Structural and Functional Characterization of Tick Anticoagulant Peptide (TAP): A Potent and Selective Inhibitor of Blood Coagulation Factor Xa

• References

• 1 Hellman K, Hawkins RI. The action of tick extracts on blood coagulation and fibrinolysis. Thromb Diath Haemorrh 1967; 18: 617-625
• 2 Limo MK, Voigt WP, Tumbo-Oeri AG, Njogu RM, Ole-Moi Yoi OK. Purification and characterization of an anticoagulant from the salivary glands of the ixodid tick Rhipicephalus appendiculatus . Exper Parasitol 1991; 72: 418-429
• 3 Waxman L, Connolly TM. Isolation of an inhibitor selective for collagen-stimulated platelet aggregation from the soft tick Ornithodorus moubata . J Biol Chem 1993; 268: 5445-5449
• 4 Waxman L, Smith DE, Arcuri KE, Vlasuk GP. Tick anticoagulant peptide: a highly selective inhibitor of blood coagulation factor Xa. Science 1990; 248: 593-596
• 5 Neeper MP, Waxman L, Smith DE, Schulman CA, Sardana M, Ellis RE, Schaffer LW, Siegal PKS, Vlasuk GP. Characterization of recombinant tick anticoagulant peptide. J Biol Chem 1990; 265: 17746-17752
• 6 Lehman ED, Schaefer TF, Przysiecki CT, Joyce JG, Bailey FJ, Schulman CA, Burke CJ, Ramjit HG, Miller WJ. Large scale purification and characterization of recombinant tick anticoagulant peptide. J Chromatog 1992; 574: 225-235
• 7 Sardana M, Sardana V, Rodkey J, Wood T, Ng A, Vlasuk GP, Wax-man L. Determination of disulfide bond pairs and stability in recombinant tick anticoagulant peptide. J Biol Chem 1991; 266: 13560-13563
• 8 Jordan SP, Waxman L, Smith DE, Vlasuk GP. Tick anticoagulant peptide: kinetic analysis of the recombinant inhibitor with blood coagulation factor Xa. Biochemistry 1990; 29: 11095-11100
• 9 Jordan SP, Mao SS, Lewis SD, Shafer JA. Reaction pathway for inhibition of blood coagulation factor Xa by tick anticoagulant peptide. Biochemistry 1992; 31: 5374-5380
• 10 Rydel TJ, Tulinsky A, Bode W, Huber R. Refined structure of the hirudin-thrombin complex. J Mol Biol 1991; 221: 583-601
• 11 DeCristorfaro R, Fenton JW, DiCera E. Modulation of thrombin-hirudin interaction by specific ion effects. J Mol Biol 1992; 226: 263-269
• 12 Bode W, Huber H. Proteinase-protein inhibitor interaction. Biomed Biochem Acta 1991; 50: 437-446
• 13 Dunwiddie C, Thornberry NA, Bull HG, Sardana M, Friedman PA, Jacobs JW, Simpson E. Antistasin, a leech-derived inhibitor of factor Xa: kinetic analysis of enzyme inhibition and identification of the reactive site. J Biol Chem 1989; 264: 16694-16699
• 14 Dunwiddie CT, Neeper MP, Nutt EM, Waxman L, Smith DE, Hofmann KJ, Lumma PK, Garsky VM, Vlasuk GP. Site-directed analysis of the functional domains in the factor Xa inhibitor tick anticoagulant peptide: identification of two distinct regions that constitute the enzyme recognition sites. Biochemistry 1992; 31: 12126-12131
• 15 Dunwiddie CT, Vlasuk GP, Nutt EM. The hydrolysis and resynthesis of a single reactive site peptide bond in recombinant antistasin by coagulation factor Xa. Arch Biochem Biophys 1992; 294: 647-653
• 16 Laskowski Jr. M, Kato I. Protein inhibitors of proteinases. Ann Rev Biochem 1980; 49: 593-626
• 17 Dunwiddie CT, Smith DE, Nutt EM, Vlasuk GP. Anticoagulant effects of the selective factor Xa inhibitors tick anticoagulant peptide and antistasin in the APTT assay are determined by the relative rate of prothrombinase inhibition. Thromb Res 1991; 64: 787-794
• 18 Mann KG, Nesheim ME, Church WR, Haley P, Krishnaswamy S. Surface-dependent reactions of the vitamin K-dependent enzyme complexes. Blood 1990; 76: 1-16
• 19 Teitel JM, Rosenberg RD. Protection of factor Xa from neutralization by the heparin antithrombin III complex. J Clin Invest 1983; 71: 1383-1391
• 20 Vlasuk GP, Ramjit D, Fujita T, Dunwiddie CT, Nutt EM, Smith DE, Shebuski RJ. Comparison of the in vivo anticoagulant properties of standard heparin and the highly selective factor Xa inhibitors antistasin and tick anticoagulant peptide (rTAP) in a rabbit model of venous thrombosis. Thromb Haemostas 1991; 65: 257-262
• 21 Schaffer LW, Davidson JT, Vlasuk GP, Siegl PKS. Antithrombotic efficacy of recombinant tick anticoagulant peptide. A potent inhibitor of coagulation factor Xa in a primate model of arterial thrombosis. Circulation 1991; 84: 1741-1748
• 22 Kelly AP, Hanson SR, Dunwiddie CT, Harker LA. Safe lasting interruption of arterial thrombosis by transient intravenous administration of tick anticoagulant peptide (TAP). Circulation 1992; 86 (01) 411 (abstr #1639)
• 23 Sitko GR, Ramjit DR, Stabilito II, Lehman D, Lynch JJ, Vlasuk GP. Conjunctive enhancement of enzymatic thrombolysis and prevention of thrombotic reocclusion with the selective factor Xa inhibitor tick anticoagulant peptide: comparison to hirudin and heparin in a canine model of acute coronary thrombosis. Circulation 1992; 85: 805-815
• 24 Dunwiddie CT, Sitko GR, Mellott MJ, Lynch JL. Sustained coronary artery patency following thrombolysis with a selective factor Xa inhibitor compared to hirudin, utilizing a high dose loading/low dose maintainence infusion regimen in a canine model of arterial thrombosis. Circulation 1992; 86 (01) 867 (abstr #3453)
• 25 Mellott MJ, Stranieri MT, Sitko G, Stabilito II, Lynch JJ, Vlasuk GP. Enhancement of recombinant tissue plasminogen activator-induced reperfusion by recombinant tick anticoagulant peptide, a selective factor Xa inhibitor, in a canine model of femoral arterial thrombosis. Fibrinolysis. 1993 in press
• 26 Hauptmann J, Kaiser B, Nowak G, Struzebecher J, Markwardt F. Comparison of the anticoagulant and antithrombotic effects of synthetic thrombin and factor Xa inhibitors. Thromb Haemostas 1990; 63: 220-223
• 27 Hanson SR, Harker LA. Interruption of acute platelet-dependent thrombosis by the synthetic antithrombin D-phenylalanyl-L-prolyl-L-arginylchloromethyl ketone. Proc Natl Acad Sci USA 1988; 85: 3184-3188
• 28 Kelly AB, Marzec UM, Krupski W, Bass A, Cadroy Y, Hanson SR, Harker LA. Hirudin interruption of heparin-resistant arterial thrombus formation in baboons. Blood 1991; 77: 1006-1012
• 29 Jang IK, Gold HK, Ziskind AA, Leinback RC, Fallon JT, Collen D. Prevention of platelet-rich arterial thrombosis by selective thrombin inhibition. Circulation 1990; 81: 219-225
• 30 Gold HK, Torres FW, Garabedian HD, Werner W, Jang IK, Khan A, Hagstrom JN, Yasuda T, Leinbach RC, Newell JB, Bovill EG, Stump DC, Collen D. Evidence for a rebound coagulation phenomenon after cessation of a 4-hour infusion of a specific thrombin inhibitor in patients with unstable angina pectoris. J Am Coll Cardiol. 1993 in press
• 31 Topol EJ, George BS, Kerelakes DJ, Stump DC, Candela RJ, Abbott Smith CW, Aronson L, Pickel A, Boswick JM, Lee KL, Ellis SG, Califf RM. and the TAMI Study Group: A randomized controlled trial of intravenous tissue plasminogen activator and early intravenous heparin in acute myocardial infarction. Circulation 1989; 79: 281-286
• 32 Weitz JI, Hudoba M, Massel D, Maraganore J, Hirsh J. Clot-bound thrombin is protected from inhibition by heparin-antithrombin III but is susceptible to inactivation by antithrombin Ill-dependent inhibitors. J Clin Invest 1990; 86: 385-391