Therapeutic potential of protease-activated receptor-1 antagonists

Bibliography

• YUSUF S, REDDY S, OUNPUU S, ANAND S: Global burden of cardiovascular diseases: Part I: General considerations, the epidemiologic transition, risk factors, and impact of urbanization. Circulation (2001) 104:2746–2753.
   PubMed Web of Science ®Google Scholar
• •This two-part article provides an excellent summary on the epidemiology of cardiovascular disease.
   Google Scholar
• YUSUF S, REDDY S, OUNPUU S, ANAND S: Global burden of cardiovascular diseases: Part II: Variations in cardiovascular disease by specific ethnic groups and geographic regions and prevention strategies. Circulation (2001) 104:2855–2864.
   PubMed Web of Science ®Google Scholar
• •This two-part article provides an excellent summary on the epidemiology of cardiovascular disease.
   Google Scholar
• CHESEBRO JH, WEBSTER MW, ZOLDHELYI P, ROCHE PC, BADIMON L, BADIMON JJ: Antithrombotic therapy and progression of coronary artery disease. Antiplatelet versus antithrombins. Circulation (1992) 86:111100–111110.
   Google Scholar
• TURPIE AGG: Clinical potential of antithrombotic drugs in coronary syndromes. Am. j Cordial (1998) 82:11E–14E.
   Google Scholar
• WEITZ JI, BULLER HR: Direct thrombininhibitors in acute coronary syndromes: Present and future. Circulation (2002) 105:1004–1011.
   PubMed Web of Science ®Google Scholar
• MACFARLANE SR, SEATTER MJ, KANKE T, HUNTER GD, PLEVIN R: Proteinase-activated receptors. Pharmacol Rev. (2001) 53:245–282.
   PubMed Web of Science ®Google Scholar
• ••A comprehensive review on protease-activated receptors.
   Google Scholar
• VERGNOLLE N, WALLACE JL, BUNNETT NW HOLLENBERG MD: Protease-activated receptors in inflammation, neuronal signaling and pain. Trends Pharmacol Li. (2001) 22:146–152.
   PubMed Web of Science ®Google Scholar
• •A timely review on the role of PARS in inflammation.
   Google Scholar
• DERIAN CK, DAMIANO BP, D'ANDREA MR, ANDRADE-GORDON P: Thrombin regulation of cell function through protease-activated receptors: Implications for therapeutic intervention. Biochemistry Wloscow) (2002) 67:56–64.
   PubMed Web of Science ®Google Scholar
• HOLLENBERG MD, COMPTON SJ: International Union of Pharmacology. XXVIII. Proteinase-activated receptors. Pharmacol Rev (2002) 54:203–217.
   Google Scholar
• 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.
   PubMed Web of Science ®Google Scholar
• ••The original publication describing thehuman thrombin receptor PAR-1.
   Google Scholar
• RASMUSSEN UB, VOURET-CRAVIARI V, JALLAT S et al: cDNA cloning and expression of a hamster a-thrombin receptor coupled to calcium mobilization. FEBS Lett. (1991) 288:123–128.
   PubMed Web of Science ®Google Scholar
• ZHONG C, HAYZER DJ, CORSON MA, RUNGE MS: Molecular cloning of the rat vascular smooth muscle thrombin receptor. Evidence for in vitro regulation by basic fibroblast growth factor. I Biol. Chem. (1992) 267:16975–16979.
   Google Scholar
• NANEVICZ T, ISHII M, WANG L etal.: Mechanisms of thrombin receptor agonist specificity. Chimeric receptors and complementary mutations identify an agonist recognition site. I Biol. Chem. (1995) 270:21619–21625.
   Google Scholar
• BEAVERS MP, MARYANOFF BE, NGUYEN D, BLACKHART BD: A theoretical model of the human thrombin receptor (PAR-1), the first known protease-activated G-protein-coupled receptor. Adv. Med. Chem. (1999) 4:245–271.
   Google Scholar
• BLACKHART BD, RUSLIM-LITRUS L, LU C-C et al: Extracellular mutations of protease-activated receptor-1 result in differential activation by thrombin and thrombin receptor agonist peptide. Mal Pharmacol (2000) 58:1178–1187.
   PubMed Web of Science ®Google Scholar
• HAMMES SR, SHAPIRO MJ, COUGHLIN SR: Shutoff and agonist-triggered internalization of protease-activated receptor 1 can be separated by mutation of putative phosphorylation sites in the cytoplasmic tail. Biochemistry (1999) 38:9308–9316.
   PubMed Web of Science ®Google Scholar
• TREJO J, ALTSCHULER Y, FU H-W, MOSTOV KE, COUGHLIN SR: Protease-activated receptor-I down-regulation. A mutant HeLa cell line suggests novel requirements for PAR1 phosphorylation and recruitment to clathrin-coated pits. _J. Biol. Chem. (2000) 275:31255–31265.
   Google Scholar
• NYSTEDT S, EMILSSON K, WAHLESTEDT C, SUNDELIN J: Molecular cloning of a potential proteinase activated receptor. Proc. Nail. Acad. Sci. USA (1994) 91:9208–9212.
   PubMed Web of Science ®Google Scholar
• ••The original publication describing thecloning of murine PAR-2.
   Google Scholar
• NYSTEDT S, EMILSSON K, LARSSON A-K, STROEMBECK B, SUNDELIN J: Molecular cloning and functional expression of the gene encoding the human proteinase-activated receptor 2. Eur. Biochem. (1995) 232:84–89.
   PubMedGoogle Scholar
• •The original publication describing the cloning of human PAR-2.
   Google Scholar
• BOHM SK, KONG W BROMME D et al.: Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2. Biochem. (1996) 314:1009–1016.
   Google Scholar
• ISHIHARA H, CONNOLLY AJ, ZENG D et al.: Protease-activated receptor 3 is a second thrombin receptor in humans. Nature (1997) 386:502–506.
   PubMed Web of Science ®Google Scholar
• ••The original paper describing theidentification of PAR-3.
   Google Scholar
• KAHN ML, ZHENG Y-W HUANG W et al.: A dual thrombin receptor system for platelet activation. Nature (1998) 394:690–694.
   Google Scholar
• ••One of the two papers describing theidentification of human PAR-4.
   Google Scholar
• XU WF, ANDERSEN H, WHITMORE TE et al.: Cloning and characterization of human protease-activated receptor 4. Proc. Nail. Acad. Sci. USA (1998) 95:6642–6646.
   PubMed Web of Science ®Google Scholar
• ••One of the two papers describing theidentification of human PAR-4.
   Google Scholar
• BLACKHART BD, EMILSSON K, NGUYEN D et al: Ligand cross-reactivity within the protease-activated receptor family. j Biol. Chem. (1996) 271:16466–16471.
   PubMed Web of Science ®Google Scholar
• NISHIKAWA H, KAWABATA A, KAWAI K, KURODA R: Guinea pig platelets do not respond to GYPGKF, a protease-activated receptor-4-activating peptide: A property distinct from human platelets. Blood Coagulation Fibnnolysis (2000) 11:111–113.
   PubMed Web of Science ®Google Scholar
• 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.
   PubMed Web of Science ®Google Scholar
• ••This paper demonstrates that inhibition ofPAR-1 with a peptide-mimetic antagonist prevents restenosis.
   Google Scholar
• MIRZA H, SCHMIDT VA, DERIAN CK, JESTY J, BAHOU WF: Mitogenic responses mediated through the proteinase-activated receptor-2 are induced by expressed forms of mast cell a- or 13-tryptases. Blood(1997) 90:3914–3922.
   PubMed Web of Science ®Google Scholar
• CORVERA CU, DERY O, MCCONALOGUE K etal.: Mast cell tryptase regulates rat colonic myocytes through proteinase-activated receptor 2.1 Clin. Invest. (1997) 100:1383–1393.
   Google Scholar
• KAHN ML, NAKANISHI-MATSUI M, SHAPIRO MJ, ISHIHARA H, COUGHLIN SR: Protease-activated receptors 1 and 4 mediate activation of human platelets by thrombin. I OM. Invest. (1999) 103:879–887.
   PubMed Web of Science ®Google Scholar
• 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 (1996) 381:516–519.
   PubMed Web of Science ®Google Scholar
• ••This paper describes the generation ofPAR-1-deficient mice.
   Google Scholar
• DARROW AL, FUNG-LEUNG WE YE RD et al.: Biological consequences of thrombin receptor deficiency in mice. Thromb. Haemostasis (1996) 76:860–866.
   PubMed Web of Science ®Google Scholar
• ••This paper describes the generation of PAR-1-deficient mice.
   Google Scholar
• GRIFFIN CT, SRINIVASAN Y, ZHENG Y-W, HUANG W, COUGHLIN SR: A role for thrombin receptor signaling in endothelial cells during embryonic development. Science (2001) 293:1666–1670.
   PubMed Web of Science ®Google Scholar
• SCHMIDT VA, NIERMAN WC, MAGLOTT DR et al.: The human proteinase-activated receptor-3 (PAR-3) gene. Identification within a PAR gene cluster and characterization in vascular endothelial cells and platelets. I Biol. Chem. (1998) 273:15061–15068.
   Google Scholar
• NAKANISHI-MATSUI M, ZHENG Y-W, SULCINER DJ, WEISS EJ, LUDEMAN MJ, COUGHLIN SR: PAR3 is a cofactor for PAR4 activation by thrombin. Nature (2000) 404:609–613.
   PubMed Web of Science ®Google Scholar
• ••This paper describes the cofactorrelationship of PAR-3 and PAR–4.
   Google Scholar
• 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.
   PubMed Web of Science ®Google Scholar
• ••This paper demonstrates the antithrombotic effect of PAR-4 deficiency.
   Google Scholar
• GARCIA JGN: Molecular mechanisms ofthrombin-induced human and bovine endothelial cell activation. I Lab. Clin. Med. (1992) 120:513–519.
   PubMedGoogle Scholar
• LUM H, ANDERSEN TT, SIFLINGER-BIRNBOIM A etal.: Thrombin receptor peptide inhibits thrombin-induced increase in endothelial permeability by receptor desensitization. 1 Cell Biol. (1993) 120:1491–1499.
   Google Scholar
• SUGAMA Y, TIRUPPATHI C, JANAKIDEVI K, ANDERSEN TT, FENTON JW 2nd, MALIK AB: Thrombin-induced expression of endothelial P-selectin and intercellular adhesion molecule-1: A mechanism for stabilizing neutrophil adhesion. I Cell Biol. (1992) 119:935–944.
   Web of Science ®Google Scholar
• SHANKAR R, DE LA MOTTE CA, DICORLETO PE: 3-Deazaadenosine inhibits thrombin-stimulated platelet-derived growth factor production and endothelial-leukocyte adhesion molecule-I-mediated monocytic cell adhesion in human aortic endothelial cells. 1 Biol. Chem. (1992) 267:9376–9382.
   Google Scholar
• TSOPANOGLOU NE, PIPILI-SYNETOS E, MARAGOUDAKIS ME: Thrombin promotes angiogenesis by a mechanism independent of fibrin formation. Am. I Physiol. (1993) 264:C1302–C1307.
   PubMed Web of Science ®Google Scholar
• HARALABOPOULOS GC, GRANT DS, KLEINMAN HK, MARAGOUDAKIS ME: Thrombin promotes endothelial cell alignment in matrigel in vitro and angiogenesis in vivo. Am. I Physiol. (1997) 273:C239–C245.
   PubMed Web of Science ®Google Scholar
• COLOTTA F, SCIACCA FL, SIRONI M, LUINI W, RABIET MJ, MANTOVANI A: Expression of monocyte chemotactic protein-1 by monocytes and endothelial cells exposed to thrombin. Am. I Pathol. (1994) 144:975–985.
   PubMed Web of Science ®Google Scholar
• CHI L, LI Y, STEHNO-BITTEL L et al.: Interleukin-6 production by endothelial cells via stimulation of protease-activated receptors is amplified by endotoxin and tumor necrosis factor-alpha. I Interferon Cytokine Res. (2001) 21:231–240.
   PubMed Web of Science ®Google Scholar
• KU DD, ZALESKI JK: Receptor mechanism of thrombin-induced endothelium-dependent and endothelium-independent coronary vascular effects in dogs. I Cardiovasc. Pharmacol. (1993) 22:609–616.
   PubMed Web of Science ®Google Scholar
• 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.
   PubMed Web of Science ®Google Scholar
• GARCIA JGN, PATTERSON C, BAHLER C, ASCHNER J, HART CM, ENGLISH D: Thrombin receptor activating peptides induce calcium mobilization, barrier dysfunction, prostaglandin synthesis, and platelet-derived growth factor mRNA expression in cultured endothelium. I Cell. Physiol. (1993) 156:541–549.
   PubMed Web of Science ®Google Scholar
• O'BRIEN PJ, PREVOST N, MOLINO Meta].: Thrombin responses in human endothelial cells. Contributions from receptors other than PAR1 include the transactivation of PAR2 by thrombin-cleaved PAR1.1 Biol. Chem. (2000) 275:13502–13509.
   Google Scholar
• HAMILTON JR, FRAUMAN AG, COCKS TM: Increased expression of protease-activated receptor-2 (PAR2) and PAR4 in human coronary artery by inflammatory stimuli unveils endothelium-dependent relaxations to PAR2 and PAR4 agonists. Circ. Res. (2001) 89:92–98.
   PubMed Web of Science ®Google Scholar
• •This paper describes a functional PAR-4 on vascular endothelium.
   Google Scholar
• STOUFFER GA, SAREMBOCK IJ, MCNAMARA CA, GIMPLE LW, OWENS GK: Thrombin-induced mitogenesis of vascular SMC is partially mediated by autocrine production of PDGF-AA. Am. I Physiol. (1993) 265:C806–C811.
   PubMed Web of Science ®Google Scholar
• STOUFFER GA, RUN GE MS: The role of secondary growth factor production in thrombin-induced proliferation of vascular smooth muscle cells. Semirr. Thromb. Hemostasis (1998) 24:145–150.
   PubMed Web of Science ®Google Scholar
• GALIS ZS, KRANZHOFER R, FENTON JW 2nd, LIBBY P: Thrombin promotes activation of matrix metalloproteinase-2 produced by cultured vascular smooth muscle cells. Arterioscler. Thromb. Vasc. Biol. (1997) 17:483–489.
   PubMed Web of Science ®Google Scholar
• ABBAGH K, LAURENT GJ, MCANULTY RJ, CHAMBERS RC: Thrombin stimulates smooth muscle cell procollagen synthesis and mRNA levels via a PAR-1 mediated mechanism. Thromb. Haemostasis (1998) 79:405–409.
   PubMed Web of Science ®Google Scholar
• 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. Nati Acad. Sri. USA (1999) 96:12257–12262.
   PubMed Web of Science ®Google Scholar
• ••This paper describes the development and characterisation of a selective peptide mimetic PAR-1 antagonist.
   Google Scholar
• AHN HS, FOSTER C, BOYKOW G, STAMFORD A, MANNA M, GRAZIANO M: Inhibition of cellular action of thrombin by N3-cyclopropy1-7-{[4-(1-methylethyl)phenyllmethy11-7H-pyrrolo [3, 2-f] quinazoline-1,3-diamine (SCH 79797), a nonpeptide thrombin receptor antagonist. Biochem. Pharmacol. (2000) 60:1425–1434.
   PubMed Web of Science ®Google Scholar
• MURAMATSU I, LANIYONU A, MOORE GJ, HOLLENBERG MD: Vascular actions of thrombin receptor peptide. Carr. J Physiol. Pharmacol. (1992) 70:996–1003.
   PubMed Web of Science ®Google Scholar
• ANTONACCIO MJ, NORMANDIN D, SERAFINO R, MORELAND S: Effects of thrombin and thrombin receptor activating peptides on rat aortic vascular smooth muscle. j Pharmacol. Esp. Ther. (1993) 266:125–132.
   PubMed Web of Science ®Google Scholar
• CHEUNG W-M, ANDRADE-GORDON P, DERIAN CK, DAMIANO BP: Receptor-activating peptides distinguish thrombin receptor (PAR-1) and protease activated receptor 2 (PAR-2) mediated hemodynamic responses in vivo. Can. Physiol. Pharmacol. (1998) 76:16–25.
   PubMed Web of Science ®Google Scholar
• GLEMBOTSKI CC, IRONS CE, KROWN KA, MURRAY SE SPRENKLE AB, SET CA: Myocardial a-thrombin receptor activation induces hypertrophy and increases atrial natriuretic factor gene expression. j Biol. Chem. (1993) 268:20646–20652.
   PubMed Web of Science ®Google Scholar
• JIANG T, KUZNETSOV V, PAK E, ZHANG H, ROBINSON RB, STEINBERG SF: Thrombin receptor actions in neonatal rat ventricular myocytes. Circ. Res. (1996) 78:553–563.
   PubMed Web of Science ®Google Scholar
• SABRI A, MUSKE G, ZHANG H et al.: Signaling properties and functions of two distinct cardiomyocyte protease-activated receptors. Circ. Res. (2000) 86:1054–1061.
   PubMed Web of Science ®Google Scholar
• KU DD: Unmasking of thrombin vasoconstriction in isolated perfused dog hearts after intracoronary infusion of air embolus. j Pharmacol. Exp. Ther. (1987) 243:571–576.
   PubMed Web of Science ®Google Scholar
• DAMIANO BP, MITCHELL JA, CHEUNG W-M, FALOTICO R: Activation of vascular thrombin receptors mediates cardiac response to alpha-thrombin in isolated, perfused guinea pig heart. Am. J Physiol. (1996) 270:H1585–H1596.
   PubMed Web of Science ®Google Scholar
• RAZIN E, MARX G: Thrombin-induced degranulation of cultured bone marrow-derived mast cells. j Immurrol. (1984) 133:3282–3285.
   Web of Science ®Google Scholar
• STRUKOVA SM, DUGINA TN, KHLGATIAN SV, REDKOZUBOV AE, REDKOZUBOVA GP, PINELIS VG: Thrombin-mediated events implicated in mast cell activation. Sem. Thromb. Hemostasis (1996) 22:145–150.
   PubMed Web of Science ®Google Scholar
• HE S, WALLS AF: Human mast cell tryptase: A stimulus of microvascular leakage and mast cell activation. Eur. Pharmacol. (1997) 328:89–97.
   PubMed Web of Science ®Google Scholar
• GALLI SJ: Mast cells and basophils. Curr. Opin. Hematol. (2000) 7:32–39.
   PubMed Web of Science ®Google Scholar
• D'ANDREA MR, ROGAHN CJ, ANDRADE-GORDON P: Localization of protease-activated receptors -1 and -2 in human mast cells: Indications for an amplified mast cell degranulation cascade. Biotech. Histochem. (2000) 75:85–90.
   PubMed Web of Science ®Google Scholar
• HOFFMAN M, COOPER ST: Thrombin enhances monocyte secretion of tumor necrosis factor and interleukin-1 beta by two distinct mechanisms. Blood Cells Ma. Dis. (1995) 21:156–167.
   PubMed Web of Science ®Google Scholar
• TORDAI A, FENTON JW, II, ANDERSEN T, GELFAND EW: Functional thrombin receptors on human T lymphoblastoid cells. I Immurrol. (1993) 150:4876–4886.
   Google Scholar
• JOYCE DE, CHEN Y, ERGER RA, KORETZKY GA, LENTZ SR: Functional interactions between the thrombin receptor and the T-cell antigen receptor in human T-cell lines. Blood (1997) 90:1893–1901.
   PubMed Web of Science ®Google Scholar
• DAMIANO BP, CHEUNG W-M, MITCHELL JA, FALOTICO R: Cardiovascular actions of thrombin receptor activation in vivo. I Pharmacol. Exp. Ther. (1996) 279:1365–1378.
   PubMed Web of Science ®Google Scholar
• WILCOX JN, RODRIGUEZ J, SUBRAMANIAN R et al.: Characterization of thrombin receptor expression during vascular lesion formation. Circ. Res. (1994) 75:1029–1038.
   PubMed Web of Science ®Google Scholar
• GUITTENY A-F, HERBERT J-M: Failureof heparin to inhibit the expression of the thrombin receptor following endothelial injury of the rabbit carotid artery. Eur. Pharmacol. (1997) 327:157–162.
   PubMed Web of Science ®Google Scholar
• 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. Vase. Biol. (1999) 19:3014-3024. This paper demonstrates inhibition of restenosis in PAR-1-deficient mice.
   Google Scholar
• CIRINO G, CICALA C, BUCCI MR, SORRENTINO L, MARAGANORE JM, STONE SR: Thrombin functions as an inflammatory mediator through activation of its receptor. I Exp. Med. (1996) 183:821–827.
   PubMed Web of Science ®Google Scholar
• VERGNOLLE N, HOLLENBERG MD, WALLACE JL: Pro- and anti-inflammatory actions of thrombin: A distinct role for proteinase-activated receptor-1 (PAR1). Br. Pharmacol. (1999) 126:1262–1268.
   PubMed Web of Science ®Google Scholar
• DE GARAVILLA L, VERGNOLLE N, YOUNG SH et al.: Agonists of proteinase-activated receptor 1 induce plasma extravasation by a neurogenic mechanism. Br j Pharmacol. (2001) 133:975–987.
   PubMed Web of Science ®Google Scholar
• •This paper demonstrates anti-inflammatory effects of PAR-1 deficiency in mice.
   Google Scholar
• WEISS EJ, HAMILTON JR, LEASE KE, COUGHLIN SR: Protection against thrombosis in mice lacking PAR3. Blood (2002) 100:3240–3244.
   PubMed Web of Science ®Google Scholar
• ••This paper demonstrates the antithrombotic effect of PAR-3 deficiency in mice.
   Google Scholar
• AHN H-S, CHACKALAMANNIL S: Nonpeptide thrombin receptor antagonists. Drugs Future (2001) 26:1065–1085.
   Web of Science ®Google Scholar
• ••A comprehensive review of thedevelopment of PAR-1 antagonists.
   Google Scholar
• ANDERLUH M, DOLENC MS: Thrombin receptor antagonists; recent advances in PAR-1 antagonist development. Curr. Med. Chem. (2002) 9:1229–1250.
   PubMed Web of Science ®Google Scholar
• ••An updated review of the development ofPAR-1 antagonists.
   Google Scholar
• FURMAN MI, LIU L, BENOIT SE, BECKER RC, BARNARD MR, MICHELSON AD: The cleaved peptide of the thrombin receptor is a strong platelet agonist. Proc. Nati Acad. Sci. USA (1998) 95:3082–3087.
   PubMed Web of Science ®Google Scholar
• HASAN AAK, AMENTA S, SCHMAIER AH: Bradykinin and its metabolite, Arg-Pro-Pro-Gly-Phe, are selective inhibitors of a-thrombin-induced platelet activation. Circulation (1996) 94:517–528.
   PubMed Web of Science ®Google Scholar
• HASAN AAK, REBELLO SS, SMITH E et al.: Thrombostatin inhibits induced canine coronary thrombosis. Thromb. Haemostasis (1999) 82:1182–1187.
   PubMed Web of Science ®Google Scholar
• CONNOLLY TM, CONDRA C, FENG D-M etal.: Species variability in platelet and other cellular responsiveness to thrombin receptor-derived peptides. Thromb. Haemostasis (1994) 72:627–633.
   Google Scholar
• •This paper describes the species variation in functional PAR-1 expression.
   Google Scholar
• 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.
   Google Scholar
• •This paper describes the species variation in functional PAR-1 expression.
   Google Scholar
• BAHOU WF, COLLER BS, POTTER CL, NORTON KJ, KUTOK JL, GOLIGORSKY MS: The thrombin receptor extracellular domain contains sites crucial for peptide ligand-induced activation. j Chu. Invest. (1993) 91:1405–1413.
   PubMed Web of Science ®Google Scholar
• COOK JJ, SITKO GR, BEDNAR B et al.: An antibody against the exo-site of the cloned thrombin receptor inhibits experimental arterial thrombosis in the African green monkey. Circulation (1995) 91:2961–2971.
   PubMed Web of Science ®Google Scholar
• ••This paper demonstrated that theinhibition of PAR-1 by a blocking antibody diminishes arterial thrombosis.
   Google Scholar
• PAKALA R, LIANG TC, BENEDICT CR: A peptide ligand of the human thrombin receptor antagonizes thrombin receptor activating peptide and alpha-thrombin-induced platelet aggregation. Fibrinolysis Proteolysis (2000) 14:15–21.
   Google Scholar
• BERNATOWICZ MS, KLIMAS CE, HARTL KS, PELUSO M, ALLEGRETTO NJ, SEILER SM: Development of potent thrombin receptor antagonist peptides. Med. Chem. (1996) 39:4879–4887.
   Web of Science ®Google Scholar
• ••This paper describes the development ofpeptide antagonists of PAR-1 based on the agonist peptide sequence SFLLRN.
   Google Scholar
• KAWABATA A, SAIFEDDINE M, AL-ANT B, LEBLOND L, HOLLENBERG MD: Evaluation of proteinase-activated receptor-1 (PAR1) agonists and antagonists using a cultured cell receptor desensitization assay: Activation of PAR2 by PAR 1-targeted ligands. j Pharmacol. Exp. Ther. (1999) 288:358–370.
   PubMed Web of Science ®Google Scholar
• ZHANG HC, 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.
   PubMed Web of Science ®Google Scholar
• ••This paper describes the development ofindole and indazole-based peptide mimetic antagonists of PAR-1.
   Google Scholar
• KATO Y, KITA Y, NISHIO M et al.: In vitro antiplatelet profile of FR171113, a novel non-peptide thrombin receptor antagonist. Eur. j Pharmacol. (1999) 384:197–202.
   PubMed Web of Science ®Google Scholar
• AHN H-S, ARIK L, BOYKOW G etal.: Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists. Bioorg. Med. Chem. Lett. (1999) 9:2073–2078.
   Google Scholar
• ••This paper reports the identification ofnon-peptide PAR-1 antagonists.
   Google Scholar
• CHACKALAMANNIL S, DOLLER D, EAGEN K et al.: Potent, low molecular weight thrombin receptor antagonists. Bioorg. Med. Chem. Lett. (2001) 11:2851–2853.
   PubMed Web of Science ®Google Scholar
• •This paper reports a second series of non-peptide PAR-1 antagonists from Schering-Plough with comparable in vifro inhibitory activity against thrombin and agonist peptide.
   Google Scholar
• BARROW JC, NANTERMET PG, SELNICK HG etal.: Discovery and initial structure-activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists. Bioorg. Med. Chem. Lett. (2001) 11:2691–2696.
   Google Scholar
• •This paper reports non-peptide PAR-1 antagonists identified by Merck.
   Google Scholar
• NANTERMET PG, BARROW JC, LUNDELL GF et al.: Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1). Bioorg. Med. Chem. Lett. (2002) 12:319–323.
   PubMed Web of Science ®Google Scholar
• ••This paper describes the identification ofnon-peptide PAR-1 antagonists from Merck with comparable in vitro inhibitory activity against thrombin and agonist peptide.
   Google Scholar
• GILCHRIST A, VANHAUWE JF, LI A, THOMAS TO, VOYNO-YASENETSKAYA T, HAMM HE: Ga minigenes expressing C-terminal peptides serve as specific inhibitors of thrombin-mediated endothelial activation. j Biol. Chem. (2001) 276:25672–25679.
   PubMed Web of Science ®Google Scholar
• COVIC L, GRESSER AL, TALAVERA J, SWIFT S, KULIOPULOS A: Activation and inhibition of G protein-coupled receptors by cell-penetrating membrane-tethered peptides. Proc. Nati Acad. Sri. USA (2002) 99:643–648.
   PubMed Web of Science ®Google Scholar
• ••This paper describes a novel approach toinhibiting GPCR function through targeting of the intracellular/G protein interaction.
   Google Scholar
• DERIAN CK, DAMIANO BP, ADDO MF etal.: Blockade of the thrombin receptor protease-activated receptor-1 (PAR-1) with a small-molecule antagonist prevents thrombus formation and vascular occlusion in non-human primates. I Pharmacol. Exp. Ther. (In Press).
   Google Scholar
• ••This report describes the first in vivoevidence that a small molecule antagonist of PAR-1 is antithrombotic in non-human primates.
   Google Scholar
• HERBERT JM, GUY AF, LAMARCHE I, MARES AM, SAVI P, DOL F: Intimal hyperplasia following vascular injury is not inhibited by an antisense thrombin receptor oligodeoxynucleotide. j Cell. Physiol. (1997) 170:106–114.
   PubMed Web of Science ®Google Scholar
• TAKADA M, TANAKA H, YAMADA T etal.: 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.
   Google Scholar