Results 301 to 310 of about 793,543 (339)
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This is not a G protein-coupled receptor
Trends in Pharmacological Sciences, 1993On his canvas entitled 'La trahison des Images' ('The Perfidy of Images'), René Magritte painted a tobacco pipe in a very realistic manner and added the words: 'Ceci n'est pas une pipe' ('This is not a pipe'). In similar style, it is of prime importance to state that the first three-dimensional (3D) models of G protein-coupled receptors (GPCRs) that ...
M F, Hibert +3 more
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Current Biology, 1992
The diversity of the G protein-coupled receptor superfamily is now being realised with the molecular cloning of DNA encoding many new receptors and receptor subfamilies. The existing pharmacological definitions of receptor subtypes have been extended dramatically with identification of additional subtypes at the molecular level.
T P, Iismaa, J, Shine
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The diversity of the G protein-coupled receptor superfamily is now being realised with the molecular cloning of DNA encoding many new receptors and receptor subfamilies. The existing pharmacological definitions of receptor subtypes have been extended dramatically with identification of additional subtypes at the molecular level.
T P, Iismaa, J, Shine
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2008
G-Protein-coupled receptors mediate many of the hypnotic and analgesic actions of the drugs employed in anesthesia. Notably, opioid agonists represent the most successful and efficacious class of analgesic agents employed over the last century. Also, major clinical advances have been made by the study of alpha(2) adrenoceptor agonists, which possess ...
R D, Sanders, D, Brian, M, Maze
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G-Protein-coupled receptors mediate many of the hypnotic and analgesic actions of the drugs employed in anesthesia. Notably, opioid agonists represent the most successful and efficacious class of analgesic agents employed over the last century. Also, major clinical advances have been made by the study of alpha(2) adrenoceptor agonists, which possess ...
R D, Sanders, D, Brian, M, Maze
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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 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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Palmitoylation and G-protein coupled receptors
2022More and more it is being appreciated that not all GPCRs are the same, sub-populations of GPCRs exist within a cell and function differently than others. The question is, how does one regulate a given sub-population? One way is through the addition of post-translational modifications to G-protein coupled receptors (GPCR).
Georges, Chalhoub, Peter J, McCormick
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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 ...
B B, Fredholm, T, Hökfelt, G, Milligan
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G Protein-Coupled Receptor Pharmacogenetics
2008Common 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 ...
Miles D, Thompson +2 more
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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 ...
M K, Dean +8 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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