Clopidogrel: Interactions with the P2Y₁₂ Receptor and Clinical Relevance

References

• Daniel, J.L., Dangelmaier, C., Jin, J., Ashby, B., Smith, J.B. and Kunapuli, S.P. (1998) "Molecular basis for ADP-induced platelet activation I: evidence for three distinct ADP receptors on platelets", J. Biol. Chem. 273, 2024–2029.
   PubMed Web of Science ®Google Scholar
• Jantzen, H.-M., Gousset, L., Bhaskar, V, Vincent, D., Tai, A., Reynolds, E. and Conley, ED. (1999) "Evidence for two distinct G protein-coupled ADP receptors mediating platelet activation", Thromb. Haemost. 81, 111–117.
   PubMed Web of Science ®Google Scholar
• Jin, J. and Kunapuli, S.P. (1998) "Coactivation of two different G protein-coupled receptors is essential for ADP-induced platelet aggregation", Proc. Nat! Acad. Sci. USA 95,8070–8074.
   PubMed Web of Science ®Google Scholar
• Zhang, EL., Luo, L., Gustafson, E., Lachowicz, J., Smith, M., Qiao, X., Liu, Y.H., Chen, G., Pramanik, B., Laz, T.M., Palmer, K., Bayne, M. and Monsma, F. (2001) "ADP is the cognate ligand for the orphan G-protein coupled receptor 5P1999", J. Biol. Chem. 276, 8608–8615.
   PubMed Web of Science ®Google Scholar
• Takasaki, J., Kamohara, M., Saito, T., Matsumoto, M., Matsumoto, S., Ohishi, T., Soga, T., Matsushime, H. and Furuichi, K. (2001) "Molecular cloning of the platelet P2T(AC) ADP receptor: pharmacological comparison with another ADP receptor, the P2Y(1) receptor", Mol. Pharmacol. 60, 432–439.
   PubMed Web of Science ®Google Scholar
• Hollopeter, G., Jantzen, H.M., Vincent, D., Li, G., England, L., Ramakrishnan, V, Yang, R.B., Nurden, E, Nurden, A., Julius, D. and Conley, P.B. (2001) "Identification of the platelet ADP receptor targeted by antithrombotic drugs", Nature 409, 202–207.
   PubMed Web of Science ®Google Scholar
• Jin, J., Daniel, J.L. and Kunapuli, S.P. (1998) "Molecular basis for ADP-induced platelet activation. II. The P2Y1 receptor mediates ADP-induced intracellular calcium mobilization and shape change in platelets", J. Biol. Chem. 273, 2030–2034.
   PubMed Web of Science ®Google Scholar
• Kunapuli, S.P. (1998) "Multiple P2 receptor subtypes on platelets: a new interpretation of their function", Trends Pharmacol. Sci. 19, 391–394.
   PubMed Web of Science ®Google Scholar
• Cattaneo, M. and Cachet, C. (1999) "ADP receptors and clinical bleeding disorders", Arterioscler. Thromb. Vasc. Biol. 19, 2281–2285.
   PubMed Web of Science ®Google Scholar
• Jantzen, H.M., Milstone, D.S., Gousset, L., Conley, P.B. and Mortensen, R.M. (2001) "Impaired activation of murine platelets lacking Galpha(i2)", J. Clin. Investig. 108, 477–483.
   PubMed Web of Science ®Google Scholar
• Yang, J., Wu, J., Jiang, H., Mortensen, R., Austin, S., Manning, D.R., Woulfe, D. and Brass, L.F. (2002) "Signaling through Gi family members in platelets. Redundancy and specificity in the regulation of adenylyl cyclase and other effectors", J. Biol. Chem. 277, 46035–46042.
   PubMed Web of Science ®Google Scholar
• Dangelmaier, C., Jin, J., Smith, J.B. and Kunapuli, S.P. (2001) "Potentiation of thromboxane A2-induced platelet secretion by Gi signaling through the phosphoinositide-3 kinase pathway", Thromb. Haemost. 85, 341–348.
   PubMed Web of Science ®Google Scholar
• Jin, J., Quinton, T.M., Zhang, J., Rittenhouse, S.E. and Kunapuli, S.P. (2002) "Adenosine diphosphate (ADP)-induced thromboxane A(2) generation in human platelets requires coordinated signaling through integrin alpha(lb)-beta(3) and ADP receptors", Blood 99, 193–198.
   PubMed Web of Science ®Google Scholar
• Dorsam, R.T., Kim, S., Jin, J. and Kunapuli, S.P. (2002) "Coordinated signaling through both G12/13 and G(i) pathways is sufficient to activate GPIlb /Ma in human platelets", J. Biol. Chem. 277, 47588–47595.
   PubMed Web of Science ®Google Scholar
• Kim, S., Foster, C., Lecchi, A., Quinton, T.M., Prosser, D.M., Jin, J., Cattaneo, M. and Kunapuli, SE (2002) "Protease-activated receptors 1 and 4 do not stimulate G(i) signaling pathways in the absence of secreted ADP and cause human platelet aggregation independently of G(i) signaling", Blood 99, 3629–3636.
   PubMed Web of Science ®Google Scholar
• Paul, B.Z., Jin, J. and Kunapuli, SE (1999) "Molecular mechanism of thromboxane A(2)-induced platelet aggrega-tion. Essential role for p2t(ac) and alpha(2a) receptors", J. Biol. Chem. 274, 29108–29114.
   PubMed Web of Science ®Google Scholar
• Ayyanathan, K., Naylor, S.L. and Kunapuli, SE (1996) "Structural characterization and fine chromosomal mapping of the human P2Y1 purinergic receptor gene (P2YR1)", Som. Cell. Mol. Genet. 22, 419–424.
   PubMedGoogle Scholar
• Chambers, J.K., Macdonald, L.E., Sarau, H.M., Ames, R.S., Freeman, K., Foley, J.J., Zhu, Y., McLaughlin, M.M., Murdock, P., McMillan, L., Trill, J., Swift, A., Aiyar, N., Taylor, P., Vawter, L., Naheed, S., Szekeres, P., Hervieu, G., Scott, C., Watson, J.M., Murphy, A.J., Duzic, E., Klein, C., Bergsma, D.J., Wilson, S. and Livi, G.P. (2000) "A G protein-coupled receptor for UDP-glucose", J. Biol. Chem. 275, 10767–10771.
   PubMed Web of Science ®Google Scholar
• Bennett, J.S. (2001) "Novel platelet inhibitors", Annu. Rev. Med. 52, 161–184.
   PubMed Web of Science ®Google Scholar
• Sugidachi, A., Asai, F., Yoneda, K., Iwamura, R., Ogawa, T., Otsuguro, K. and Koike, H. (2001) "Antiplatelet action of R-99224, an active metabolite of a novel thienopyridine-type G(i)-linked P2T antagonist, CS-747", Br. J. Pharmacol. 132, 47–54.
   PubMed Web of Science ®Google Scholar
• Savi, P., Labouret, C., Delesque, N., Guette, F., Lupker, J. and Herbert, J.M. (2001) "P2y(12), a new platelet ADP receptor, target of clopidogrel", Biochem. Biophys. Res. Commun. 283, 379–383.
   PubMed Web of Science ®Google Scholar
• Jiang, Q., Guo, D., Lee, B.X., Van Rhee, A.M., Kim, Y.C., Nicholas, R.A., Schachter, J.B., Harden, T.K. and Jacobson, K.A. (1997) "A mutational analysis of residues essential for ligand recognition at the human P2Y1 receptor", Mol. Pharmacol. 52, 499–507.
   PubMed Web of Science ®Google Scholar
• Hoffmann, C., Moro, S., Nicholas, R.A., Harden, T.K. and Jacobson, K.A. (1999) "The role of amino acids in extracellular loops of the human P2Y1 receptor in surface expression and activation processes", J. Biol. Chem. 274, 14639–14647.
   PubMed Web of Science ®Google Scholar
• Moro, S., Hoffmann, C. and Jacobson, K.A. (1999) "Role of the extracellular loops of G protein-coupled receptors in ligand recognition: a molecular modeling study of the human P2Y1 receptor", Biochemistry 38, 3498–3507.
   PubMed Web of Science ®Google Scholar
• Cattaneo, M., Zighetti, M.L., Lombardi, R., Martinez, C., Lecchi, A., Conley, P.B., Ware, J. and Ruggeri, Z.M. (2003) "Molecular bases of defective signal transduction in the platelet P2Y12 receptor of a patient with congenital bleeding", Proc. Natl Acad. Sci. USA 100, 1978–1983.
   PubMed Web of Science ®Google Scholar
• Savi, E, Combalbert, J., Gaich, C., Rouchon, M.C., Maffrand, J.P., Berger, Y. and Herbert, J.M. (1994) "The antiaggregating activity of clopidogrel is due to a metabolic activation by the hepatic cytochrome P450-1A", Thromb. Haemost. 72, 313–317.
   PubMed Web of Science ®Google Scholar
• Clarke, T.A. and Waskell, L.A. (2003) "The metabolism of clopidogrel is catalyzed by human cytochrome P450 3A and is inhibited by atorvastatin", Drug Metab. Dispos. 31, 53–59.
   PubMed Web of Science ®Google Scholar
• Savi, P., Herbert, J.M., Pflieger, A.M., Dol, F., Delebassee, D., Combalbert, J., Defreyn, G. and Maffrand, J.P. (1992) "Importance of hepatic metabolism in the antiaggregating activity of the thienopyridine dopidogrel", Biochem. Pharma-col. 44, 527–532.
   PubMed Web of Science ®Google Scholar
• Maayani, S., Tagliente, T.M., Schwarz, T., Craddock-Royal, B., Alcala, C., Marrero, G. and Martinez, R. (2001) "Deaggrega-tion is an integral component of the response of platelets to ADP in vitro: kinetic studies of literature and original data", Platelets 12, 279–291.
   PubMed Web of Science ®Google Scholar
• Savi, P., Pereillo, J.M., Uzabiaga, M.F., Combalbert, J., Picard, C., Maffrand, J.P., Pascal, M. and Herbert, J.M. (2000) "Identification and biological activity of the active metabolite of clopidogrel", Thromb. Haemost. 84, 891–896.
   PubMed Web of Science ®Google Scholar
• Pereillo, J.M., Maftouh, M., Andrieu, A., Uzabiaga, ME, Fedeli, O., Savi, E, Pascal, M., Herbert, J.M., Maffrand, J.P. and Picard, C. (2002) "Structure and stereochemistry of the active metabolite of clopidogrel", Drug Metab. Dispos. 30, 1288–1295.
   PubMed Web of Science ®Google Scholar
• Rao, A.K. and Kowalska, M.A. (1987) "ADP-induced platelet shape change and mobilization of cytoplasmic ionized calcium are mediated by distinct binding sites on platelets: 5'-p-fluorosulfonylbenzoyladenosine is a weak platelet agonist", Blood 70, 751–756.
   PubMed Web of Science ®Google Scholar
• Cristalli, G. and Mills, D.C.B. (1993) "Identification of a receptor for ADP on blood platelets by photoaffinity labelling", Biochem. J. 291, 875–881.
   PubMed Web of Science ®Google Scholar
• Sugidachi, A., Asai, F., Ogawa, T., Inoue, T. and Koike, H. (2000) "The in vivo pharmacological profile of CS-747, a novel antiplatelet agent with platelet ADP receptor antagonist properties", Br. J. Pharmacol. 129, 1439–1446.
   PubMed Web of Science ®Google Scholar
• Ding, Z., Kim, S., Dorsam, R.T., Jin, J. and Kunapuli, S.P. (2003) "Inactivation of the human P2Y12 receptor by thiol reagents requires interaction with both extra-cellular cysteine residues, C17 and C270", Blood 101(10), 3908–3914.
   PubMed Web of Science ®Google Scholar
• Kam, P.C. and Nethery, C.M. (2003) "The thienopyridine derivatives (platelet adenosine diphosphate receptor anta-gonists), pharmacology and clinical developments", Anaes-thesia 58, 28–35.
   PubMed Web of Science ®Google Scholar
• Theroux, P., Angioi, M., Gallo, R., Ghitescu, M. and Frojmovic, M. Inter-individual variability in inhibition of platelet activation and aggregation by clopidogrel. Sup-plement to the Journal of Thrombosis and Haemostasis. 2003; Supplement for ISTH Meeting 2003: Session: Platelet Pharmocology I, Abstract P0235.
   Google Scholar
• A randomised, blinded, trial of clopidogrel versus aspirin in patients at risk of ischaemic events (CAPRIE). CAPRIE Steering Committee. Lancet. 1996; 348: 1329–1339.
   PubMed Web of Science ®Google Scholar
• Bertrand, M.E., Rupprecht, H.J., Urban, P., Gershlick, A.H. and Investigators, ET. (2000) "Double-blind study of the safety of clopidogrel with and without a loading dose in combination with aspirin compared with ticlopidine in combination with aspirin after coronary stenting: the clopidogrel aspirin stent international cooperative study (CLASSICS)", Circulation 102, 624–629.
   PubMed Web of Science ®Google Scholar
• (2001) New insights from PCI-CURE study. Cardiovasc J. S. Afr. 12, 290.
   PubMedGoogle Scholar
• Mitka, M. (2001) "Results of CURE trial for acute coronary syndrome", JAMA 285, 1828–1829.
   PubMed Web of Science ®Google Scholar
• Khot, U.N. and Nissen, S.E. (2002) "Is CURE a cure for acute coronary syndromes? Statistical versus clinical significance", J. Am. Coll. Cardiol. 40, 218–219.
   PubMed Web of Science ®Google Scholar
• (2001) The Clopidogrel in Unstable Angina to Prevent Recurrent Events trial Investiators (CURE). N. Engl. J. Med. 345, 494–502.
   PubMed Web of Science ®Google Scholar
• Hacke, W. (2002) "From CURE to MATCH: ADP receptor antagonists as the treatment of choice for high-risk atherothrombotic patients", Cerebrovasc. Dis. 13, 22–26.
   PubMed Web of Science ®Google Scholar