Inhibition of plasminogen activator inhibitor-1: Antibody fragments and their unique sequences as a tool for the development of profibrinolytic drugs

Journal of Thrombosis and Haemostasis

Volumn 2, Issue 2, 2004, Pages 298-305

  Verbeke, K ^a   Gils, A ^a   Declerck, Paul J ^a  

^a UNIVERSITY OF LEUVEN   (Belgium)

Author keywords

Antibody; PAI 1; PAI 1 inhibitor; scFv

Indexed keywords

FIBRINOLYTIC AGENT; MONOCLONAL ANTIBODY; NEUTRALIZING ANTIBODY; PLASMINOGEN ACTIVATOR INHIBITOR 1; SINGLE CHAIN FRAGMENT VARIABLE ANTIBODY; IMMUNOGLOBULIN FRAGMENT; IMMUNOGLOBULIN FV;

ANTIBODY STRUCTURE; ARTICLE; BINDING AFFINITY; BINDING KINETICS; CONTROLLED STUDY; DOSE RESPONSE; DRUG DESIGN; DRUG STRUCTURE; GENE EXPRESSION; MOLECULAR CLONING; PRIORITY JOURNAL; SEQUENCE ANALYSIS; AMINO ACID SEQUENCE; ANTIBODY AFFINITY; GENETICS; HUMAN; IC 50; IMMUNOLOGY; KINETICS;

AMINO ACID SEQUENCE; ANTIBODY AFFINITY; CLONING, MOLECULAR; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; FIBRINOLYTIC AGENTS; HUMANS; IMMUNOGLOBULIN FRAGMENTS; INHIBITORY CONCENTRATION 50; KINETICS; PLASMINOGEN ACTIVATOR INHIBITOR 1;

EID: 4644224651     PISSN: 15387933     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1538-7933.2004.00583.x     Document Type: Article

References (61)

1. Collen D. The plasminogen (fibrinolytic) system. Thromb Haemost 1999; 82: 259-70.
2. Pannekoek H, Veerman H, Lambers H, Diergaarde P, Verweij CL, van Zonneveld AJ, van Mourik JA. Endothelial plasminogen activator inhibitor (PAI): a new member of the Serpin gene family. EMBO J 1986; 5: 2539-44.
3. Ny T, Sawdey M, Lawrence D, Millan JL, Loskutoff DJ. Cloning and sequence of a cDNA coding for the human beta- migrating endothelial-cell-type plasminogen activator inhibitor. Proc Natl Acad Sci USA 1986; 83: 6776-80.
4. Ginsburg D, Zeheb R, Yang AY, Rafferty UM, Andreasen PA, Nielsen L, Dano K, Lebo RV, Gelehrter TD. cDNA cloning of human plasminogen activator-inhibitor from endothelial cells. J Clin Invest 1986; 78: 1673-80.
5. Andreasen PA, Nielsen LS, Kristensen P, Grondahl Hansen J, Skriver L, Dano K. Plasminogen activator inhibitor from human fibrosarcoma cells binds urokinase-type plasminogen activator, but not its proenzyme. J Biol Chem 1986; 261: 7644-51.
6. Thorsen S, Philips M, Selmer J, Lecander I, Astedt B. Kinetics of inhibition of tissue-type and urokinase-type plasminogen activator by plasminogen-activator inhibitor type 1 and type 2. Eur J Biochem 1988; 175: 33-9.
7. Lindahl TL, Ohlsson PI, Wiman B. The mechanism of the reaction between human plasminogen-activator inhibitor 1 and tissue plasminogen activator. Biochem J 1990; 265: 109-13.
8. Hekman CM, Loskutoff DJ. Endothelial cells produce a latent inhibitor of plasminogen activators that can be activated by denaturants. J Biol Chem 1985; 260: 11581-7.
9. Declerck PJ, De Mol M, Alessi MC, Baudner S, Paques EP, Preissner KT, Muller Berghaus G, Collen D. Purification and characterization of a plasminogen activator inhibitor 1 binding protein from human plasma. Identification as a multimeric form of S protein (vitronectin). J Biol Chem 1988; 263: 15454-61.
10. Declerck PJ, De Mol M, Vaughan DE, Collen D. Identification of a conformationally distinct form of plasminogen activator inhibitor-1, acting as a noninhibitory substrate for tissue-type plasminogen activator. J Biol Chem 1992; 267: 11693-6.
11. Urano T, Strandberg L, Johansson LB, Ny T. A substrate-like form of plasminogen-activator-inhibitor type 1: conversions between different forms by sodium dodecyl sulphate. Eur J Biochem 1992; 209: 985-92.
12. Munch M, Heegaard CW, Andreasen PA. Interconversions between active, inert and substrate forms of denatured/refolded type-1 plasminogen activator inhibitor. Biochim Biophys Acta 1993; 1202 29-37.
13. Fay WP, Parker AC, Condrey LR, Shapiro AD. Human plasminogen activator inhibitor 1 (pai 1) deficiency: characterization of a large kindred with a null mutation in the pai 1 gene. Blood 1997; 90 204-8.
14. Declerck PJ, Juhan Vague I, Felez J, Wiman B. Pathophysiology of fibrinolysis. J Intern Med 1994; 236: 425-32.
15. Pralong G, Calandra T, Glauser MP, Schellekens J, Verhoef J, Bachmann F, Kruithof EK. Plasminogen activator inhibitor 1: a new prognostic marker in septic shock. Thromb Haemost 1989; 61: 459-62.
16. Kohler HP, Grant PJ. Plasminogen-activator inhibitor type 1 and coronary artery disease. N Engl J Med 2000; 342: 1792-801.
17. Robbie LA, Booth NA, Brown PAJ, Bennett B. Inhibitors of fibrinolysis are elevated in atherosclerotic plaque. Arterioscler Thromb Vasc Biol 1996; 16: 539-45.
18. Juhan Vague I, Alessi MC, Morange PE. Hypofibrinolysis and increased PAI-1 are linked to atherothrombosis via insulin resistance and obesity. Ann Med 2000; 32 (Suppl. 1): 78-84.
19. Stoop AA, Lupu F, Pannekoek H. Colocalization of thrombin, PAI-1, and vitronectin in the atherosclerotic vessel wall: a potential regulatory mechanism of thrombin activity by PAI-1/vitronectin complexes. Arterioscler Thromb Vasc Biol 2000; 20: 1143-9.
20. Eitzman DT, Fay WP, Lawrence DA, Francis Chmura AM, Shore JD, Olson ST, Ginsburg D. Peptide-mediated inactivation of recombinant and platelet plasminogen activator inhibitor-1 in vitro. J Clin Invest 1995; 95: 2416-20.
21. Kvassman JO, Lawrence DA, Shore JD. The acid stabilization of plasminogen activator inhibitor-1 depends on protonation of a single group that affects loop insertion into beta-sheet A. J Biol Chem 1995; 270: 27942-7.
22. Folkes A, Brown SD, Canne LE, Chan J, Engelhardt E, Epshteyn S, Faint R, Golec J, Hanel A, Kearney P, Leahy JW, MacM, Matthews D, Prisbylla MP, Sanderson J, Simon RJ, Tesfai Z, Vicker N, Wang S, Webb RR, Charlton P. Design, synthesis and in vitro evaluation of potent, novel, small molecule inhibitors of plasminogen activator inhibitor-1. Bioorg Med Chem Lett 2002; 12: 1063-6.
23. Charlton PA, Faint RW, Bent F, Bryans J, Chicarelli-Robinson I, Mackie I, Machin S, Bevan P. Evaluation of a low molecular weight modulator of human plasminogen activator inhibitor-1 activity. Thromb Haemost 1996; 75: 808-15.
24. Friederich PW, Levi MR, Biemond BJ, Charlton P, Templeton D, Vanzonneveld AJ, Bevan P, Pannekoek H, Tencate JW. Novel low molecular weight inhibitor of pai-1 (XR5118) promotes endogenous fibrinolysis and reduces postthrombolysis thrombus growth in rabbits. Circulation 1997; 96: 916-21.
25. Stec WJ, Cierniewski CS, Okruszek A, Kobylanska A, Pawlowska Z, Koziolkiewicz M, Pluskota E, Maciaszek A, Rebowska B, Stasiak M. Stereodependent inhibition of plasminogen activator inhibitor type 1 by phosphorothioate oligonucleotides: proof of sequence specificity in cell culture and in vivo rat experiments. Antisense Nucleic Acid Drug Dev 1997; 7: 567-73.
26. Buczko W, Cierniewski C, Kobylanska A, Koziolkiewicz M, Okruszek A, Pawlowska Z, Pluskota E, Stec WJ. Modulation of plasminogen activator inhibitor type-1 biosynthesis in vitro and in vivo with oligo (nucleoside phosphorothioate)s and related constructs. Pharmacol Ther 1997; 76: 161-75.
27. Nielsen LS, Andreasen PA, Grondahl Hansen J, Huang JY, Kristensen P, Dano K. Monoclonal antibodies to human 54,000 molecular weight plasminogen activator inhibitor from fibrosarcoma cells - inhibitor neutralization and one-step affinity purification. Thromb Haemost 1986; 55: 206-12.
28. Keijer J, Linders M, van Zonneveld AJ, Ehrlich HJ, de Boer JP, Pannekoek H. The interaction of plasminogen activator inhibitor 1 with plasminogen activators (tissue-type and urokinase-type) and fibrin: localization of interaction sites and physiologic relevance. Blood 1991; 78: 401-9.
29. Debrock S, Declerck PJ. Neutralization of plasminogen activator inhibitor-1 inhibitory properties: identification of two different mechanisms. Biochim Biophys Acta 1997; 1337: 257-66.
30. Bijnens AP, Gils A, Stassen JM, Komissarov AA, Knockaert I, Brouwers E, Shore JD, Declerck PJ. The distal hinge of the reactive site loop and its proximity: a target to modulate plasminogen activator inhibitor-1 activity. J Biol Chem 2001; 276: 44912-8.
31. Verhamme I, Kvassman JO, Day DE, Debrock S, Vleugels N, Declerck PJ, Shore JD. Accelerated conversion of human plasminogen activator inhibitor-1 to its latent form by antibody binding. J Biol Chem 1999; 274: 17511-7.
32. Bijnens AP, Gils A, Knockaert I, Stassen JM, Declerck PJ. Importance of the hinge region between α-helix F and the main part of serpins, based upon identification of the epitope of plasminogen activator inhibitor type 1 neutralizing antibodies. J Biol Chem 2000; 275: 6375-80.
33. Biemond BJ, Levi M, Coronel R, Janse MJ, Pannekoek H. Thrombolysis and reocclusion in experimental jugular vein and coronary artery thrombosis: effects of a plasminogen activator inhibitor type 1-neutralizing monoclonal antibody. Circulation 1995; 91: 1175-81.
34. van Giezen JJ, Wahlund G, Nerme Abrahamson T. The Fab-fragment of a PAI-1 inhibiting antibody reduces thrombus size and restores blood flow in a rat model of arterial thrombosis. Thromb Haemost 1997; 77: 964-9.
35. Berry CN, Lunven C, Lechaire I, Girardot C, O'Connor SE. Antithrombotic activity of a monoclonal antibody inducing the substrate form of plasminogen activator inhibitor type 1 in rat models of venous and arterial thrombosis. Br J Pharmacol 1998; 125: 29-34.
36. Montes R, Declerck PJ, Calvo A, Montes M, Hermida J, Munoz MC, Rocha E. Prevention of renal fibrin deposition in endotoxin-induced DIC through inhibition of PAI-1. Thromb Haemost 2000; 84: 65-70.
37. Rupin A, Martin F, Vallez MO, Bonhomme E, Verbeuren TJ. Inactivation of plasminogen activator inhibitor-1 accelerates thrombolysis of a platelet-rich thrombus in rat mesenteric arterioles. Thromb Haemost 2001; 86: 1528-31.
38. Strohal R, Kroemer G, Wick G, Kofler R. Complete variable region sequence of a nonfunctionally rearranged kappa light chain transcribed in the nonsecretor P3-X63-Ag8.653 myeloma cell line. Nucl Acids Res 1987; 15: 2771.
39. Ostermeier C, Michel H. Improved cloning of antibody variable regions from hybridomas by an antisense-directed RNase H digestion of the P3-X63-Ag8.653 derived pseudogene mRNA. Nucl Acids Res 1996; 24 1979-80.
40. Whitlow M, Bell BA, Feng SL, Filpula D, Hardman KD, Hubert SL, Rollence ML, Wood JF, Schott ME, Milenic DE, Yokota T, Schlom J. An improved linker for single-chain Fv with reduced aggregation and enhanced proteolytic stability. Protein Eng 1993; 6: 989-95.
41. Desplancq D, King DJ, Lawson AD, Mountain A. Multimerization behaviour of single chain Fv variants for the tumour-binding antibody B72. 3 Protein Eng 1994; 7: 1027-33.
42. Mallender WD, Carrero J, Voss EW-JR. Comparative properties of the single chain antibody and Fv derivatives of mAb 4-4-20. Relationship between interdomain interactions and the high affinity for fluorescein ligand. J Biol Chem 1996; 271: 5338-46.
43. Nieba L, Honegger A, Krebber C, Pluckthun A. Disrupting the hydrophobic patches at the antibody variable/constant domain interface: improved in vivo folding and physical characterization of an engineered scFv fragment. Protein Eng 1997; 10: 435-44.
44. Vleugels N, Gils A, Mannaerts S, Knockaert I, Declerck PJ. Evaluation of the mechanism of inactivation of plasminogen activator inhibitor-1 by monoclonal antibodies using a stable variant. Fibrinolysis Proteolysis 1998; 12: 277-82.
45. Gils A, Knockaert I, Declerck PJ. Substrate behavior of plasminogen activator inhibitor-1 is not associated with a lack of insertion of the reactive site loop. Biochemistry 1996; 35: 7474-81.
46. Jönsson U, Malmqvist M. Real time biospecific interaction analysis. The integration of surface plasmon resonance detection, general biospecific interface chemistry and microfluidics into one analytical system. In: Turner, A, ed. Advances in Biosensors. London: JAI Press, 1992: 291-336.
47. Verheijen JH, Chang GT, Kluft C. Evidence for the occurrence of a fast-acting inhibitor for tissue-type plasminogen activator in human plasma. Thromb Haemost 1984; 51: 392-5.
48. Laune D, Molina F, Ferrieres G, Mani JC, Cohen P, Simon D, Bernardi T, Piechaczyk M, Pau B, Granier C. Systematic exploration of the antigen binding activity of synthetic peptides isolated from the variable regions of immunoglobulins. J Biol Chem 1997; 272: 30937-44.
49. Eaton DL, Malloy BE, Tsai SP, Henzel W, Drayna D. Isolation, molecular cloning, and partial characterization of a novel carboxypeptidase B from human plasma. J Biol Chem 1991; 266: 21833-8.
50. Kabat EA, Wu TT, Perry HM, Gottesman KS, Foeller C. Sequences of Proteins of Immunological Interest, 5th edn. NIH Publication no. 91-324, 1991. Bethesda, MD: NIH.
51. Komissarov AA, Declerck PJ, Shore JD. Mechanisms of Conversion of plasminogen activator inhibitor 1 from a suicide inhibitor to a substrate by monoclonal antibodies. J Biol Chem 2002; 277 43858-65.
52. Carrell RW, Stein PE. The biostructural pathology of the serpins: critical function of sheet opening mechanism. Biol Chem Hoppe Seyler 1996; 377: 1-17.
53. Naessens D, Gils A, Compernolle G, Declerck P. Elucidation of the epitope of a latency-inducing antibody: identification of a new molecular target for PAI-1 inhibition. Thromb Haemost 2003; 90 52-8.
54. Rocha E, Paramo JA. The relationship between impaired fibrinolysis and coronary heart disease: a role for PAI-1. Fibrinolysis 1994; 8: 294-303.
55. Wiman B. Predictive value of fibrinolytic factors in coronary heart disease. Scand J Clin Lab Invest 1999; 59: 23-31.
56. Debrock S, Sironi L, Declerck PJ. Cloning of a single-chain variable fragment (scFv) switching active plasminogen activator inhibitor-1 to substrate. Gene 1997; 189: 83-8.
57. Verbeke K, Gils A, Declerck PJ. Cloning and paratope analysis of an antibody fragment, a rational approach for the design of a PAI-1 inhibitor. J Thromb Haemost 2004: 2: 289-97
58. Williams WV, Kieber-Emmons T, VonFeldt J, Greene MI, Weiner DB. Design of bioactive peptides based on antibody hypervariable region structures. Development of conformationally constrained and dimeric peptides with enhanced affinity. J Biol Chem 1991; 266: 5182-90.
59. Monnet C, Laune D, Laroche-Traineau J, Biard-Piechaczyk M, Briant L, Bes C, Pugniere M, Mani JC, Pau B, Cerutti M, Devauchelle G, Devaux C, Granier C, Chardes T. Synthetic peptides derived from the variable regions of an anti-CD4 monoclonal antibody bind to CD4 and inhibit HIV-1 promoter activation in virus-infected cells. J Biol Chem 1999; 274: 3789-96.
60. Todorovska A, Roovers RC, Dolezal O, Kortt AA, Hoogenboom HR, Hudson PJ. Design and application of diabodies, triabodies and tetrabodies for cancer targeting. J Immunol Meth 2001; 248: 47-66.
61. Chapman AP, Antoniw P, Spitali M, West S, Stephens S, King DJ. Therapeutic antibody fragments with prolonged in vivo half-lives. Nat Biotechnol 1999; 17: 780-3.