Bibliography
- American Heart Association. Heart disease and stroke statistics—2006 update. American Heart Association, Dallas; 2006
- WHO. Atlas of heart disease and stroke. World Health Organization, Geneva; 2004
- Brass LF. Thrombin and platelet activation. Chest 2003;124:18S-25S
- Davi G, Patrono C. Platelet activation and atherothrombosis. N Engl J Med 2007;357:2482-94
- Varga-Szabo D, Pleines I, Nieswandt B. Cell adhesion mechanisms in platelets. Arterioscler Thromb Vasc Biol 2008;28:403-12
- Offermanns S. Activation of platelet function through G protein-coupled receptors. Circ Res 2006;99:1293-304
- Storey RF, Judge HM, Wilcox RG, Heptinstall S. Inhibition of ADP-induced Pselectin expression and platelet-leukocyte conjugate formation by clopidogrel and the P2Y12 receptor antagonist AR-C69931MX but not aspirin. Thromb Haemost 2002;88:488-94
- Andre P, Prasad KS, Denis CV, CD40L stabilizes arterial thrombi by a beta3 integrin-dependent mechanism. Nat Med 2002;8:247-52
- Hagihara M, Higuchi A, Tamura N, Platelets, after exposure to a high shear stress, induce IL-10-producing, mature dendritic cells in vitro. J Immunol 2004;172:5297-303
- Andersen H, Greenberg DL, Fujikawa K, Protease-activated receptor 1 is the primary mediator of thrombin-stimulated platelet procoagulant activity. Proc Natl Acad Sci USA 1999;96:11189-93
- Ohlmann P, Eckly A, Freund M, ADP induces partial platelet aggregation without shape change and potentiates collagen-induced aggregation in the absence of Galphaq. Blood 2000;96:2134-9
- Meadows TA, Bhatt DL. Clinical aspects of platelet inhibitors and thrombus formation. Circ Res 2007;100:1261-75
- Foster CJ, Prosser DM, Agans JM, Molecular identification and characterization of the platelet ADP receptor targeted by thienopyridine antithrombotic drugs. J Clin Invest 2001;107:1591-8
- Antithrombotic Trialists' Collaboration. Collaborative meta-analysis of randomized trials of antiplatelet therapy for prevention of death, myocardial infarction, and stroke in high risk patients. Br Med J 2002;324:71-86
- Lewis HD Jr, Davis JW, Archibald DG, Protective effects of aspirin against acute myocardial infarction and death in men with unstable angina. Results of a Veterans Administration Cooperative Study. N Engl J Med 1983;309:396-403
- Schwartz L, Bourassa MG, Lesperance J, Aspirin and dipyridamole in the prevention of restenosis after percutaneous transluminal coronary angioplasty. N Engl J Med 1988;318:1714-19
- Antiplatelet Trialists' Collaboration. Collaborative overview of randomised trials of antiplatelet therapy. I: prevention of death, myocardial infarction, and stroke by prolonged antiplatelet therapy in various categories of patients. Br Med J 1994;308:81-106
- CAPRIE Steering Committee. A randomised, blinded, trial of clopidogrel versus aspirin in patients at risk of ischaemic events (CAPRIE). Lancet 1996;348:1329-39
- Yusuf S, Zhao F, Mehta SR, Effects of clopidogrel in addition to aspirin in patients with acute coronary syndromes without ST-segment elevation. N Engl J Med 2001;345:494-502
- Steinhubl SR, Berger PB, Mann JT III, Early and sustained dual oral antiplatelet therapy following percutaneous coronary intervention: a randomized controlled trial. J Am Med Assoc 2002;288:2411-20
- Sabatine MS, Cannon CP, Gibson CM, Addition of clopidogrel to aspirin and fibrinolytic therapy for myocardial infarction with ST-segment elevation. N Engl J Med 2005;352:1179-89
- Chen ZM, Jiang LX, Chen YP, Addition of clopidogrel to aspirin in 45,852 patients with acute myocardial infarction: randomized placebo-controlled trial. Lancet 2005;366:1607-21
- Leon C, Alex M, Klocke A, Platelet ADP receptors contribute to the initiation of intravascular coagulation. Blood 2004;103:594-600
- van der Meijden PE, Feijge MA, Giesen PL, Platelet P2Y12 receptors enhance signalling towards procoagulant activity and thrombin generation. A study with healthy subjects and patients at thrombotic risk. Thromb Haemost 2005;93:1128-36
- Gurbel PA, Bliden KP, Guyer K, Delayed thrombin-induced platelet-fibrin clot generation by clopidogrel: a new dose-related effect demonstrated by thrombelastography in patients undergoing coronary artery stenting. Thromb Res 2007;119:563-70
- Bal dit Sollier C, Mahe I, Berge N, Reduced thrombus cohesion in an ex vivo human model of arterial thrombosis induced by clopidogrel treatment: kinetics of the effect and influence of single and double loading-dose regimens. Thromb Res 2003;111:19-27
- Angiolillo DJ, Capranzano P, Desai B, Impact of P2Y12 inhibitory effects induced by clopidogrel on platelet procoagulant activity in type 2 diabetes mellitus patients. Thromb Res 2009;124:318-22
- Angiolillo DJ, Guzman LA, Bass TA. Current antiplatelet therapies: benefits and limitations. Am Heart J 2008;156:S3-9
- Angiolillo DJ, Fernandez-Ortiz A, Bernardo E, Variability in individual responsiveness to clopidogrel: clinical implications, management, and future perspectives. J Am Coll Cardiol 2007;49:1505-16
- Krasopoulos G, Brister SJ, Beattie WS, Buchanan MR. Aspirin ‘resistance’ and risk of cardiovascular morbidity: systematic review and meta-analysis. Br Med J 2008;336:195-8
- Serebruany VL, Malinin AI, Ferguson JJ, Bleeding risks of combination vs. single antiplatelet therapy: a meta-analysis of 18 randomized trials comprising 129,314 patients. Fundam Clin Pharmacol 2008;22(3):315-21
- Wiviott SD, Braunwald E, McCabe CH, ; TRITON TIMI 38 Investigators. Prasugrel versus clopidogrel in patients with acute coronary syndromes. N Engl Med 2007;357:2001-15
- Wallentin L, Becker RC, Budaj A, ; for the PLATO investigators. Ticagrelor versus Clopidogrel in patients with acute coronary syndromes. N Engl J Med 2009;361:1045-57
- Coughlin SR. Protease-activated receptors in heamostasis, thrombosis and vascular biology. J Thromb Heamost 2005;3:1800-14
- Brummel KE, Paradis SG, Butenas S, Thrombin functions during tissue factor-induced blood coagulation. Blood 2002;100:148-52
- Ossovskaya VS, Bunnett NW. Protease-activated receptors: contribution to physiology and disease. Physiol Rev 2004;84:579-621
- Shah R. Protease-activated receptors in cardiovascular health and diseases. Am Heart J 2009;157:253-62
- Kahn ML, Nakanishi-Matsui M, Shapiro MJ, Protease-activated receptors 1 and 4 mediate activation of human platelets by thrombin. J Clin Invest 1999;103:879-87
- Steinhoff M, Buddenkotte J, Shpacovitch V, Proteinase-activated receptors: transducers of proteinase-mediated signaling in inflammation and immune response. Endocr Rev 2005;26:1-43
- Henriksen RA, Hanks VK. PAR-4 agonist AYPGKF stimulates thromboxane production by human platelets. Arterioscler Thromb Vasc Biol 2002;22:861-6
- Covic L, Singh C, Smith H, Kuliopulos A. Role of the PAR4 thrombin receptor in stabilizing platelet-platelet aggregates as revealed by a patient with Hermansky–Pudlak syndrome. Thromb Haemost 2002;87:722-7
- Lova P, Campus F, Lombardi R, Contribution of protease-activated receptors 1 and 4 and glycoprotein Ib-IX-V in the Gi-independent activation of platelet Rap1B by thrombin. J Biol Chem 2004;279:25299-306
- Smith CC, Wilson AP, Prichard BN, Betteridge DJ. Stimulus-induced release of endogenous catecholamines from human washed platelets. Clin Sci (Lond) 1986;70:495-500
- Henn V, Slupsky JR, Grafe M, CD40 ligand on activated platelets triggers an inflammatory reaction of endothelial cells. Nature 1998;391:591-4
- Stenberg PE, McEver RP, Shuman MA, A platelet alpha-granule membrane protein (GMP-140) is expressed on the plasma membrane after activation. J Cell Biol 1985;101:880-6
- Shattil SJ, Kashiwagi H, Pampori N. Integrin signaling: the platelet paradigm. Blood 1998;91:2645-57
- Offermanns S, Toombs CF, Hu YH, Simon MI. Defective platelet activation in Galphaq-deficient mice. Nature 1997;389:183-6
- Andersen H, Greenberg DL, Fujikawa K, Protease-activated receptor 1 is the primary mediator of thrombin-stimulated platelet procoagulant activity. Proc Natl Acad Sci USA 1999;96:11189-93
- Goldsack NR, Chambers RC, Dabbagh K, Laurent GJ. Thrombin. Int J Biochem Cell Biol 1998;30:641-6
- Faruqi TR, Weiss EJ, Shapiro MJ, Structure-function analysis of protease-activated receptor 4 tethered ligand peptides. Determinants of specificity and utility in assays of receptor function. J Biol Chem 2000;275:19728-34
- Leger AJ, Covic L, Kuliopulos A. Protease-activated receptors in cardiovascular diseases. Circulation 2006;114:1070-7
- The TRACER Exective and Steering Committees. The Thrombin Receptor Antagonist for Clinical Event Reduction in Acute Coronary Syndrome (TRACER) trial: study design and rationale. Am Heart J 2009;158:327-34
- Morrow DA, Scirica BM, Fox KA, 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 P)-TIMI 50 trial. Am Heart J 2009;158:335-41
- Safety and tolerability of E5555 and its effects on markers of intravascular inflammation in subjects with coronary artery disease. Bethesda, MD: US National Institutes of Health, 2006. Available from: http://www.clinicaltrials.gov/ct2/show/NCT00312052. [Last accessed 7 September 2010]
- Goto S, Ogawa H, Takeuchi M, Flather MD, Bhatt DL; on Behalf of the J-LANCELOT (Japanese-Lesson from Antagonizing the cellular Effect of Thrombin) investigators. 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. 2010 Aug 30 [Epub ahead of print]
- Leonardi S, Tricoci P, Becker RC. Thrombin receptor antagonists for the treatment of atherothromosis: therapeutic potential of vorapaxar and e-5555. Drugs 2010;70(14):1771-83
- Chackalamannil S, Davies RJ, Asberom T, A highly efficient total synthesis of (+)-himbacine. J Am Chem Soc 1996;118:9812-13
- Doller D, Chackalamannil S, Czarniecki M, Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists. Bioorg Med Chem Lett 1999;9:901-6
- Oestreich J. SCH-530348, a thrombin receptor (PAR-1) antagonist for the prevention and treatment of atherothrombosis. Curr Opin Invest Drugs 2009;10:988-96
- Chintala MS, Chiu PJ, Bernadino V, Disparate effects of thrombin receptor activating peptide on platelets and peripheral vasculature in rats. Eur J Pharmacol 1998;349:237-43
- Chackalamannil S, Xia Y, Greenlee WJ, Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents. J Med Chem 2005;48:5884-7
- Chintala M, Ahn H, Foster C, Antithrombotic effects of SCH 205831: a potent, selective and orally active antagonist of the PAR-1 thrombin receptor. J Thromb Haemost 2005;3: abstract OR286
- Chintala M, Kurowski S, Vemulapalli S, Efficacy of SCH 602539, a selective thrombin receptor antagonist alone and in combination with cangrelor in a Folts model of thrombosis in anesthetized monkeys. Eur Heart J 2007;28(Suppl 1):, abstract 188
- Chackalamannil S, Wang Y, Greenlee WJ, Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity. J Med Chem 2008;51:3061-4
- Chintala M, Shimizu K, Ogawa M, Basic and translational research on proteinase-activated receptors: antagonism of the proteinase-activated receptor 1 for thrombin, a novel approach to antiplatelet therapy for atherothrombotic disease. J Pharmacol Sci 2008;108:433-8
- Kosoglou T, Reyderman L, Fales RR, Pharmacodynamics and pharmacokinetics of a novel protease-activated receptor (PAR-1) antagonist SCH 530348. Circulation 2005;112(Suppl II): II-32
- Kosoglou T, Tiessen R, Van Vliet AA, Safety and tolerability of SCH 530348, a novel antiplatelet agent, after single and multiple oral dosing in healthy subjects. Eur Heart J 2008;29(Suppl 201):P1340
- Reyderman L, Kosoglou T, Kasserra C, Lack of ethnic differences in the pharmacodynamics (PD) and pharmacokinetics (PK) of SCH 530348, a novel oral antiplatelet agent, in Japanese and Caucasian subjects. Clin Pharmacol Ther 2009;85(Suppl S21): PI-41
- Kosoglou T, Reyderman L, Kasserra C, Optimizing dose of the novel thrombin receptor antagonist SCH 530348 based on pharmacodynamics and pharmacokinetics in healthy subjects. Clin Pharmacol Ther 2008;83(Suppl 1):S55
- Becker RC, Moliterno DJ, Jennings LK, Safety and tolerability of SCH 530348 in patients undergoing non-urgent percutaneous coronary intervention: a randomised, double-blind, placebo-controlled Phase II study. Lancet 2009;373:919-28
- Goto S, Yamaguchi T, Ikeda Y, Safety and exploratory efficacy of the novel thrombin receptor (PAR-1) antagonist SCH530348 for non-ST-segent elevation acute coronary syndrome. J Atheroscler Thromb 2010;17(2):156-64
- Shinihara Y, Goto S, Doi M, Jensen P. Safety of the Novel Protese-Activated Receptor-1 Antagonist Vorapaxar in Japanese Patients with A History of Ischemic Stroke. J Stroke Cererovasc Dis 2010; In press
- Matsuoka T, Kogushi M, Kawata T, Inhibitory effect of E5555, an orally active thrombin receptor antagonist, on intimal hyperplasia following balloon injury [abstract]. JACC 2004;43:68A
- Kogushi M, Yokohama H, Kitamura S, Hishinuma I. Effects of E5555, a protease-activated receptor-1 antagonist, on the inflammatory markers in vitro. J Thromb Haemost 2007;5: P-M-059
- Kai Y, Hirano K, Maeda Y, Prevention of the hypercontractile response to thrombin by proteinase-activated receptor-1 antagonist in subarachnoid hemorrhage. Stroke 2007;38:3259-65
- Serebruany VL, Kogushi M, Dastros-Pitei D, The in-vitro effects of E5555, a protease-activated receptor (PAR)-1 antagonist, on platelet biomarkers in healthy volunteers and patients with coronary artery disease. Thromb Haemost 2009;102:111-19
- Takeuchi M, Kageyama M, Kitamura S, Pharmacodinamics and safety of a novel protease activated receptor-1 antagonist E5555 in healthy volunteers. Eur Heart J 2007;28(Suppl):14
- Kato Y, Kita Y, Hirasawa-Taniyama T, Inhibition of arterial thrombosis by a protease activeted receptor 1 antagonist, FR171113 in the guinea pig. Eur J Pharmacol 2003;473:163-9
- Angiolillo DJ, Capodanno D, Goto S. Platelet thrombin receptor antagonism and atherothrombosis. Eur Heart J 2010;31:17-28