Article
Competitive mode and site of interaction of ticagrelor at the human platelet P2Y12 -receptor.
Journal of thrombosis and haemostasis : JTH - 1 Nov 2014
Hoffmann K, Lutz D A, Straßburger J, Baqi Y, Müller C E, von Kügelgen I
Abstract excerpt
BACKGROUND: The G-protein-coupled P2Y12 -receptor plays a crucial role in platelet aggregation. Recently, ticagrelor was licensed as the first perorally active and reversible P2Y12 -receptor antagonist. OBJECTIVE: The present study investigated the site and the antagonistic mode of action of ticagrelor at wild-type or mutant human P2Y12 -receptors. METHODS: Recombinant wild-type or mutant human P2Y12 -receptors...
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