Results 161 to 170 of about 500,528 (216)
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Structural diversity of G protein-coupled receptors and significance for drug discovery
Nature Reviews Drug Discovery, 2008Malin C Lagerström, Helgi B Schiöth
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Pharmacogenetics of the G Protein-Coupled Receptors
2014Pharmacogenetics investigates the influence of genetic variants on physiological phenotypes related to drug response and disease, while pharmacogenomics takes a genome-wide approach to advancing this knowledge. Both play an important role in identifying responders and nonresponders to medication, avoiding adverse drug reactions, and optimizing drug ...
M. D. Thompson +6 more
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G Protein-Coupled Receptor Pharmacogenetics [PDF]
, 2008 Common G protein-coupled receptor (GPCR) gene variants that encode receptor proteins with a distinct sequence may alter drug efficacy without always resulting in a disease phenotype. GPCR genetic loci harbor numerous variants, such as DNA insertions or deletions and single-nucleotide polymorphisms that alter GPCR expression and function, thereby ...
Katherine A. Siminovitch +2 more
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G protein-coupled receptors in rheumatology
Nature Reviews Rheumatology, 2014G protein-coupled receptors (GPCRs) are transmembrane receptor proteins that allow the transfer of signals across the cell membrane. In addition to their physiological role, GPCRs are involved in many pathophysiological processes including pathways relevant in rheumatoid arthritis (RA), osteoarthritis (OA) and psoriatic arthritis.
Elena Neumann +2 more
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2012
G protein coupled receptors play an important role due to physiological and pathophysiological processes and are responsible for signal transduction in the cell. Furthermore, about 30 % of drugs, present on market, address G protein coupled receptors. First, the families for classification of G protein coupled receptors are presented.
Andrea Strasser, Hans-Joachim Wittmann
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G protein coupled receptors play an important role due to physiological and pathophysiological processes and are responsible for signal transduction in the cell. Furthermore, about 30 % of drugs, present on market, address G protein coupled receptors. First, the families for classification of G protein coupled receptors are presented.
Andrea Strasser, Hans-Joachim Wittmann
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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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