Figure 2 Binding properties of P2Y12-receptor inhibitors

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Figure 2 Binding properties of P2Y12-receptor inhibitors Figure 2 | Binding properties of P2Y12-receptor inhibitors.23 a | ADP binds to the P2Y12 receptor, which b | leads to a conformational change of the receptor and to G-protein activation. c | Competitive binding of the active metabolite of thienopyridines to the P2Y12 receptor. Binding is irreversible, which renders the receptor nonfunctional for the life of the platelet. d | Ticagrelor binds reversibly to the P2Y12 receptor at a site that is distinct from the ADP-binding site (noncompetitive binding). Ticagrelor inhibits ADP signalling and conformational change of the receptor by 'locking' the receptor in an inactive state; the receptor is functional after dissociation of the ticagrelor molecule. ADP can still bind at its binding site, and the degree of receptor inhibition is dependent on the concentration of ticagrelor. Modified with permission from Husted, S. & van Giezen, J. J. Ticagrelor: the first reversibly binding oral P2Y12 receptor antagonist. Cardiovasc. Ther. 27 (4), 259–274 (2009), with permission from Wiley. Modified with permission from Husted, S. & van Giezen, J. J. Ticagrelor: the first reversibly binding oral P2Y12 receptor antagonist. Cardiovasc. Ther. 27 (4), 259–274 (2009), with permission from Wiley Rollini, F. et al. (2015) Switching P2Y12-receptor inhibitors in patients with coronary artery disease Nat. Rev. Cardiol. doi:10.1038/nrcardio.2015.113