Substitution of serine or threonine at position 473 of tissue-type plasminogen activator increases its stability in plasma

Thrombosis and Haemostasis

Volumn 75, Issue 1, 1996, Pages 107-112

  Alibhai, Murtaza ^a   Chow, Alice M ^a   Paoni, Nicholas F ^a  

^a GENENTECH INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALPHA 2 ANTIPLASMIN; SERINE; THREONINE; TISSUE PLASMINOGEN ACTIVATOR;

AMINO ACID SUBSTITUTION; ARTICLE; DRUG CLEARANCE; DRUG INACTIVATION; DRUG STABILITY; EMBRYO; HUMAN; HUMAN CELL; PRIORITY JOURNAL;

EID: 0030034664     PISSN: 03406245     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0038-1650229     Document Type: Article

References (41)

1. Pennica D, Holmes WE, Kohr WJ, Harkins RN, Vehar GA, Ward CA, Bennett WF, Yelverton E, Seeburg PH, Heyneker HL, Goeddel DV, Collen D. Cloning and expression of human tissue-type plasminogen activator cDNA in E. coli. Nature 1983; 301: 214-21.
2. Collen D, Topol EJ, Tiefenbrunn AJ, Gold HK, Weisfeldt ML, Sobel BE, Leinback RC, Brinker JA, Ludbrook PA, Yasuda I, Bulkley BH, Robison AK, Hutter AM Jr., Bell WR, Spadard JJJ, Khaw BA, Grossbard EB. Coronary thrombolysis with recombinant human tissue-type plasminogen activator: a prospective, randomized, placebo-controlled trial. Circulation 1984; 70: 1012-7.
3. Topol EJ, Califf RM, George BS, Kereiakes DJ, Lee KL, for the TAMI Study Group. Insight derived from the thrombolysis and angioplasty in myocardial infarction (TAMI) Trials J Am Coll Cardiol 1988; 12: 24A-31A.
4. Stump DC, Calif RM, Topol EJ, Sigmon K, Thornton D, Masek R, Anderson L, Collen D, and the TAMI Study Group. Pharmacodynamics of thrombolysis with recombinant tissue-type plasminogen activator. Correlation with characteristics of and clinical outcomes in patients with acute myocardial infarction. Circulation 1989; 80: 1222-30.
5. The TIMI Study Group. Comparison of invasive and conservative strategies after treatment with intravenous tissue plasminogen activator in acute myocardial infarction: Results of the thrombolysis in myocardial infarction (TIMI) phase II trial. N Engl J Med 1989, 320: 618-27.
6. Goldhaber SZ, Kessler CM, Heit J, Markis J, Sharma GV, Dawley D, Nagel JS, Meyerovitz M, Kim D, Vaughan DE, Parker JA, Tumeh SS, Drum D, Loscalzo J, Reagan K, Selwyn AP, Anderson J, Braunwald E. Randomised controlled trial of recombinant tissue plasminogen activator versus urokinase in the treatment of acute pulmonary embolism. Lancet 1988; 2: 293-8.
7. Parker JA, Markis JE, Palla A, Goldhaber SZ, Royal HD, Tumeh S, Kim D, Rustgi AK, Holman BL, Kolodny GM. Braunwald E. Pulmonary perfusion after rt-PA therapy for acute embolism: Early improvement assessed with segmental perfusion scanning. Radiology 1988; 166: 441-5.
8. Higgins DL, Bennett WF. Tissue plasminogen activator: The biochemistry and pharmacology of variants produced by mutagenesis. Annu Rev Pharmacol Toxicol 1990; 30: 91-121.
9. Lijnen HR, Collen D. Strategies for the improvement of thrombolytic agents. Thromb Haemost 1991; 66: 88-110.
10. Madison EL. Probing structure-function relationships of tissue-type plasminogen activator by site-specific mutagenesis. Fibrinolysis 1994; 8 (Suppl 1): 221-36.
11. Larsen GR, Timony GA, Morgan PG, Barone KM, Henson KS, Angus LB, Stoudemire JB. Protein engineering of novel plasminogen activators with increased thrombolytic potency in rabbits relative to Activase®. J Biol Chem 1991; 266: 8156-61.
12. Martin U, von Mollendorf E, Akpan W, Kientsch-Engel R, Kaufmann B, Neugebauer G. Thrombolysis with an E. coli-produced recombinant plasminogen activator (BM 06.022) in the rabbit model of jugular vein thrombosis. Thromb Haemost 1991; 65: 550-64.
13. Martin U, Fischer S, Kohnert U, Lill H, Rudolph R, Sponer G, Stern A, Strein K. Thrombolytic potency of an E. coli-produced novel variant of rt-PA in dogs. Fibrinolysis 1990; 4 (Suppl 3): 9 (Abstract #26).
14. Wikstrom K, Mattsson C, Sterky C, Pohl G. Tissue plasminogen activator mutants lacking the growth factor domain and the first kringle domain. Fibrinolysis 1991; 5: 31-41.
15. Smith GF, Craft TJ, Quay JF. Pharmacodynamics of modified tissue plasminogen activator LY210825 in the conscious dog as evaluated with immunocapture assays. Fibrinolysis 1993; 7: 264-74.
16. Burck PJ, Berg DH, Warrick MW, Berg DT, Walls JD, Jaskunas SR, Crisel RM, Weigel B, Vlahos CJ, McClure DB, Grinnell BW. Characterization of a modified human plasminogen activator comprising a kringle-2 and a protease domain. J Biol Chem 1990; 265: 5170-7.
17. Jackson CV, Crowe VG, Trelia JC, Sundboom JL, Grinnell BW, Bobbitt JL, Burck PJ, Quay JF, Smith GF. Thrombolytic activity of a novel plasminogen activator, LY210825, compared with recombinant tissue-type plasminogen activator in a canine model of coronary artery thrombosis. Circulation 1990; 82: 930-40.
18. Madison EL, Goldsmith EJ, Gerard RD, Gething M-JK, Sambrook JF. Serpin-resistant mutants of human tissue-type plasminogen activator. Nature 1989; 339: 721-4.
19. Madison EL, Goldsmith EJ, Gething M-JH, Sambrook JF, Gerard RD. Restoration of serine protease-inhibitor interaction by protein engineering. J Biol Chem 1990; 265: 21423-6.
20. Madison EL, Goldsmith EJ, Gerard RD, Gething M-J, Sambrook JF, Bassel-Duby RS. Amino acid residues that affect interaction of tissue-type plasminogen activator with plasminogen activator inhibitor 1 Proc Natl Acad Sci USA 1990; 87: 3530-3.
21. Bennett WF, Paoni NF, Keyt BA, Botstein D, Jones AJS, Presta L, Wurm FM, Zoller MJ. High resolution analysis of functional determinants on human tissue-type plasminogen activator. J Biol Chem 1991; 266: 5191-201.
22. Refino CJ, Paoni NF, Keyt BA, Pater CS, Badillo JM, Wurm FM, Ogez J, Bennett WF. A variant of tPA (T103N, KHRR 296-299 AAAA) that, by bolus, has increased potency and decreased systemic activation of plasminogen. Thromb Haemost 1993; 70: 313-9.
23. Shohet RV, Spitzer S, Madison EL, Bassel-Duby R, Gething M-J, Sambrook JF. Inhibitor resistant tissue plasminogen activator: An improved thrombolytic agent in vivo. Thromb Haemost 1994; 71: 124-8.
24. Fay WP, Eitzman DT, Shapiro AD, Madison EL, Ginsburg D. Platelets inhibit fibrinolysis in vitro by both plasminogen activator inhibitor-1-dependent and -independent mechanisms. Blood 1994; 83: 351-6.
25. Paoni NF, Chow AM, Pena LC, Keyt BA, Zoller MJ, Bennett WF. Making tissue-type plasminogen activator more fibrin specific. Protein Engng 1993; 6: 529-34.
26. Madison EL, Gething MJ, Sambrook JF. Mutations in at least five distinct regions increase the "fibrin selectivity" of tissue-type plasminogen activator. Fibrinolysis 1992; 6: 105 (Abstract #273).
27. Paoni NF, Keyt BA, Refino CJ, Chow AM, Nguyen HV, Berleau LT, Badillo J, Pena LC, Brady K, Wurm FM, Ogez J, Bennett WF. A slow clearing, fibrin-specific, PAI-1 resistant variant of tPA (T103N, KHRR 296-299 AAAA). Thromb Haemost 1993; 70: 307-12.
28. Gardell SJ, Ramjit DR, Stabilito II, Fujita T, Lynch JJ, Cuca GC, Jain D, Wang S, Tung J-S, Mark GE, Shebuski RJ. Effective thrombolysis without marked plasminemia after bolus intravenous administration of vampire bat salivery plasminogen activator in rabbits. Circulation 1991; 84: 244-53.
29. a1, alteplase, and streptokinase following intravenous bolus injection in a rabbit model of carotid artery thrombosis. Fibrinolysis 1993; 7: 284-90.
30. Keyt BA, Paoni NF, Refino CJ, Ogez J, Etcheverry T, Botstein D, Bennett WF. A faster-acting and more potent form of tissue plasminogen activator Proc Natl Acad Sci 1994; 91: 3670-4.
31. Higgins DL, Kelley RF, Anderson S. Laboratory-directed evolution: The road to an improved Activase®. Proceedings of the BIOTECH USA 1989; 6: 463-6.
32. Hinzmann B, Wernicke D, Pfeifer M, Zacharias U, Fischer B, Eisenmenger F, Will H. Tissue-type plasminogen activator mutants imitating urokinase in the peptide link between kringle and protease domains and at selected sites within the protease domain. Eur J Biochem 1993; 213: 437-43.
33. Korninger C, Collen D. Neutralization of human extrinsic (tissue-type) plasminogen activator in human plasma: No evidence for a specific inhibitor. Thromb Haemost 1981; 46: 662-5.
34. 2-antiplasmin and of mutants obtained by site-directed mutagene-sis of the reactive site. Biochemistry 1987; 26: 5133-40.
35. Kunkel TA. Rapid and efficient site-specific mutagenesis without phenotypic selection. Proc Natl Acad Sci USA 1985, 82: 477-92.
36. Gorman CM, Gies DR, McCray G. Transient production of proteins using an adenovirus transformed cell line. DNA and Protein Engineering Techniques 1990; 2: 3-10.
37. Paoni NF, Refino CJ, Brady K, Pena LC, Nguyen HV, Kerr EM, Johnson AC, Wurm FM, Reis R, Botstein D, Bennett WF. Involvement of residues 296-299 in the enzymatic activity of tissue-type plasminogen activator. Protein Engng 1992; 5: 259-66.
38. Bell JE, Bell ET. Chemical Modification. Side Chain Specific Reagents. In: Proteins and Enzymes. Prentice-Hall. NJ 1988; pp 139-41.
39. Ranby M, Bergsdorf N, Nilsson T. Enzymatic properties of the one- and two-chain form of tissue plasminogen activator. Thromb Res 1982; 27: 175-83.
40. Hoylaerts M, Rijken DC, Lijnen HR, Collen D. Kinetics of the activation of plasminogen by tissue plasminogen activator. J Biol Chem 1982; 257: 2912-9.
41. Rijken DC, Hoylaerts M, Collen D. Fibrinolytic properties of one-chain and two-chain human extrinsic (tissue-type) plasminogen activator. J Biol Chem 1982; 257: 2920-5.