Article
Identification of determinants required for agonistic and inverse agonistic ligand properties at the ADP receptor P2Y12.
Molecular pharmacology - 1 Jan 2013
Schmidt Philipp, Ritscher Lars, Dong Elizabeth N, Hermsdorf Thomas, Cöster Maxi, Wittkopf Doreen, Meiler Jens, Schöneberg Torsten
Abstract excerpt
The ADP receptor P2Y(12) belongs to the superfamily of G protein-coupled receptors (GPCRs), and its activation triggers platelet aggregation. Therefore, potent antagonists, such as clopidogrel, are of high clinical relevance in prophylaxis and treatment of thromboembolic events. P2Y(12) displays an elevated basal activity in vitro, and as such, inverse agonists may be therapeutically beneficial compared with...
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