Hirunorms, novel hirudin-like thrombin inhibitors

General Pharmacology

Volumn 30, Issue 4, 1998, Pages 565-568

  Cappiello, Mario ^a   Vilardo, Pier Giuseppe ^a   Del Corso, Antonella ^a   Mura, Umberto ^a  

^a UNIVERSITY OF PISA   (Italy)

Author keywords

Hirudin; Hirunorm; Thrombin; Thrombin inhibitors; Thrombosis

Indexed keywords

HIRUDIN; HIRUGEN; HIRULOG; HIRUNORM; LEPIRUDIN; SYNTHETIC PEPTIDE; THROMBIN; THROMBIN INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL MODEL; CONTROLLED STUDY; DRUG DESIGN; ENZYME INHIBITION; HUMAN; HUMAN CELL; IN VITRO STUDY; NONHUMAN; PRIORITY JOURNAL; SHORT SURVEY; THROMBOCYTE AGGREGATION; THROMBOSIS;

EID: 0032053457     PISSN: 03063623     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0306-3623(97)00306-6     Document Type: Article

References (30)

1. Bar-Shavit R., Eldor A., Vlodavasky I. Binding of thrombin to subendothelial extracellular matrix. protection and expression of functional properties J. Clin. Invest. 84:1989;1096-1104.
2. Bode W., Turk D., Karshikov A. The refined 1.9-Angstrom X-ray crystal structure of D-Phe-Pro-Arg-Chloro-methylketone-inhibited human α-thrombin - structure analysis, overall structure, electrostatic properties, detailed active site geometry, and structure-function relationship. Protein Sci. 1:1992;426-471.
3. Callas D., Fareed J. Comparative pharmacology of site directed antithrombin agents. Implication in drug development. Thromb. Haemostasis. 74:1995;473-481.
4. Cappiello M., Vilardo P. G., Lippi A., Criscuoli M., Del Corso A., Mura U. Kinetics of human thrombin inhibition by two novel peptide inhibitors (hirunorm IV and hirunorm V). Biochem. Pharmacol. 52:1996;1141-1146.
5. Chari S., Chauan V. S. Hirudin-based synthetic peptides as inhibitors of thrombin. Semin. Thromb. Hemostasis. 20:1994;315-318.
6. Cirillo M., Lippi A., Subissi A., Agnelli G., Criscuoli M. Experimental pharmacology of hirunorm. a novel synthetic peptide thrombin inhibitor Thromb. Haemostasis. 76:1996;384-392.
7. Deutsch E., Rao A. K., Colman R. W. Selective thrombin inhibitors. the next generation of anticoagulants JACC. 22:1993;1089-1092.
8. Fenton II J. W., Olson T. A., Zabinski M. P., Wilner G. D. Anion-binding exosite of human α-thrombin and fibrin(ogen) recognition. Biochemistry. 27:1988;7106-7112.
9. Gibaldi M., Wittkowsky A. K. Contemporary use of and future roles for heparin in antithrombotic therapy. J. Clin. Pharmacol. 35:1995;1031-1045.
10. Grutter M. G., Priestle J. P., Rahuel J., Grossenbacher H., Bode W., Hofsteenge J., Stone S. R. Crystal structure of the thrombin-hirudin complex. a novel mode of serine protease inhibition EMBO J. 9:1990;2361-2365.
11. Harker L. A., Hanson S. R., Kelly A. B. Antithrombotic benefits and hemorrhagic risks of direct thrombin antagonists. Thromb. Haemostasis. 74:1995;464-472.
12. Hirsch J. Heparin. N. Engl. J. Med. 324:1991;1565-1574.
13. Johnson P. H. Hirudin. clinical potential of a thrombin inhibitor Annu. Rev. Med. 45:1994;167-177.
14. 2Cl. A selective affinity label for thrombin. Thromb. Res. 14:1979;969-973.
15. 2-[(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl) sulfonyl]-L-arginyl)]-2-piperidinecarboxylic acid. Biochemistry. 23:1984;85-90.
16. Maranagore J. M., Bourdon P., Jablonski J., Ramachandran K. L., Fenton J. W. II. Design and characterization of hirulogs. a novel class of bivalent peptide inhibitors of thrombin Biochemistry. 29:1990;7095-7101.
17. Maranagore J. M., Adelman B. A. Hirulog. a direct thrombin inhibitor for management of acute coronary syndromes Coronary Artery Dis. 7:1996;438-448.
18. Markwardt F. Hirudin. the promising antithrombotic Cardiovasc. Drug Rev. 10:1992;71-87.
19. Markwardt F. The development of hirudin as antithrombotic drug. Thromb. Res. 74:1994;1-23.
20. Morrison J. F. Kinetics of the reversible inhibition of enzyme catalysed reaction by tight-binding inhibitors. Biochim. Biophys. Acta. 185:1969;269-286.
21. Olson S. T., Biörk I. Regulation of thrombin activity by antithrombin and heparin. Semin. Thromb. Hemostasis. 20:1994;373-409.
22. Simoons M. L., Deckers J. W. New directions in anticoagulant and antiplatelet treatment. Br. Heart J. 74:1995;337-340.
23. Skrzypczak-Jankun E., Carperos V. E., Ravichandran K. G., Tulinsky A., Westbrook M., Maranagore J. M. Structure of the hirugen and hirulog 1 complexes of α-thrombin. J. Mol. Biol. 221:1991;1379-1393.
24. Stone S. R., Hofsteenge J. Kinetics of the inhibition of thrombin by hirudin. Biochemistry. 25:1986;4622-4628.
25. Tapparelli C., Metternich R., Ehrhardt C., Cook N. S. Synthetic low-molecular weight thrombin inhibitors. molecular design and pharmacological profile TIPS. 14:1993;366-376.
26. Toschi V., Lettino M., Gallo R., Badimon J. J., Chesebro J. H. Biochemistry and biology of hirudin. Coronary Artery Dis. 7:1996;420-428.
27. Turpie A. G. G., Weitz J. I., Hirsch J. Advances in antithrombotic therapy. novel agents Thromb. Haemostasis. 74:1995;565-571.
28. Weitz J. I. Biological rationale for the therapeutic role of specific antithrombins. Coronary Artery Dis. 7:1996;409-419.
29. Weitz J. I., Hudoba M., Massel D., Maranagore J., Hirsh J. Clot-bound thrombin is protected from inhibition by heparin-antithrombin III but is susceptible to inactivation by antithrombin III-independent inhibitors. J. Clin. Invest. 86:1990;385-391.
30. Witting J. I., Bourdon P., Brezniak D. V., Maranagore J. M., Fenton II J. W. Thrombin-specific inhibition by and slow cleavage of hirulog-1. Biochem. J. 283:1992;737-743.