RWJ-58259: A Selective Antagonist of Protease Activated Receptor-1

Cardiovascular Drug Reviews

Volumn 21, Issue 4, 2003, Pages 313-326

  Damiano, Bruce P ^a   Derian, Claudia K ^a   Maryanoff, Bruce E ^a   Zhang, Han Cheng ^a   Gordon, Patricia Andrade ^a  

^a J W Johnson Pharmaceutical Res I   (United States)

Author keywords

Antithrombotics; Platelet aggregation; Protease activated receptor (PAR 1); Restenosis; Thrombin; Vascular injury

Indexed keywords

15 HYDROXY 11ALPHA,9ALPHA EPOXYMETHANOPROSTA 5,13 DIENOIC ACID; ACETYLSALICYLIC ACID; G PROTEIN COUPLED RECEPTOR; INOGATRAN; N [3 AMINO 1 [[(PHENYLMETHYL)AMINO]CARBONYL]PROPYL] ALPHA [[[[[1 (2,6 DICHLOROPHENYL)METHYL] 3 (1 PYRROLIDINYLMETHYL) 1H INDAZOL 6 YL]AMINO]CARBONYL]AMINO] 3,4 DIFLUOROBENZENEPROPANAMIDE; PROTEINASE ACTIVATED RECEPTOR 1; PROTEINASE ACTIVATED RECEPTOR 3; PROTEINASE ACTIVATED RECEPTOR 4; RECEPTOR BLOCKING AGENT; RECOMBINANT HIRUDIN; RWJ 56110; RWJ 58259; THROMBIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTERIOVENOUS SHUNT; ARTERY OCCLUSION; ATHEROSCLEROSIS; BLOOD CLOTTING; CALCIUM CELL LEVEL; CALCIUM SIGNALING; CAROTID ARTERY INJURY; CELL PROLIFERATION; CELL TYPE; DISEASE ASSOCIATION; DRUG ANTAGONISM; DRUG EFFICACY; DRUG POTENCY; DRUG SELECTIVITY; GUINEA PIG; HEART INFARCTION; HUMAN; HUMAN CELL; HYDROXYLATION; IC 50; INFLAMMATION; NEOPLASM; NERVE DEGENERATION; NONHUMAN; OXIDATION; PERCUTANEOUS TRANSLUMINAL ANGIOPLASTY; PHOTOACTIVATION; PRIMATE; PRIORITY JOURNAL; PROTEIN DEGRADATION; PROTEIN EXPRESSION; PROTEIN FUNCTION; RAT; REVIEW; SIGNAL TRANSDUCTION; SMOOTH MUSCLE FIBER; STROKE; THROMBOCYTE; THROMBOCYTE AGGREGATION; THROMBOGENESIS; THROMBOSIS; TREATMENT INDICATION; TREATMENT OUTCOME;

EID: 0348050052     PISSN: 08975957     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1527-3466.2003.tb00124.x     Document Type: Review

References (40)

1. Andrade-Gordon P, Maryanoff BE, Derian CK, et al. Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. Proc Natl Acad Sci USA 1999;96:12257-12262.
2. Andrade-Gordon P, Derian CK, Maryanoff BE, et al. Administration of a potent antagonist of protease-activated receptor-1 (PAR-1) attenuates vascular restenosis following balloon angioplasty in rats. J Pharmacol Exp Ther 2001;298:34-42.
3. Antonaccio MJ, Normandin D, Serafino R, Moreland S. Effects of thrombin and thrombin receptor activating peptides on rat aortic vascular smooth muscle. J Pharmacol Exp Ther 1993;266:125-132.
4. Chambers RC, Leoni P, Blanc-Brude OP, Wembridge DE, Laurent GJ. Thrombin is a potent inducer of connective tissue growth factor production via proteolytic activation of protease-activated receptor-1. J Biol Chem 2000;275:35584-35591.
5. Cheung W-M, D'Andrea MR, Andrade-Gordon P, Damiano BP. Altered vascular injury responses in mice deficient in protease-activated receptor-1. Arterioscler Thromb Vasc Biol 1999;19:3014-3024.
6. Connolly AJ, Ishihara H, Kahn ML, Farese RV, Jr., Coughlin SR. Role of the thrombin receptor in development and evidence for a second receptor. Nature (London) 1996;381:516-519.
7. Connolly TM, Condra C, Feng D-M, et al. Species variability in platelet and other cellular responsiveness to thrombin receptor-derived peptides. Thromb Haemostas 1994;72:627-633.
8. Corvera CU, Dery O, McConalogue K, et al. Mast cell tryptase regulates rat colonic myocytes through proteinase-activated receptor 2. J Clin Invest 1997;100:1383-1393.
9. Coughlin SR. Protease-activated receptors and platelet function. Thromb Haemostas 1999;82:353-356.
10. Dabbagh K, Laurent GJ, McAnulty RJ, Chambers RC. Thrombin stimulates smooth muscle cell procollagen synthesis and mRNA levels via a PAR-1 mediated mechanism. Thromb Haemostas 1998;79:405-409.
11. Damiano BP, Mitchell JM, Giardino EG, et al. Antiplatelet and antithrombotic activity of RWJ-53308, a novel orally active glycoprotein IIb/IIIa antagonist. Thromb Res 2001;104:113-126.
12. Derian CK, Santulli RJ, Tomko KA, Haertlein BJ, Andrade-Gordon P. Species differences in platelet responses to thrombin and SFLLRN. Receptor-mediated calcium mobilization and aggregation, and regulation by protein kinases. Thromb Res 1995;78:505-519.
13. Derian CK, Damiano BP, D'Andrea MR, Andrade-Gordon P. Thrombin regulation of cell function through protease-activated receptors: Implications for therapeutic intervention. Biokhimiya [in Russian] 2002;67:56-64.
14. 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.
15. Derian CK, Maryanoff BE, Andrade-Gordon P, Zhang H-C. Design and evaluation of potent peptide-mimetic PAR-1 Antagonists. Drug Dev Res 2003;51:1-12.
16. Derian CK, Maryanoff BE, Zhang HC, Andrade-Gordon P. Therapeutic potential of protease-activated receptor-1 antagonists. Exp Opin Invest Drugs 2003;12:209-221.
17. Dugina TN, Kiseleva EV, Chistov IV, Umarova BA, Strukova SM. Receptors of the PAR family as a link between blood coagulation and inflammation. Biokhimiya [in Russian] 2002;67:65-74.
18. Emori T, Hirata Y, Imai T, et al. Cellular mechanism of thrombin on endothelin-1 biosynthesis and release in bovine endothelial cell. Biochem Pharmacol 1992;44:2409-2411.
19. Fiorucci S, Distrutti E. Role of PAR2 in pain and inflammation. Trends Pharmacol Sci 2002;23:153-155.
20. 2+ mobilization, barrier dysfunction, prostaglandin synthesis, and platelet-derived growth factor messenger RNA expression in cultured endothelium. J Cell Physiol 1993;156:541-549.
21. Ishihara H, Connolly AJ, Zeng D, et al. Protease-activated receptor 3 is a second thrombin receptor in humans. Nature (London) 1997;386:502-506.
22. Kahn ML, Zheng Y-W, Huang W, et al. A dual thrombin receptor system for platelet activation. Nature (London) 1998;394:690-694.
23. 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.
24. Kranzhoefer R, Clinton SK, Ishii K, Coughlin SR, Fenton JW, II, Libby P. Thrombin potently stimulates cytokine production in human vascular smooth muscle cells but not in mononuclear phagocytes. Circ Res 1996;79:286-294.
25. Ku DD, Zaleski JK. Receptor mechanism of thrombin-induced endothelium-dependent and endothelium-independent coronary vascular effects in dogs. J Cardiovasc Pharmacol 1993;22:609-616.
26. Malik AB, Fenton JW, II. Thrombin-mediated increase in vascular endothelial permeability. Sem Thromb Hemostas 1992;18:193-199.
27. McNamara CA, Sarembock IJ, Gimple LW, Fenton JW, II, Coughlin SR, Owens GK. Thrombin stimulates proliferation of cultured rat aortic smooth muscle cells by a proteolytically activated receptor. J Clin Invest 1993;91:94-98.
28. Molino M, Woolkalis MJ, Reavey-Cantwell J, et al. Endothelial cell thrombin receptors and PAR-2. Two protease-activated receptors located in a single cellular environment. J Biol Chem 1997;272:11133-11141.
29. Muramatsu I, Laniyonu A, Moore GJ, Hollenberg MD. Vascular actions of thrombin receptor peptide. Can J Physiol Pharmacol 1992;70:996-1003.
30. Nakanishi-Matsui M, Zheng Y-W, Sulciner DJ, Weiss EJ, Ludeman MJ, Coughlin SR. PAR3 is a cofactor for PAR4 activation by thrombin. Nature (London) 2000;404:609-613.
31. Nystedt S, Emilsson K, Wahlestedt C, Sundelin J. Molecular cloning of a potential proteinase activated receptor. Proc Natl Acad Sci USA 1994;91:9208-9212.
32. Shankar R, de la Motte CA, Poptic EJ, DiCorleto PE. Thrombin receptor-activating peptides differentially stimulate platelet-derived growth factor production, monocytic cell adhesion, and E-selectin expression in human umbilical vein endothelial cells. J Biol Chem 1994;269:13936-13941.
33. Storck J, Kusters B, Zimmermann ER. The tethered ligand receptor is the responsible receptor for the thrombin induced release of von Willebrand factor from endothelial cells (HUVEC). Thromb Res 1995;77:249-258.
34. Takada M, Tanaka H, Yamada T, et al. Antibody to thrombin receptor inhibits neointimal smooth muscle cell accumulation without causing inhibition of platelet aggregation or altering hemostatic parameters after angioplasty in rat. Circ Res 1998;82:980-987.
35. Takiguchi Y, Wada K, Nakashima M. Arterial thrombosis model with photochemical reaction in guinea-pig and its property. Thromb Res 1992;67:435-445.
36. Vu TKH, 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.
37. Wilcox JN, Rodriguez J, Subramanian R, et al. Characterization of thrombin receptor expression during vascular lesion formation. Circ Res 1994;75:1029-1038.
38. Xu W-F, Andersen H, Whitmore TE, et al. Cloning and characterization of human protease-activated receptor 4. Proc Natl Acad Sci USA 1998;95:6642-6646.
39. Zhang H-C, Hoekstra WJ, Maryanoff BE, et al. Novel indole-based peptidomimetics as potent thrombin receptor (PAR-1) antagonists. In: Book of Abstracts. 218th ACS National Meeting. New Orleans. Aug. 22-26; 1999:MEDI-005.
40. Zhang H-C, Derian CK, Andrade-Gordon P, et al. Discovery and optimization of a novel series of thrombin receptor (PAR-1) antagonists: Potent, selective peptide mimetics based on indole and indazole templates. J Med Chem 2001;44:1021-1024.