Blood Reviews
Volume 23, Issue 2 , Pages 61-65 , March 2009

Protease-activated receptors as targets for antiplatelet therapy

References 

  1. Heart Disease and Stroke Statistics: 2006 update. Dallas, USA: American Heart Association; 2006.
  2. World Health Report 2002. Geneva, Switzerland: World Health Organisation; 2002.
  3. Antithrombotic triallists collaboration. Collaborative meta-analysis of randomised trials of antiplatelet therapy for prevention of death, myocardial infarction, and stroke in high risk patients. Brit Med J 2002;324:71–86.
  4. Tran HA, Anand SS, Hankey GJ, Eikelboom JW. Aspirin resistance. Thromb Res. 2007;120:337–346
  5. Gurbel PA, Tantry US. Aspirin and clopidogrel resistance: consideration and management. J Interv Cardiol. 2006;19:439–448
  6. Gladding P, Webster M, Ormiston J, Olsen S, White H. Antiplatelet drug nonresponsiveness. Am Heart J. 2008;155:591–599
  7. Gum PA, Kottke-Marchant K, Welsh PA, White J, Topol EJ. A prospective, blinded determination of the natural history of aspirin resistance among stable patients with cardiovascular disease. J Am Coll Cardiol. 2003;41:961–965
  8. Englyst NA, Horsfield G, Kwan J, Byrne CD. Aspirin resistance is more common in lacunar strokes than embolic strokes and is related to stroke severity. J Cereb Blood Flow Metab. Advance online publication, 5 March 2008. doi:10.1038/jcbfm.2008.9.
  9. Coma-Canella I, Velasc A. Variability in individual responsiveness to aspirin: clinical implications and treatment. Cardiovasc Hematol Disord Drug Targets. 2007;7:274–287
  10. Patel D, Moonis M. Clinical implications of aspirin resistance. Expert Rev Cardiovasc Ther. 2007;5:969–975
  11. CAPRIE Steering Committee . A randomised, blinded, trial of clopidogrel versus aspirin in patients at risk of ischaemic events (CAPRIE). Lancet. 1996;348:1329–1339
  12. Bhatt DL, Fox KA, Hacke W, et al. Clopidogrel and aspirin versus aspirin alone for the prevention of atherothrombotic events. New Engl J Med. 2006;354:1706–1717
  13. Gurbel PA, Bliden KP, Hiatt BL, O’Connor CM. Clopidogrel for coronary stenting: response variability, drug resistance, and the effect of pretreatment platelet reactivity. Circulation. 2003;107:2908–2913
  14. Karvouni E, Katritsis DG, Ioannidis JP. Intravenous glycoprotein IIb/IIIa receptor antagonists reduce mortality after percutaneous coronary interventions. J Am Coll Cardiol. 2003;41:26–32
  15. Sane DC, Damaraju LV, Topol EJ, et al. Occurrence and clinical significance of pseudothrombocytopenia during abciximab therapy. J Am Coll Cardiol. 2000;36:75–83
  16. Chew DP, Bhatt DL, Sapp S, Topol EJ. Increased mortality with oral platelet glycoprotein IIb/IIIa antagonists: a meta-analysis of phase III multicenter randomized trials. Circulation. 2001;103:201–206
  17. Furie B, Furie BC. Thrombus formation in vivo. J Clin Invest. 2005;115:3355–3362
  18. Brass LF. Thrombus formation: stability matters. Blood. 2006;108:2883–2884
  19. Hamilton JR, Kaplan Z, Jackson SP, Opat S. Antiplatelet therapy: current status & future prospects. Expert Opin Drug Discov. 2007;2:1–6
  20. Savage B, Saldivar E, Ruggeri ZM. Initiation of platelet adhesion by arrest onto fibrinogen or translocation on von Willebrand factor. Cell. 1996;84:289–297
  21. Kato K, Kanaji T, Russell S, et al. The contribution of glycoprotein VI to stable platelet adhesion and thrombus formation illustrated by targeted gene deletion. Blood. 2003;102:1701–1707
  22. Denis CV, Wagner DD. Platelet adhesion receptors and their ligands in mouse models of thrombosis. Arterioscler Thromb Vasc Biol. 2007;27:728–739
  23. Brass LF, Jiang H, Wu J, Stalker TJ, Zhu L. Contact-dependent signaling events that promote thrombus formation. Blood Cells Mol Dis. 2006;36:157–161
  24. Coughlin SR. Thrombin signalling and protease-activated receptors. Nature. 2000;407:258–264
  25. Kahn ML, Nakanishi-Matsui M, Shapiro MJ, Ishihara H, Coughlin SR. Protease-activated receptors 1 and 4 mediate activation of human platelets by thrombin. J Clin Invest. 1999;103:879–887
  26. Jackson SP. The growing complexity of platelet aggregation. Blood. 2007;109:5087–5095
  27. Kahn ML, Zheng Y-W, Huang W, et al. A dual thrombin receptor system for platelet activation. Nature. 1998;394:690–694
  28. Nakanishi-Matsui M, Zheng YW, Sulciner DJ, Weiss EJ, Ludeman MJ, Coughlin SR. PAR3 is a cofactor for PAR4 activation by thrombin. Nature. 2000;404:609–613
  29. Sambrano GR, Weiss EJ, Zheng YW, Huang W, Coughlin SR. Role of thrombin signalling in platelets in haemostasis and thrombosis. Nature. 2001;413:74–78
  30. Hamilton JR, Cornelissen I, Coughlin SR. Impaired hemostasis and protection against thrombosis in protease-activated receptor 4-deficient mice is due to lack of thrombin signaling in platelets. J Thromb Haemost. 2004;2:1429–1435
  31. Vandendries ER, Hamilton JR, Coughlin SR, Furie B, Furie BC. Par4 is required for platelet thrombus propagation but not fibrin generation in a mouse model of thrombosis. Proc Natl Acad Sci USA. 2007;104:288–292
  32. Camerer E, Duong DN, Hamilton JR, Coughlin SR. Combined deficiency of protease-activated receptor-4 and fibrinogen recapitulates the hemostatic defect but not the embryonic lethality of prothrombin deficiency. Blood. 2004;103:152–154
  33. Ishihara H, Zeng D, Connolly AJ, Tam C, Coughlin SR. Antibodies to protease-activated receptor 3 inhibit activation of mouse platelets by thrombin. Blood. 1998;91:4152–4157
  34. Weiss EJ, Hamilton JR, Lease KE, Coughlin SR. Protection against thrombosis in mice lacking PAR3. Blood. 2002;100:3240–3244
  35. Cook JJ, Sitko GR, Bednar B, et al. An antibody against the cloned thrombin receptor inhibits experimental arterial thrombosis in the African green monkey. Circulation. 1995;91:2961–2971
  36. Derian CK, Damiano BP, Addo MF, et al. Blockade of the thrombin receptor protease-activated receptor-1 with a small-molecule antagonist prevents thrombus formation and vascular occlusion in nonhuman primates. J Pharmacol Exp Ther. 2003;304:855–861
  37. Vu T-KH, Hung DT, Wheaton VI, Coughlin SR. Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation. Cell. 1991;64:1057–1068
  38. Coughlin SR, Vu T-KH, Hung DT, Wheaton VI. Characterization of a functional thrombin receptor. J Clin Invest. 1992;89:351–355
  39. Chackalamannil S, Xia Y, Greenlee WJ, et al. Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents. J Med Chem. 2005;48:5884–5887
  40. Chelliah MV, Chackalamannil S, Xia Y, et al. Heterotricyclic himbacine analogs as potent, orally active thrombin receptor (protease activated receptor-1) antagonists. J Med Chem. 2007;50:5147–5160
  41. Schering-Plough announces initiation of two phase III clinical trials for novel selective antiplatelet therapy (TRA-SCH 530348); 2007. <http://www.schering-plough.com/schering_plough/news/release.jsp?releaseID=987054>.
  42. A double-blind study of E5555 in Japanese patients with acute coronary syndrome; 2008. <http://clinicaltrials.gov/ct2/show/NCT00619164>.

PII: S0268-960X(08)00053-2

doi: 10.1016/j.blre.2008.06.002

Blood Reviews
Volume 23, Issue 2 , Pages 61-65 , March 2009

Article Tools

* Image Usage & Resolution