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Research Article

Patent Update: Inhibitors of Coagulation Factor Xa: From Macromolecular Beginnings to Small Molecules

Pages 1173-1179 | Published online: 03 Mar 2008

References to Primary literature

  • BRUNDISH DE: Thrombin inhibitors. Carr. Opin. Thera. Patents (1992) 2(9):1457–1466.
  • Nurr E, GASIC T, RODKEY J, GASIC GJ, JACOBS JW, FRIEDMAN PA, SIMPSON E: The amino acid sequence of antistasin a po-tent inhibitor of factor Xa reveals repeated internal structure. J. Biol. Chem. (1988) 263:10162–10167.
  • Nurr E, GASIC T, RODKEY J, GASIC GJ, JAcoBs AV, FRIEDMAN PA, SIMPSON E: The amino acid sequence of antistasin. J. Biol. Chem. (1988) 263:10162–10167.
  • DUNWIDDIE CT, THORNBERRY NA, But HG, SARDANA M, FRIEDMAN PA, JAcoss JW, SIMPSON E: Antistasin a leech-derived in-hibitor of factor Xa: kinetic analysis of en-zyme inhibition and identification of the re-active site. J. Biol. Chem. (1989) 264:16694–16699.
  • NUIT EM, JAIN D, LENNY AB, SCHAPI,E,R L, SIEGL PK, DUNWIDDIE CT: Purification and characterization of recombinant antistasin: a leech-derived inhibitor of factor Xa. Arch. Biochem. Biophys. (1991) 285:37–44.
  • DUNWIDDIE CT, VLASUK GP, Nurr EM: The hydrolysis and resynthesis of a single re-active site peptide bond in recombinant antistasin by coagulation factor Xa. Arch. Biochem. Biophys. (1992) 294:647–653.
  • HOFMANN KJ, NUTT EM, DUNWIDDIE CT: Site-directed mutagenesis of the leech-de-rived factor Xa inhibitor antistasin. Prob-ing of the reactive site. Biochem. J. (1992) 287:943–949.
  • VLASUK GP, RANurr D, FlurrA T, DUNWIDDM CT, Nun- EM, SMITH DE, SHEBUSKI RJ: Com-parison of the in vivo anticoagulant prop-erties of standard heparin and the highly selective factor Xa inhibitors antistasin and tick anticoagulant peptide (TAP) in a rab-bit model of venous thrombosis. Thromb. Haemostas. (1991) 65:257–262.
  • MELLOT MJ, HOLAHAN MA, LYNCH JJ, VLASUK GP, DUNWIDDIE CT: Acceleration of recom-binant tissue-type plasminogen activator-in-duced reperfusion and prevention of reoc-elusion by recombinant antistasin, a selec-tive factor Xa inhibitor in a canine model of femoral arterial thrombosis. Circulation Res. (1992) 70:1152–1160.
  • SCHAFFER LW, DAVIDSON JT, VLASUK GP, DUNWIDDIE CT, SIEGL PKS: Selective fac-tor Xa inhibition by recombinant antistasin prevents vascular graft thrombosis in ba-boons. Arteriosclerosis and Thrombosis (1992) 12:879–885.
  • CONDRA C, NUTT E, FETROSKI CJ, SIMPSON E, FRIEDMAN PA, JACOBS JW: Isolation and structural characterisation of a po-tent inhibitor of coagulation factor Xa from the leech Haementeria ghilianii. Thromb. Haemostas (1989) 61:437–441.
  • HOLSTEIN TW, MALA C, KURZ E, BAUER K, GREBER M, DAVID CN: The primitive meta-zoan Hydra expresses antistasin, a serine protease inhibitor of vertebrate blood coag-ulation: cDNA cloning, cellular localisation and developmental regulation. FEBS Lett. (1992) 309:288–292.
  • JORDAN SP, WAXMAN L, SMITH DE, VLASUK GP: Tick anticoagulant peptide: kinetic anal-ysis of the recombinant inhibitor with blood coagulation factor Xa. Biochemistry (1990) 29:11095–11100.
  • WAXMAN L, SMITH DE, ARCURI ICE, VLASUK GP: Tick anticoagulant peptide (TAP) is a novel inhibitor of blood coagulation factor Xa. Science (1990) 248:593–596.
  • SARDANA M, SARDANA V. RODKEY J, WOOD T, NG A, VLASUK GP, WAXMAN L: Determi-nation of disulphide bond pairs and stability in recombinant tick anticoagulant peptide. J. Biol. Chem. (1991) 266:13560–13563.
  • NEEPER MP, WAXMAN L, SMITH DE, SCHULMAN CA, SARDANA M, ELLIS RW, SCHAFFER RW, SIEGL PKS, VLASUK GP: Characterization of recombinant tick anticoagulant peptide, a highly selective inhibitor of blood co-agulation factor Xa. J. Biol. Chem. (1990) 265:17746–17752.
  • JORDAN SP, MAO S-S, LEWIS SD, SHAFER JA: Reaction pathway for inhibition of blood co-agulation factor Xa by tick anticoagulant peptide. Biochemistry (1992) 31:5374–1380.
  • DUNWIDDM CT, NEEPER MP, Nun. EM, WAXMAN L, SMITH DE, HOFMANN KJ, LUMMA PK, GARSKY VM, VLASUK GP: Site-directed analysis of the functional domains in fac-tor Xa inhibitor tick anticoagulant peptide: identification of two distinct regions that constitute the enzyme recognition sites. Bio-chemistry (1992) 31:12126–12131.
  • SCHAFFER LW, DAVIDSON JT, VLASUK GP, SIEGL PKS: Antithrombotic efficacy of re-combinant tick anticoagulant peptide, a po-tent inhibitor of coagulation factor Xa in a primate model of arterial thrombosis. Circu-lation (1991) 84:1741–1748.
  • SITKO GR, RAMJIT DR, STABILITO II, LEHMAN D, LYNCH JJ, VLASUK GP: Conjunctive en-hancement of enzymatic thrombolysis and prevention of thrombotic reocclusion withthe selective factor Xa inhibitor, tick antico-agulant peptide. Comparison to hirudin and heparin in a canine model of acute coronary artery thrombosis. Circulation (1992) 85:805–815.
  • DUNWIDDM CT, Nun EM, VLASUK GP, SIEGL PKS, SCHAH±R LW: Anticoagulant efficacy and immunogenicity of the selective factor Xa inhibitor antistasin following subcuta-neous administration in the rhesus monkey. Thromb. Haemostas. (1992) 67:371–376.
  • STORZEBECHER J, MARKWARDT F, WALSMANN P: Synthetic inhibitors of serine proteases XIV Inhibition of factor Xa by derivatives of benzamidine. Thromb. Res. (1976) 9:637–646.
  • STURZEBECHER J, STÜRZEBECHER U: Are fac-tor Xa inhibitors superior to thrombin in-hibitors in anticoagulation. Folia Haematol. (1988) 115:S152–S156.
  • STÜRZEBECHER J, STURZEBECHER U, VIEWEG H, WAGNER G, HAUPTMANN J, MARKWARDT F: Synthetic inhibitors of bovine factor Xa and thrombin comparision of their antico-agulant efficacy. Thromb. Res. (1989) 54:245–252.
  • TIDWELL RR, WEBSTER WP, SHAVER SR, GERATZ JD: Strategies for anticoagulation with synthetic protease inhibitors. Xa in-hibitors versus thrombin inhibitors. Thromb. Res. (1980) 19:339–349.
  • YOKOYAMA T, FUJI' S: New synthetic in-hibitors of chymotrypsin, trypsin, throm-bin, plasmin, urikinase, tissue plasminogen activator, factor Xa, tissue kallikrein and plasma kallikrein. Jap. J. Clin. Chem. (1986) 15:338–344.

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