Results 211 to 220 of about 507,235 (262)
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Dimerization of G-Protein-Coupled Receptors
Journal of Medicinal Chemistry, 2001The evolutionary trace (ET) method, a data mining approach for determining significant levels of amino acid conservation, has been applied to over 700 aligned G-protein-coupled receptor (GPCR) sequences. The method predicted the occurrence of functionally important clusters of residues on the external faces of helices 5 and 6 for each family or ...
Christopher Higgs +8 more
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G‐protein‐coupled receptors: an update
Acta Physiologica, 2007Abstract The receptors that couple to G proteins (GPCR) and which span the cell membranes seven times (7‐TM receptors) were the focus of a symposium in Stockholm 2006. The ensemble of GPCR has now been mapped in several animal species. They remain a major focus of interest in drug development, and their diverse physiological and pathophysiological ...
T. Hökfelt +2 more
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Science's STKE, 2005
This Teaching Resource provides lecture notes and slides for a class covering G protein–coupled receptors (GPCRs) and is part of the course "Cell Signaling Systems: A Course for Graduate Students." The lecture begins with a discussion of the major classes of GPCRs and then proceeds to describe the mechanisms of receptor diversity, ligand interaction ...
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This Teaching Resource provides lecture notes and slides for a class covering G protein–coupled receptors (GPCRs) and is part of the course "Cell Signaling Systems: A Course for Graduate Students." The lecture begins with a discussion of the major classes of GPCRs and then proceeds to describe the mechanisms of receptor diversity, ligand interaction ...
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G-Protein-Coupled Receptor Microarrays
ChemBioChem, 2002Membrane-bound proteins represent the single most important class of drug targets. Arraying these proteins is difficult because they typically need to be embedded in membranes to maintain their correctly folded conformations. We describe here the fabrication of microarrays consisting of G-protein-coupled receptors (GPCRs)--the single largest family of ...
Anthony G. Frutos +2 more
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Efficacy at g-protein-coupled receptors [PDF]
Nature Reviews Drug Discovery, 2002 At present, the drug-discovery process centres on ligands that either block or produce physiological responses. However, there are therapeutic uses for ligands that do neither of these things, but which still affect receptors in other ways. This review discusses the intimate relationship between the affinity of a ligand for its receptor, and the ...
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G-protein coupled receptors in bone
Frontiers in Bioscience, 1998The skeleton is a dynamic structure that undergoes continuous remodeling, a prerequisite to meeting the constant loading demands placed upon it. This process is controlled by a multitude of systemic and local factors which interact with receptors presented on the surface of both osteoblasts and osteoclasts; the osteogenic and osteolytic cells of bone ...
W.B. Bowler +2 more
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Deorphanization of G-Protein-Coupled Receptors
2007G-protein-coupled receptors constitute one of the major families of drug targets. Orphan receptors, for which the ligands and function are still unknown, are an attractive set of future targets for presently unmet medical needs. Screening strategies have been developed over the years in order to identify the natural ligands of these receptors.
Parmentier, Marc, Detheux, Michel
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Activation of G Protein–Coupled Receptors
2007G protein-coupled receptors (GPCRs) mediate responses to hormones and neurotransmitters, as well as the senses of sight, smell, and taste. These remarkably versatile signaling molecules respond to structurally diverse ligands. Many GPCRs couple to multiple G protein subtypes, and several have been shown to activate G protein-independent signaling ...
Brian K. Kobilka, Xavier Deupi
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2019
NOVEL LIGANDS: LIGAND SCREENING SYSTEMS AND ORPHAN RECEPTORS Measurement of Competitive and Allosteric Interactions in Radioligand Binding Studies-S. Lazareno and N.Birdsall Ligand Screening of G Protein-Coupled Receptors in Yeast-J. Hadcock and M. Pausch Ligand Screening Using Melanophore Cells: Frog Skin to Combinatorial Chemistry-J.
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NOVEL LIGANDS: LIGAND SCREENING SYSTEMS AND ORPHAN RECEPTORS Measurement of Competitive and Allosteric Interactions in Radioligand Binding Studies-S. Lazareno and N.Birdsall Ligand Screening of G Protein-Coupled Receptors in Yeast-J. Hadcock and M. Pausch Ligand Screening Using Melanophore Cells: Frog Skin to Combinatorial Chemistry-J.
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G protein—coupled receptor kinases
Cell, 1993G protein‐coupled receptor kinases (GRKs) constitute a family of six mammalian serine/threonine protein kinases that phosphorylate agonist-bound, or activated, G protein‐coupled receptors (GPCRs) as their primary substrates. GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling, or desensitization.
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