J Alcedo
    Institut fur Molekularbiologie II der Universitat Zurich, Switzerland
    Cell 86:221-32. 1996
    ..Based on its predicted physical characteristics and on its position in the Hh signaling pathway, we suggest that smo encodes a receptor for the Hh signal...
  70. pmc Trace amine-associated receptors and their ligands
    R Zucchi
    Dipartimento di Scienze dell Uomo e dell Ambiente, University of Pisa, Pisa, Italy
    Br J Pharmacol 149:967-78. 2006
    ....
  71. ncbi Historical review: a brief history and personal retrospective of seven-transmembrane receptors
    Robert J Lefkowitz
    Howard Hughes Medical Institute, James B Duke Professor of Medicine, Duke University Medical Center, Room 468, CARL Bldg, Research Drive, DUMC Box 3821, Durham, NC 27710, USA
    Trends Pharmacol Sci 25:413-22. 2004
    ..Numerous opportunities for novel therapeutics should emerge from current and future research on 7TM receptor biology...
  72. pmc The structure and function of G-protein-coupled receptors
    Daniel M Rosenbaum
    Department of Molecular and Cellular Physiology, Stanford University School of Medicine, 279 Campus Drive, Palo Alto, California 94305, USA
    Nature 459:356-63. 2009
    ..Recent high-resolution structural studies have provided insights into the molecular mechanisms of GPCR activation and constitutive activity...
  73. ncbi Heterotrimeric G protein activation by G-protein-coupled receptors
    William M Oldham
    Department of Pharmacology, Vanderbilt University School of Medicine, 442 Robinson Research Building, 2222 Pierce Avenue, Nashville, TN 37232 6600, USA
    Nat Rev Mol Cell Biol 9:60-71. 2008
    ....
  74. pmc The planar polarity pathway promotes coordinated cell migration during Drosophila oogenesis
    Rebecca Bastock
    Centre for Developmental and Biomedical Genetics, Department of Biomedical Science, University of Sheffield, Western Bank, Sheffield S10 2TN, UK
    Development 134:3055-64. 2007
    ..We conclude that, during collective cell migration, the planar polarity pathway can mediate communication between motile and non-motile cells, which enhances the efficiency of migration via the modulation of actin dynamics...
  75. pmc Advanced vaginal opening and precocious activation of the reproductive axis by KiSS-1 peptide, the endogenous ligand of GPR54
    V M Navarro
    Department of Cell Biology, Physiology and Immunology, University of Cordoba, 14004 Cordoba, Spain
    J Physiol 561:379-86. 2004
    ....
  76. ncbi Distinct narcolepsy syndromes in Orexin receptor-2 and Orexin null mice: molecular genetic dissection of Non-REM and REM sleep regulatory processes
    Jon T Willie
    Department of Molecular Genetics, University of Texas Southwestern Medical Center at Dallas, Dallas, TX 75390, USA
    Neuron 38:715-30. 2003
    ....
  77. pmc Reverse physiology in drosophila: identification of a novel allatostatin-like neuropeptide and its cognate receptor structurally related to the mammalian somatostatin/galanin/opioid receptor family
    N Birgul
    Institut fur Zellbiochemie und klinische Neurobiologie, Universitat Hamburg, Martinistrasse 52, 20246 Hamburg, Germany
    EMBO J 18:5892-900. 1999
    ....
  78. pmc Cloning and characterization of a cell surface receptor for xenotropic and polytropic murine leukemia viruses
    C S Tailor
    Department of Biochemistry and Molecular Biology, Oregon Health Sciences University, Portland, OR 97201 3098, USA
    Proc Natl Acad Sci U S A 96:927-32. 1999
    ..We propose that X-MLVs and P-MLVs comprise a single family of retroviruses that have coevolved in response to diversification in X-receptor genes of the host...
  79. pmc Altered localization of Drosophila Smoothened protein activates Hedgehog signal transduction
    Alan Jian Zhu
    Departments of Developmental Biology and Genetics, Howard Hughes Medical Institute, Beckman Center B300, Stanford University School of Medicine, Stanford, California 94305 5329, USA
    Genes Dev 17:1240-52. 2003
    ..Conversely, trapping of activated Smo mutants in the ER prevents Hh target gene activation. Control of Smo localization appears to be a crucial step in Hh signaling in Drosophila...
  80. pmc Ryk cooperates with Frizzled 7 to promote Wnt11-mediated endocytosis and is essential for Xenopus laevis convergent extension movements
    Gun Hwa Kim
    Department of Life Science, Division of Molecular and Life Sciences, Pohang University of Science and Technology, Hyoja Dong, Pohang, Kyungbuk 790 784, Republic of Korea
    J Cell Biol 182:1073-82. 2008
    ..Our study suggests that Ryk functions as an essential regulator for noncanonical Wnt/Fz-mediated endocytosis in the regulation of X. laevis CE movements...
  81. ncbi Identification of a gene (GPR30) with homology to the G-protein-coupled receptor superfamily associated with estrogen receptor expression in breast cancer
    C Carmeci
    Department of Surgery, Stanford University, Stanford, California, 94305, USA
    Genomics 45:607-17. 1997
    ..The pattern of expression of GPCR-Br indicates that this receptor may be involved in physiologic responses specific to hormonally responsive tissues...
  82. ncbi Hedgehog induces opposite changes in turnover and subcellular localization of patched and smoothened
    N Denef
    European Molecular Biology Laboratory, Heidelberg, Germany
    Cell 102:521-31. 2000
    ..Comparable effects can be produced by removing Patched from cells by RNA-mediated interference. These findings raise the possibility that Patched acts indirectly to regulate Smoothened activity...
  83. ncbi Selective expression of the chemokine receptor XCR1 on cross-presenting dendritic cells determines cooperation with CD8+ T cells
    Brigitte G Dorner
    Molecular Immunology, Robert Koch Institute, 13353 Berlin, Germany
    Immunity 31:823-33. 2009
    ..Absence of XCL1 impaired the development of cytotoxicity to antigens cross-presented by CD8(+) DCs. The XCL1-XCR1 axis thus emerges as an integral component in the development of efficient cytotoxic immunity in vivo...
  84. ncbi Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14
    R S Ames
    Department of Molecular Biology, Smith Kline Beecham Pharmaceuticals, King of Prussia, Pennsylvania 19406 0939, USA
    Nature 401:282-6. 1999
    ..Furthermore, as U-II immunoreactivity is also found within central nervous system and endocrine tissues, it may have additional activities...
  85. ncbi The receptors and cells for mammalian taste
    Jayaram Chandrashekar
    Howard Hughes Medical Institute and Departments of Neurobiology and Neurosciences, University of California at San Diego, La Jolla, California 92093 0649, USA
    Nature 444:288-94. 2006
    ..Importantly, receptor cells for each taste quality function as dedicated sensors wired to elicit stereotypic responses...
  86. pmc Arousal effect of orexin A depends on activation of the histaminergic system
    Z L Huang
    Department of Molecular Behavioral Biology, Osaka Bioscience Institute, Japan
    Proc Natl Acad Sci U S A 98:9965-70. 2001
    ..These findings strongly indicate that the arousal effect of orexin A depends on the activation of histaminergic neurotransmission mediated by H1R...
  87. pmc GPR40 is necessary but not sufficient for fatty acid stimulation of insulin secretion in vivo
    Martin G Latour
    Centre de recherche du Centre Hospitalier de l Universite de Montreal, Technopole Angus, 2901 Rachel Est, Montreal, QC, H1W 4A4 Canada
    Diabetes 56:1087-94. 2007
    ..We conclude that GPR40 contributes approximately half of the full acute insulin secretory response to fatty acids in mice but does not play a role in the mechanisms by which fatty acids chronically impair insulin secretion...
  88. ncbi Receptors for polytropic and xenotropic mouse leukaemia viruses encoded by a single gene at Rmc1
    Y L Yang
    Department of Medicine, Brigham and Women s Hospital and Harvard Medical School, Boston, Massachusetts 02115, USA
    Nat Genet 21:216-9. 1999
    ..We also obtained the cDNA encoding human SYG1. When expressed in hamster cells, it establishes infectivity by MCF MLV as well as xenotropic MLV, which do not infect laboratory mice...
  89. pmc Prokineticin 1 signaling and gene regulation in early human pregnancy
    Jemma Evans
    Medical Research Council Human Reproductive Sciences Unit, The Queen s Medical Research Institute, Edinburgh EH16 4TJ, United Kingdom
    Endocrinology 149:2877-87. 2008
    ..These data demonstrate that PROK1 and PROKR1 expression is elevated in human decidua during early pregnancy and that PROK1-PROKR1 interaction regulates expression of a host of implantation-related genes...
  90. ncbi Mutation of Celsr1 disrupts planar polarity of inner ear hair cells and causes severe neural tube defects in the mouse
    John A Curtin
    GlaxoSmithKline Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, CM19 5AW, United Kingdom
    Curr Biol 13:1129-33. 2003
    ....
  91. ncbi Oleic acid interacts with GPR40 to induce Ca2+ signaling in rat islet beta-cells: mediation by PLC and L-type Ca2+ channel and link to insulin release
    Ken Fujiwara
    Dept of Physiology, Div of Integrative Physiology, Jichi Medical School, Minamikawachi, Tochigi 329 0498, Japan
    Am J Physiol Endocrinol Metab 289:E670-7. 2005
    ..These results demonstrate that OA interacts with GPR40 to increase [Ca(2+)](i) via PLC- and L-type Ca(2+) channel-mediated pathway in rat islet beta-cells, which may be link to insulin release...
  92. ncbi Molecular properties of apelin: tissue distribution and receptor binding
    Y Kawamata
    Discovery Research Laboratories 1, Pharmaceutical Discovery Research Division, Takeda Chemical Industries, Ltd, Wadai 10, Tsukuba, 300 4293, Ibaraki, Japan
    Biochim Biophys Acta 1538:162-71. 2001
    ..Our results demonstrate that the long and short forms of apelin differently interact with APJ...
  93. ncbi Adaptive diversification of bitter taste receptor genes in Mammalian evolution
    Peng Shi
    Laboratory of Molecular Evolution and Genome Diversity, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, China
    Mol Biol Evol 20:805-14. 2003
    ....
  94. ncbi Direct binding of the PDZ domain of Dishevelled to a conserved internal sequence in the C-terminal region of Frizzled
    Hing C Wong
    Department of Structural Biology, St Jude Children s Research Hospital, Memphis, TN 38105, USA
    Mol Cell 12:1251-60. 2003
    ..Together, our results identify a missing molecular connection within the Wnt pathway. Differences in the binding affinity of the Dvl PDZ domain and its binding partners may be important in regulating signal transduction by Dvl...
  95. pmc Hypogonadotropic hypogonadism due to loss of function of the KiSS1-derived peptide receptor GPR54
    Nicolas de Roux
    Institut National de la Santé et de la Recherche Médicale Unité 135, Unité de Recherches Hormones Gènes et Reproduction, Hopital de Bicetre, 94275 Le Kremlin Bicetre, France
    Proc Natl Acad Sci U S A 100:10972-6. 2003
    ..The present study shows that loss of function of GPR54 is a cause of IHH, and it identifies GPR54 and possibly KiSS1 protein-derived peptide as playing a major and previously unsuspected role in the physiology of the gonadotropic axis...
  96. ncbi G protein-coupled receptors stimulation and the control of cell migration
    Mathieu Cotton
    Department of Pharmacology, University of Montreal, Montreal, QC, Canada
    Cell Signal 21:1045-53. 2009
    ..In this review, we will discuss the role of GPCR mediated signal transduction and review their importance in the regulation of actin remodeling leading to cell migration...
  97. pmc The PCP genes Celsr1 and Vangl2 are required for normal lung branching morphogenesis
    Laura L Yates
    Medical Research Council, Harwell, Oxfordshire OX11 0RD, UK
    Hum Mol Genet 19:2251-67. 2010
    ....
  98. ncbi Taste receptors in the gastrointestinal tract. I. Bitter taste receptors and alpha-gustducin in the mammalian gut
    Enrique Rozengurt
    Division of Digestive Diseases and CURE Digestive Diseases Research Center, David Geffen School of Medicine, University of California at Los Angeles, Los Angeles, CA 90095 1786, USA
    Am J Physiol Gastrointest Liver Physiol 291:G171-7. 2006
    ....
  99. ncbi Patched1 regulates hedgehog signaling at the primary cilium
    Rajat Rohatgi
    Departments of Developmental Biology, Genetics, and Bioengineering and Howard Hughes Medical Institute, Stanford University School of Medicine, Stanford, CA 94305, USA
    Science 317:372-6. 2007
    ..When Shh bound to Ptc1, Ptc1 left the cilia, leading to accumulation of Smo and activation of signaling. Thus, primary cilia sense Shh and transduce signals that play critical roles in development, carcinogenesis, and stem cell function...
  100. ncbi The orexin OX1 receptor regulates Ca2+ entry via diacylglycerol-activated channels in differentiated neuroblastoma cells
    Johnny Näsman
    A I Virtanen Institute for Molecular Sciences, Department of Neurobiology, University of Kuopio, FIN 70211 Kuopio, Finland
    J Neurosci 26:10658-66. 2006
    ..The results suggest that the OX1R activates a Ca2+ entry pathway that involves diacylglycerol-activated TRPC channels in neuronal cells...
  101. ncbi An amino-acid taste receptor
    Greg Nelson
    Howard Hughes Medical Institute and Departments of Biology and Neurosciences, University of California at San Diego, La Jolla, California, 92093 0649, USA
    Nature 416:199-202. 2002
    ..We also show that sequence differences in T1R receptors within and between species (human and mouse) can significantly influence the selectivity and specificity of taste responses...

Research Grants74

  1. H1R Signaling and Immune Deviation in EAE
    Cory Teuscher; Fiscal Year: 2013
    ....
  2. FASEB SRC on Lysophospholipd Mediators in Health and Disease
    Julie D Saba; Fiscal Year: 2011
    ....
  3. Sex Steroid Hormone Regulation of Drug Reinforcement
    Diane Lebesgue; Fiscal Year: 2012
    ..fellow and instructor, I have studied the molecular biology and signal transduction mechanisms of G protein coupled receptors (GPCRs)...
  4. Canonical Transient Receptor Potential (TRPC) subfamily function in Hippocampus.
    David E Clapham; Fiscal Year: 2013
    ....
  5. Diverse Roles for RIC8 During G Protein Signaling in Fungi
    Katherine A Borkovich; Fiscal Year: 2012
    ..b>G protein coupled receptors (GPCRs) have been characterized as guanine nucleotide exchange factors (GEFs) for Ga subunits...
  6. Histamine modulation of biliary proliferation and damage
    Heather L Francis; Fiscal Year: 2013
    ..synthesis may be important in the inhibition of biliary hyperplasia, overexpression of HDC (leading to enhanced histamine release) may be key for stimulating biliary proliferation in ductopenic conditions associated with biliary damage ..
  7. Neuropeptide regulation of neurohypophyseal function
    Francis W Flynn; Fiscal Year: 2012
    ..The nuclear translocation of the neurokinin receptor to the nucleus is novel and has implications for a large number of pathologies, such as epilepsy, that are linked to this receptor system in the brain. ..
  8. Genetic Study of PP-Fold Polypeptide-Receptor Axis on Metabolic Syndrome Risk
    PEI AN SHIH; Fiscal Year: 2013
    ....
  9. Role of endothelin receptors in glaucomatous optic neuropathy
    Raghu R Krishnamoorthy; Fiscal Year: 2013
    ..The information gained from this study could be useful in developing endothelin receptor antagonists as neuroprotective agents in glaucoma treatment. ..
  10. Sphingosine 1-phosphate and cardioprotection
    JOEL SAMUEL KARLINER; Fiscal Year: 2012
    ....
  11. Role of G-gamma-7 in striatal cannabinoid and D2 dopamine
    Dana E Selley; Fiscal Year: 2010
    ..These studies will provide information that contributes to our understanding of the neural mechanisms of drug addiction and possibly neuropsychiatric and movement disorders, such as schizophrenia and Parkinsonism. ..
  12. Regulation of alpha2A-adrenergic receptor signaling and trafficking by spinophili
    Qin Wang; Fiscal Year: 2013
    ....
  13. Discovery of Selective MT1 Melatonin Receptor Ligands for Sleep Disorders
    Margarita L Dubocovich; Fiscal Year: 2010
    ....
  14. Disruption of Autonomic Pathways in Left Atrium by Inhibition of G Proteins
    Alan H Kadish; Fiscal Year: 2010
    ..In the heart, G protein coupled receptors (GPCRs) and their cognate signaling partners, the heterotrimeric G-proteins, regulate most mechanical ..
  15. SIGNALING THROUGH RHO GTP/GDP EXCHANGE FACTORS
    Philip B Wedegaertner; Fiscal Year: 2013
    ..The research in this application will provide new knowledge about the functions of RhoGEFs and thus better define how the RhoGEFs can be therapeutically inhibited in disease without affecting their critical normal functions. ..
  16. Pharmacology of Risperidone Effects on Bone Remodeling and Energy Metabolism
    Karen L Houseknecht; Fiscal Year: 2013
    ..The pharmacology of SGAs is complex: they potently antagonize multiple G protein coupled receptors (GPCRs) including dopamine, serotonin, alpha- adrenergic and histamine receptors...
  17. Harness Germinal Matrix Hemorrhage
    John H Zhang; Fiscal Year: 2013
    ..The long-term goals of this proposal are to provide non-invasive therapeutic approaches for GMH patients. ..
  18. Ligand Interaction of Glucagon Receptor by Structural and Functional Analyses
    FAI YIU SIU; Fiscal Year: 2012
    ....
  19. Modulation of insulin and glucagon secretion by GPCR ligands
    TARA ASHLEY SCHWETZ; Fiscal Year: 2011
    ....
  20. Molecular Components Affecting Ocular Retinoid Homeostasis
    JOHANNES FRIEDERICH VONLINTIG; Fiscal Year: 2012
    ..abstract_text> ..
  21. MECHANISMS OF MALADAPTATION IN HEART FAILURE
    Howard A Rockman; Fiscal Year: 2013
    ..Furthermore, the proposed studies will lead to new targets to treat cardiac hypertrophy and heart failure in humans. ..
  22. Role of Gsalpha in Regulating Osteoblast Differentiation
    JOY Y WU; Fiscal Year: 2012
    ..Finally, Aim 3 will focus on determining the ability of osteoprogenitors to differentiate towards other mesenchymal lineages such as adipocytes, using lineage tracing in vivo and cell differentiation assays in vitro. ..
  23. Roles of Gs Alpha and interaction with Wnt signaling in regulation of adipocyte d
    Partha S Sinha; Fiscal Year: 2011
    ..PUBLIC HEALTH RELEVANCE: This study focuses on mechanisms underlying how fat cells and bone cells develop from the bone marrow. This may help improve understanding and treatment of diseases such as obesity and osteoporosis. ..
  24. MOLECULAR PROPERTIES OF IONIC PERMEABILITY IN NERVE
    Bertil Hille; Fiscal Year: 2013
    ..This project will study the kinetics of membrane phosphoinositide metabolism and signaling by G protein coupled receptors to modulate ion channels...
  25. Mechanisms of glucagon-like peptide 1 (GLP-1) in fatty liver disease
    Frank A Anania; Fiscal Year: 2013
    ..Additional data indicate that exendin-4 suppresses CHOP expression both in vitro and in mice fed a high-fat diet, but in CHOP knockout mice fed an identical diet, fat-laden hepatocytes are protected from apoptotic death. ..
  26. The bioorganic chemistry of RNA editing by ADARs
    Peter A Beal; Fiscal Year: 2013
    ..Finally, this project will produce new molecules for crystallization trials of ADAR-RNA complexes. ..
  27. CIRCUITS MEDIATING BEHAVIORAL CONSEQUENCES OF STEROID SENSATION
    Timothy E Holy; Fiscal Year: 2013
    ..Olfactory detection may represent a major, previously-unrecognized mechanism for steroid action in mice;understanding this phenomenon will provide critical new insights for interpreting studies that alter the steroid milieu. ..
  28. Disruption of Autonomic Pathways in the Left Atrium by Inhibition of G-proteins
    Rishi Arora; Fiscal Year: 2013
    ..In the heart, G protein coupled receptors (GPCRs) and their cognate signaling partners, the heterotrimeric G-proteins, regulate most mechanical ..
  29. Genetic Mapping Of Novel Molecular Players in Itch
    RACHEL BETH BREM; Fiscal Year: 2013
    ..Identification of candidate itch factors will provide new targets for development of drugs and therapies to treat intractable itch. ! ..
  30. Calcium-sensing receptor signaling in the regulation of colonic epithelial cells
    JUAN ENRIQUE ROZENGURT; Fiscal Year: 2012
    ..The completion of the proposed studies will provide a robust intellectual framework for targeting the colonic CaSR in the chemoprevention of CRC in US veterans as well as in the US population at large. ..
  31. Role of Neuropeptide Y in Obesity-Receptor Specific Analogs
    Ambikaipakan Balasubramaniam; Fiscal Year: 2013
    ..This could enhance recall opportunities and reduce the burden on the Veterans Health Care cost. ..
  32. Development of PAR2 Inhibitors for the Treatment of Nonalcoholic steatohepatitis
    Athan Kuliopulos; Fiscal Year: 2013
    ....
  33. Molecular Analysis of Juvenile Hormone Action
    Subba R Palli; Fiscal Year: 2013
    ....
  34. Mechanism and functional role of AKAP79/150 in M current control
    Mark S Shapiro; Fiscal Year: 2012
    ....
  35. REGULATION OF CELLULAR RESPONSES TO NEUROPEPTIDES
    Nigel W Bunnett; Fiscal Year: 2010
    ..For type specifications, see Specific Instructions onpage 10.) RESEARCH GRANT TABLE OF CONTENTS PAGE NUMBERS Face page 1 Description, ..
  36. Novel STIM1-dependent cyclic AMP signaling pathway in colonic epithelial function
    Aldebaran M Hofer; Fiscal Year: 2013
    ....
  37. Endocannabinoid Discrimination
    Jenny L Wiley; Fiscal Year: 2013
    ....
  38. ROLE AND REGULATION OF PROTEIN KINASE C ISOENZYMES
    Yusuf Awni Hannun; Fiscal Year: 2013
    ..We are defining the significance and mechanisms by which this process occurs and is regulated. In particular we focus on a key signaling protein known as protein kinase C (PKC) and its activating lipids. ..
  39. Physiological Regulation of MLCK in Intact Arteries
    Withrow Gil Wier; Fiscal Year: 2013
    ..This research will utilize a mouse model of salt-induced hypertension to provide specific new information on the role of MLCK in high blood pressure. ..
  40. RhoA mediated survival signals in cardiomyocytes
    Joan Heller Brown; Fiscal Year: 2013
    DESCRIPTION (provided by applicant): Many known and unknown ligands for G protein coupled receptors, released in the heart in response to stress, converge on RhoA activation, making it a nodal point in determining cardiomyocyte ..
  41. Central TRPV1 in Cardiovascular Regulation
    MICHAEL CHRISTIAN ANDRESEN; Fiscal Year: 2013
    ....
  42. Rho- and GPCR-mediated signaling through novel cellular effectors
    Joan Heller Brown; Fiscal Year: 2012
    ....
  43. Propofol and Protein Kinase C: Molecular Interactions in Cardiomyocytes
    DEREK SCOTT DAMRON; Fiscal Year: 2011
    ..We believe these studies represent a logical extension of our previous work in cardiomyocytes and provide an innovative approach to better understand the cellular and molecular mechanisms of anesthetic action in the heart. ..
  44. The Role of Intracellular Metabotropic Glutamate Receptor 5 at the Synapse
    CAROLYN ANN PURGERT; Fiscal Year: 2012
    ..For Fragile X Syndrome and possibly autism, understanding the role of intracellular mGluR5 will be crucial in developing suitable mGluR5 antagonists for therapeutic treatments. ..
  45. The S1P1 receptor regulates sarcomere assembly and cardiac development
    Roland S Wu; Fiscal Year: 2013
    ..The effects of this disruption will then be assayed by echocardiography, immunohistochemistry, and electron microscopy. ..
  46. MEMBRANE BASIS OF VISUAL EXCITATION
    Michael F Brown; Fiscal Year: 2012
    ..Understanding the protein and lipid components of visual membranes is vitally significant to the prevention of human diseases. ..
  47. Endogenous G-Protein Coupled Receptor Antagonists
    Carrie Haskell-Luevano; Fiscal Year: 2012
    ..This research project proposes to generate knowledge for the rational design of molecules as potential therapeutic agents to prevent or treat the diseases associated with over or under eating. ..
  48. Control of Nociception in the Spinal Cord
    Sukhbir S Mokha; Fiscal Year: 2013
    ..Our postulate that estrogen-induced negative regulation of the function of many G protein coupled receptors (GPCRs) such as the opioid receptor like1 (ORL1) and 12-adrenoceptors makes women more susceptible to ..
  49. Lysophosphatidic Acid in Oncogenesis
    Xianjun Fang; Fiscal Year: 2010
    ..These proposed studies together will establish the role of LPA4 in tumor suppression and may lead to identification of novel anticancer targets. ..
  50. Sweet taste receptors and glucose metabolism in healthy and T2DM humans
    Karen L Teff; Fiscal Year: 2012
    ..Our overall hypothesis is that in healthy subjects, the STR receptor is involved in the regulation of post-prandial glucose metabolism and GLP levels but in T2DM, the STR receptor is unresponsive to activation or inhibition ..
  51. Personalized therapeutics for inhibiting breast cancer metastasis
    DEBRA AUGUSTE; Fiscal Year: 2012
    ....
  52. Exploring the Role of the Prokineticin System in Human Reproduction
    ANA PAULA DE ABREU E SILVA METZGER; Fiscal Year: 2013
    ....
  53. Synthetic Fabs for Crystallization of Chemokine:Receptor Complexes
    Tracy M Handel; Fiscal Year: 2013
    ....
  54. BIOLOGY OF NEUROENDOCRINE PEPTIDES
    Marc R Montminy; Fiscal Year: 2013
    ..Specifying the contributions of the CRF family of ligands and receptors to the maintenance of homeostasis and to stress-linked allostasis may improve our ability to manage diseases, including mood and metabolic disorders ..
  55. Nanopore Biosensor for Kinetics of Reparative Antibodies on Plasma Membranes
    Sang Hyun Oh; Fiscal Year: 2013
    ..The problem is compounded for transmembrane proteins such as G protein coupled receptors (GPCR) because proteins in direct contact with a solid substrate, in particular with the gold substrate ..
  56. Control of Oocyte Maturation in C. elegans
    DAVID IRWIN GREENSTEIN; Fiscal Year: 2013
    ..The small roundworm C. elegans is an established model for studying the hormonal control of meiosis. These studies will define the signaling mechanisms controlling female meiosis and provide insights into the origin of meiotic errors. ..
  57. Novel Ca receptor signaling pathways for control of renal ion transport
    Richard Tyler Miller; Fiscal Year: 2012
    ..This information will result in recognition of a new way to control the amount of salt in the body and hopefully new ways to treat high and low blood pressure. ..
  58. Neuronal-Astrocytic Communication In Vivo
    KEN DOUGLAS MCCARTHY; Fiscal Year: 2013
    ..The goal of this proposal is to take a genetic approach to investigate the role of astrocytes in a wide array of physiological and behavioral processes. ..
  59. Olfactory Coding in Mammals
    Minghong Ma; Fiscal Year: 2013
    ..These studies will also help to design better therapeutic agents targeting other G protein-coupled receptors, which play pivotal roles in signal transduction in all body organs. ..
  60. The GABA-B receptor is a novel drug target for pancreatic cancer
    Hildegard M Schuller; Fiscal Year: 2012
    ..Since GABA and baclophen are already approved for the treatment of non-cancerous conditions in humans, results of this research can be rapidly translated into clinical trials. ..
  61. Quantitative Analysis of RET Receptor Activation and Signaling
    Adrian Whitty; Fiscal Year: 2013
    ..abstract_text> ..
  62. BK Virus Receptor and polyomavirus nephropathy
    Andrey Sorokin; Fiscal Year: 2012
    ..This proposal will uncover the protein component of BKV receptor and provide the basis for a novel strategy for therapeutical intervention in BKN to ultimately improve long-term graft survival after renal transplantation. ..
  63. HUMAN GASTRIN-RELEASING PEPTIDE RECEPTOR GENE REGULATION
    Horst Weber; Fiscal Year: 2004
    ..Due to its important relationship to mitogenic and other factors involved in carcinogenesis, these studies will greatly contribute to the general understanding of malignant transformation in gastrointestinal and other tissues. ..
  64. G PROTEINS AND SIGNAL TRANSDUCTION IN NEUROSPORA CRASSA
    KATHERINE BORKOVICH; Fiscal Year: 2006
    ..one G-gamma (GNG-1) 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...
  65. Molecular basis of congenital disorders of glycosylation: mechanisms of oligosach
    Smita Mohanty; Fiscal Year: 2010
    ..Thus understanding the molecular basis of function of this complex integral membrane protein is very critical for the treatment or for therapeutic intervention of the above diseases. ..
  66. Methods for the Development of Arrestin2 Inhibitors.
    Spiro Pavlopoulos; Fiscal Year: 2010
    ..This work will lead to the development of tools to better understand these processes and may contribute to the design of therapeutic agents that help to treat addiction and circumvent tolerance to therapeutic drugs. ..
  67. G Proteins and Endothelial Barrier Regulation
    Tatyana Voyno Yasenetskaya; Fiscal Year: 2004
    ..abstract_text> ..
  68. Neurokinin 3 Receptor: Nuclear Localization in Supraoptic Neurons
    CELIA SLADEK; Fiscal Year: 2009
    ....
  69. Bivalent ligands as molecular probes for CB1/OX1 receptor heterodimers
    Yanan Zhang; Fiscal Year: 2010
    ..Our efforts in development of bivalent ligands as molecular probes for cannabinoid/orexin heterodimers will further our understanding of receptor heterodimerization and may ultimately lead to novel heterodimer based pharmacotherapies. ..
  70. MODULATION OF SODIUM CHANNELS BY G PROTEINS
    Todd Scheuer; Fiscal Year: 2001
    ..An understanding of how they are modulated physiologically will provide the basis for developing pharmacologic means of controlling them to achieve specific therapeutic goals. ..
  71. REGULATORY DOMAINS OF G PROTEIN COUPLED RECEPTORS
    Ellen Weiss; Fiscal Year: 2002
    ....
  72. Hydrogen Deuterium Exchange Mapping of Chemokine Receptor Complex Interfaces
    Tracy Handel; Fiscal Year: 2009
    ..Developing methods like DXMS to understand the molecular details of chemokine:receptor interactions and function, may facilitate the design of small molecule and protein therapeutics for many diseases. ..
  73. INTERACTIONS AND ACTIVATION OF THE FSH RECEPTOR
    TAE JI; Fiscal Year: 2003
    ..in the understanding for the mechanism of multiple signal generation by not only FSHR but also other G protein coupled receptors. We propose to extend our observations (1) to determine the roles of individual amino acids in exoloops ..
  74. G Protein-Coupled Receptors with Leucine-Rich Repeats
    Aaron Hsueh; Fiscal Year: 2002
    ..Eventual purification of the ligand(s) for LGR4 could provide understanding of its physiological roles in ovary and other tissues. ..