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Sunday, July 13, 2008

Evidence for a free thiol necessary for GPCR activation

P2Y12, a G protein-coupled receptor that plays a central role in platelet activation is the receptor targeted by the antithrombotic drug, clopidogrel. The mechanism of action of clopidogrel involved cysteine 97 within the first extracellular loop of P2Y12. This provides supporting evidence for a free thiol or sulfhydryl group necessary for GPCR activation.

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