Antithrombotic efficacy in the guinea pig of a derivative of human protein C with enhanced activation by thrombin

Blood

Volumn 89, Issue 2, 1997, Pages 534-540

  Kurz, Ken D ^a   Smith, Tommy ^a   Wilson, Alexander ^a   Gerlitz, Bruce ^a   Richardson, Mark A ^a   Grinnell, Brian W ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACTIVATED PROTEIN C; ANTICOAGULANT AGENT; ENZYME PRECURSOR; FIBRIN; FLIN Q3; PROTEIN C; PROTEIN DERIVATIVE; RECOMBINANT PROTEIN; SODIUM CHLORIDE; THROMBIN; THROMBOMODULIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTERIOVENOUS SHUNT; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG EFFICACY; GUINEA PIG; INTRAVENOUS DRUG ADMINISTRATION; MALE; NONHUMAN; PARTIAL THROMBOPLASTIN TIME; PRIORITY JOURNAL; THROMBOSIS; THROMBUS;

EID: 0031028066     PISSN: 00064971     EISSN: None     Source Type: Journal    
DOI: 10.1182/blood.v89.2.534     Document Type: Article

References (49)

1. Kisiel W: Human plasma protein C: Isolation, characterization, and mechanism of activation by α-thrombin. J Clin Invest 64:761, 1979
2. Kisiel W, Canfield WM, Erickson LH, Davie EW: Anticoagulant properties of bovine protein C following activation by thrombin. Biochemistry 16:5824, 1977
3. Esmon CT, Owen WG: Identification of an endothelial cell cofactor for thrombin-catalyzed activation of protein C. Proc Natl Acad Sci USA 78:2249, 1981
4. Owen WG, Esmon CT: Functional properties of an endothelial cell cofactor for thrombin-catalyzed activation of protein C. J Biol Chem 256:5532, 1981
5. Esmon NL, Owen WG, Esmon CT: Isolation of a membrane-bound cofactor for thrombin-catalyzed activation of protein C. J Biol Chem 257:859, 1982
6. Esmon NL: Thrombomodulin. Prog Hemost Thromb 9:29, 1989
7. Esmon CT: The roles of protein C and thrombomodulin in the regulation of blood coagulation. J Biol Chem 264:4743, 1989
8. Walker FJ, Sexton PW, Esmon CT: The inhibition of blood coagulation by activated protein C through selective inactivation of activated factor V. Biochem Biophys Acta 571:333, 1979
9. Vehar GA, Davie EW: Preparation and properties of factor VIII: Biochemistry 19:401, 1980
10. Marlar RA, Kleiss AJ, Griffin JH: Mechanism of action of human activated protein C, a thrombin-dependent anticoagulant enzyme. Blood 59:1067, 1982
11. Taylor FB, Chang A, Esmon CT, D'Angelo A, Vigano-D'Angelo S, Blick KE: Protein C prevents the coagulopathic and lethal effects of Escherichia coli infusion in the baboon. J Clin Invest 79:918, 1987
12. Okajima K, Imamura H, Koga S, Inoue M, Takatsuki K, Aoki N: Treatment of patients with disseminated intravascular coagulation by protein C. Am J Hematol 33:277, 1990
13. Dreyfus M, Magny JF, Bridey F, Schwarz HP, Planche C, Dehan M, Tchernia G: Treatment of homozygous protein C deficiency and neonatal purpura fulminans with a purified protein C concentrate. N Engl J Med 325:1565, 1991
14. Busch C, Cancilla P, DeBault L, Goldsmith J, Owen W: Use of endothelium cultured on microcarriers as a model for the microcirculation. Lab Invest 47:498, 1982
15. Seegers WH, Nieff M, Shafer JA: Notes on the absorption of thrombin on fibrin. Science 101:520, 1945
16. Francis CW, Markham RE, Barlow GH, Florack TM, Dobrzynski DM, Marder VJ: Thrombin activity of fibrin thrombi and soluble plasmic derivatives. J Lab Clin Med 102:220, 1983
17. Hogg PJ, Jackson CM: Fibrin monomer protects thrombin from inactivation by heparin-antithrombin III: Implications for heparin efficacy. Biochemistry 86:3619, 1989
18. 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 III independent inhibitors. J Clin Invest 86:385, 1990
19. Ofosu F, Agnelli G, Hirsh J: New thrombin inhibitors: Mode of action, experimental findings and clinical potential. Recent Adv Haematol 6:45, 1991
20. Agnelli G, Renga C, Weitz JI, Nenci GG, Hirsh J: Sustained antithrombotic activity of hirudin after its plasma clearance: Comparison with heparin. Blood 80:960, 1992
21. Gast A, Tschopp TB, Schmid G, Hilpert K, Ackerman J: Inhibition of clot-bound and free (fluid-phase thrombin) by a novel synthetic thrombin inhibitor (Ro 46-6240), recombinant hirudin and heparin in human plasma. Blood Coag Fibrinol 5:879, 1994
22. Gruber A, Griffin JH, Harker LA, Hanson SR: Inhibition of platelet-dependent thrombus formation by human activated protein C in a primate model. Blood 73:639, 1989
23. Gruber A, Hanson SR, Kelly AB, Van BS, Bang N, Griffin JH, Harker LA: Inhibition of thrombus formation by activated recombinant protein C in a primate model of arterial thrombosis. Circulation 82:578, 1990
24. Smirnov MD, Pyzh MV, Borovikov DV, Atorozhilova AN, Dobrovolski AB, Golubych VL, Gratsiansky NA: Low doses of activated protein C delay arterial thrombosis in rats. Thromb Res 57:645, 1990
25. Gruber A, Harker LA, Hanson SR, Kelly AB, Griffin JH: Antithrombotic effects of combining activated protein C and urokinase in nonhuinan primates. Circulation 84:2454, 1991
26. Araki H, Nishi K, Isihara N, Okajima K: Inhibitory effects of activated protein C and heparin on thrombotic arterial occlusion in rat mesenteric arteries. Thromb Res 62:209, 1991
27. Romisch J, Diehl K-H, Reiner G, Paques E-P: Activated protein C: Antithrombotic properties and influence on fibrinolysis in an animal model. Fibrinolysis 5:191, 1991
28. Sakamoto T, Ogawa H, Yasue H, Oda Y, Kitajima S, Tsumoto K, Mizokami H: Prevention of arterial reocclusion after thrombolysis with activated protein C. Comparison with heparin in a canine model of coronary artery thrombosis. Circulation 90:427, 1994
29. Yamashita T, Matsuoka A, Funatsu A, Yamamoto J: The antithrombotic effect of human activated protein C on He-Ne laser-induced thrombosis in rat mesenteric microvessels. Thromb Res 75:33, 1994
30. Arnljots B, Bergqvist D, Dahlback B: Inhibition of microarterial thrombosis by activated protein C in a rabbit model. Thromb Haemost 72:415, 1994
31. Hoogendoorn H, Nesheim ME, Giles AR: A qualitative and quantitative analysis of the activation and inactivation of protein C in vivo in a primate model. Blood 75:2614, 1990
32. Berger H, Kirstein CG, Orthner CL: Pharmacokinetics of activated protein C in guinea pigs. Blood 77:2174, 1991
33. Espana F, Gruber A, Heeb MJ, Hanson SR, Harker LA, Griffin JH: In vivo and in vitro complexes of activated protein C with two inhibitors in baboon. Blood 77:1754, 1991
34. Griffin JH, Evatt B, Zimmerman TS, Kleiss AJ, Wideman C: Deficiency of protein C in congenital thrombotic disease. J Clin Invest 68:1370, 1981
35. Marlar RA: Protein C in thromboembolic disease. Semin Thromb Hemost 11:387, 1985
36. Okajima K, Koga S, Kaji M, Inoue M, Nakagaki T, Funatsu A, Okabe H, Takatsuki K, Aoki N: Effect of protein C on coagulation and fibrinolysis in normal human subjects. Thromb Hemost 63:48, 1990
37. Richardson MA, Gerlitz B, Grinnell BW: Enhancing protein C interaction with thrombin results in a clot-activated anticoagulant. Nature 360:261, 1992
38. Grinnell BW, Walls JD, Gerlitz B, Berg DT, McClure DB, Ehrlich H, Bang NU, Yan SB: Native and modified recombinant human protein C: Function, secretion, and post-translational modifications, in Bruley D, Drohan W (eds): Protein C and Related Anticoagulants. Houston, TX, Gulf Publishing Co, 1990, p 29
39. Yan SCB, Razzano P, Chao YB, Walls JD, Berg DT, McClure DB, Grinnell BW: Characterization and novel purification of recombinant human protein C from three mammalian cell lines. Bio/Technology 8:655, 1990
40. Smith JR, White AM: Fibrin, red cell and platelet interactions in an experimental model of thrombosis. BrJ Pharmacol 77:29, 1982
41. Ashida S, Sakuma K, Abido Y: Antithrombotic effects of ticlopidine, acetylsalicylic acid and dipyridamole in vascular shunt model in rats. Thromb Res 17:663, 1980
42. Grinnell BW, Walls JD, Gerlitz B: Glycosylation of human protein C affects its secretion, processing, functional activities and activation by thrombin. J Biol Chem 226:9778, 1991
43. Gruber A, Griffin JH: Direct detection of activated protein C in blood from human subjects. Blood 79:2340, 1992
44. Lollar P, Owen WG: Clearance of thrombin from circulation in rabbits by high-affinity binding sites on endothelium: Possible role in the inactivation of thrombin by antithrombin III. J Clin Invest 66:1222, 1980
45. Lollar P, MacIntosh SC, Owen WG: Reaction of antithrombin III with thrombin bound to vascular endothelium: Analysis in a recirculating perfused rabbit heart preparation. J Biol Chem 259:4335, 1984
46. Olson ST, Bjork I: Regulation of thrombin activity by antithrombin III and heparin. Semin Thromb Hemost 20:373, 1994
47. Moore KL, Esmon CT, Esmon NL: Tumor necrosis factor leads to the internalization and degradation of thrombomodulin from the surface of bovine aortic endothelial cells in culture. Blood 73:159, 1989
48. Drake TA, Cheng J, Chang A, Taylor FB: Expression of tissue factor, thrombomodulin and E-selectin in baboons with lethal E. coli sepsis. Am J Pathol 142:1458, 1993
49. Esmon CT: The protein C anticoagulant pathway. Arterioscler Thromb 12:135, 1992