Safety and efficacy of targeting platelet proteinase-activated receptors in combination with existing anti-platelet drugs as antithrombotics in mice

British Journal of Pharmacology

Volumn 166, Issue 7, 2012, Pages 2188-2197

  Lee, H ^a   Sturgeon, S A ^a   Mountford, J K ^a   Jackson, S P ^a   Hamilton, J R ^a  

^a MONASH UNIVERSITY   (Australia)

Author keywords

platelets; protease activated receptors; thrombin; thrombosis

Indexed keywords

ACETYLSALICYLIC ACID; ACETYLSALICYLIC ACID CALCIUM; CLOPIDOGREL; HIRUDIN; LEPIRUDIN; PROTEIN INHIBITOR; PROTEINASE ACTIVATED RECEPTOR; PROTEINASE ACTIVATED RECEPTOR INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTICOAGULATION; ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG EFFICACY; DRUG POTENTIATION; DRUG SAFETY; HEMOSTASIS; IN VIVO STUDY; MOUSE; NONHUMAN; PREVENTIVE MEDICINE; PRIORITY JOURNAL; PROTEIN FUNCTION; PROTEIN INTERACTION; PROTEIN TARGETING; THROMBOSIS; TREATMENT RESPONSE;

ANIMALS; ASPIRIN; DISEASE MODELS, ANIMAL; FIBRINOLYTIC AGENTS; HEMOSTASIS; MICE; MICE, KNOCKOUT; PLATELET ACTIVATION; PLATELET AGGREGATION INHIBITORS; RECEPTORS, PROTEINASE-ACTIVATED; THROMBOSIS; TICLOPIDINE;

EID: 84863660786     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2012.01944.x     Document Type: Article

References (37)

1. Ahn H-S, Foster C, Boykow G, Stamford A, Manna M, Graziano M, (2000). Inhibition of cellular action of thrombin by N3-cyclopropyl-7-{[4-(1- methylethyl)phenyl]methyl}-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine (SCH 79797), a nonpeptide thrombin receptor antagonist. Biochem Pharmacol 60: 1425-1434.
2. American Heart Association (2006). Heart Disease and Stroke Statistics: 2006 Update. American Heart Association: Dallas, TX.
3. Andreotti F, Testa L, Biondi-Zoccai GG, Crea F, (2006). Aspirin plus warfarin compared to aspirin alone after acute coronary syndromes: an updated and comprehensive meta-analysis of 25,307 patients. Eur Heart J 27: 519-526.
4. Antithrombotic Trialists' Collaboration. (2002). Collaborative meta-analysis of randomised trials of antiplatelet therapy for prevention of death, myocardial infarction, and stroke in high risk patients. Br Med J 324: 71-86.
5. Becker RC, (2002). Antithrombotic therapy after myocardial infarction. N Engl J Med 347: 1019-1022.
6. Becker RC, Meade TW, Berger PB, Ezekowitz M, O'Connor CM, Vorchheimer DA, et al,. (2008). The primary and secondary prevention of coronary artery disease: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines (8th Edition). Chest 133 (6 Suppl.): 776S-814S.
7. Becker RC, Moliterno DJ, Jennings LK, Pieper KS, Pei J, Niederman A, et al,. (2009). Safety and tolerability of SCH 530348 in patients undergoing non-urgent percutaneous coronary intervention: a randomised, double-blind, placebo-controlled phase II study. Lancet 373: 919-928.
8. Camerer E, Duong DN, Hamilton JR, Coughlin SR, (2004). Combined deficiency of protease-activated receptor-4 and fibrinogen recapitulates the hemostatic defect but not the embryonic lethality of prothrombin deficiency. Blood 103: 152-154.
9. CAPRIE Steering Committee (1996). A randomised, blinded, trial of clopidogrel versus aspirin in patients at risk of ischaemic events (CAPRIE). Lancet 348: 1329-1339.
10. CARSC Investigators (1997). Randomised double-blind trial of fixed low-dose warfarin with aspirin after myocardial infarction. Lancet 350 (9075): 389-396.
11. Chackalamannil S, Xia Y, Greenlee WJ, Clasby M, Doller D, Tsai H, et al,. (2005). Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents. J Med Chem 48: 5884-5887.
12. Cornelissen I, Palmer D, David T, Wilsbacher L, Concengco C, Conley P, et al,. (2011). Roles and interactions among protease-activated receptors and P2ry12 in hemostasis and thrombosis. Proc Natl Acad Sci U S A 107: 18605-18610.
13. Coughlin SR, (2000). Thrombin signalling and protease-activated receptors. Nature 407: 258-264.
14. Denninger MH, Necciari J, Serre-Lacroix E, Sissmann J, (1999). Clopidogrel antiplatelet activity is independent of age and presence of atherosclerosis. Semin Thromb Hemost 25 (Suppl. 2): 41-45.
15. Derian CK, Damiano BP, Addo MF, Darrow AL, D'Andrea MR, Nedelman M, et al,. (2003). 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 304: 855-861.
16. Fiore LD, Ezekowitz MD, Brophy MT, Lu D, Sacco J, Peduzzi P, (2002). Department of Veterans Affairs Cooperative Studies Program Clinical Trial comparing combined warfarin and aspirin with aspirin alone in survivors of acute myocardial infarction: primary results of the CHAMP study. Circulation 105: 557-563.
17. Goto S, Ogawa H, Takeuchi M, Flather MD, Bhatt DL, (2010). Double-blind, placebo-controlled Phase II studies of the protease-activated receptor 1 antagonist E5555 (atopaxar) in Japanese patients with acute coronary syndrome or high-risk coronary artery disease. Eur Heart J 31: 2601-2613.
18. Hamilton JR, (2009). Protease-activated receptors as targets for antiplatelet therapy. Blood Rev 23: 61-65.
19. Hamilton JR, Cornelissen I, Coughlin SR, (2004). 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 2: 1429-1435.
20. Hurlen M, Abdelnoor M, Smith P, Erikssen J, Arnesen H, (2002). Warfarin, aspirin, or both after myocardial infarction. N Engl J Med 347: 969-974.
21. Kahn ML, Nakanishi-Matsui M, Shapiro MJ, Ishihara H, Coughlin SR, (1999). Protease-activated receptors 1 and 4 mediate activation of human platelets by thrombin. J Clin Invest 103: 879-887.
22. Kilkenny C, Browne W, Cuthill IC, Emerson M, Altman DG, (2010) NC3Rs Reporting Guidelines Working Group. Br J Pharmacol 160: 1577-1579.
23. Kuster LJ, Frolich JC, (1986). Platelet aggregation and thromboxane release induced by arachidonic acid, collagen, ADP and platelet-activating factor following low dose acetylsalicylic acid in man. Prostaglandins 32: 415-423.
24. Lee H, Sturgeon SA, Jackson SP, Hamilton JR, (2012). The contribution of thrombin-induced platelet activation to thrombus growth is diminished under pathological blood shear conditions. Thromb Haemost 107: 328-337.
25. McGrath J, Drummond G, McLachlan E, Kilkenny C, Wainwright C, (2010). Guidelines for reporting experiments involving animals: the ARRIVE guidelines. Br J Pharmacol 160: 1573-1576.
26. Maxwell MJ, Yuan Y, Anderson KE, Hibbs ML, Salem HH, Jackson SP, (2004). SHIP1 and Lyn kinase negatively regulate integrin alpha IIb beta 3 signaling in platelets. J Biol Chem 279: 32196-32204.
27. Momi S, Pitchford SC, Alberti PF, Minuz P, Del Soldato P, Gresele P, (2005). Nitroaspirin plus clopidogrel versus aspirin plus clopidogrel against platelet thromboembolism and intimal thickening in mice. Thromb Haemost 93: 535-543.
28. Morrow DA, Scirica BM, Fox KA, Berman G, Strony J, Veltri E, et al,. (2009). Evaluation of a novel antiplatelet agent for secondary prevention in patients with a history of atherosclerotic disease: design and rationale for the Thrombin-Receptor Antagonist in Secondary Prevention of Atherothrombotic Ischemic Events (TRA 2 degrees P)-TIMI 50 trial. Am Heart J 158: 335-341. e333.
29. Roger VL, Go AS, Lloyd-Jones DM, Adams RJ, Berry JD, Brown TM, et al,. (2011). Heart disease and stroke statistics-2011 update: a report from the American Heart Association. Circulation 123: e18-e209.
30. Sambrano GR, Weiss EJ, Zheng YW, Huang W, Coughlin SR, (2001). Role of thrombin signalling in platelets in haemostasis and thrombosis. Nature 413: 74-78.
31. Schoenwaelder SM, Jarman KE, Gardiner EE, Hua M, Qiao J, White MJ, et al,. (2011). Bcl-xL-inhibitory BH3 mimetics can induce a transient thrombocytopathy that undermines the hemostatic function of platelets. Blood 118: 1663-1674.
32. Sturgeon SA, Jones C, Angus JA, Wright CE, (2006). Adaptation of the Folts and electrolytic methods of arterial thrombosis for the study of anti-thrombotic molecules in small animals. J Pharmacol Toxicol Methods 53: 20-29.
33. TRA*CER Executive and Steering Committees (2009). The Thrombin Receptor Antagonist for Clinical Event Reduction in Acute Coronary Syndrome (TRA*CER) trial: study design and rationale. Am Heart J 158: 327-334. e324.
34. Tricoci P, Huang Z, Held C, Moliterno DJ, Armstrong PW, Van de Werf F, et al,. (2012). Thrombin-receptor antagonist vorapaxar in acute coronary syndromes. N Engl J Med 366: 20-33.
35. Vandendries ER, Hamilton JR, Coughlin SR, Furie B, Furie BC, (2007). Par4 is required for platelet thrombus propagation but not fibrin generation in a mouse model of thrombosis. Proc Natl Acad Sci U S A 104: 288-292.
36. Weiss EJ, Hamilton JR, Lease KE, Coughlin SR, (2002). Protection against thrombosis in mice lacking PAR3. Blood 100: 3240-3244.
37. Wu CC, Teng CM, (2006). Comparison of the effects of PAR1 antagonists, PAR4 antagonists, and their combinations on thrombin-induced human platelet activation. Eur J Pharmacol 546: 142-147.