Results 251 to 260 of about 728,478 (309)
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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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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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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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Efficacy at g-protein-coupled receptors
Nature Reviews Drug Discovery, 2002At 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 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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Crystal Structure of a Lipid G protein-Coupled Receptor
Science, 2012A Lipid-Sensing GPCR Sphingosine 1-phosphate (S1P) is a sphingolipid that binds to the G protein–coupled receptor subtype 1 (S1P1) to activate signaling pathways involved in regulation of the vascular and immune systems. Hanson et al. (p. 851) determined
M. Hanson +14 more
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G-protein-coupled receptors and cancer
Nature Reviews Cancer, 2007G-protein-coupled receptors (GPCRs), the largest family of cell-surface molecules involved in signal transmission, have recently emerged as crucial players in tumour growth and metastasis. Malignant cells often hijack the normal physiological functions of GPCRs to survive, proliferate autonomously, evade the immune system, increase their blood supply ...
Robert T, Dorsam, J Silvio, Gutkind
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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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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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