Inhibition of plasminogen activator inhibitor-1: Its mechanism and effectiveness on coagulation and fibrosis

Arteriosclerosis, Thrombosis, and Vascular Biology

Volumn 28, Issue 4, 2008, Pages 672-677

  Izuhara, Yuko ^a   Takahashi, Satoru ^b   Nangaku, Masaomi ^c   Takizawa, Shunya ^d   Ishida, Hideyuki ^d   Kurokawa, Kiyoshi ^a   Van Ypersele De Strihou, Charles ^e   Hirayama, Noriaki ^d   Miyata, Toshio ^a,f  

^a TOKAI UNIVERSITY   (Japan)

^b University of Tsukuba School of Medicine   (Japan)

^c UNIVERSITY OF TOKYO   (Japan)

^d TOKAI UNIVERSITY SCHOOL OF MEDICINE   (Japan)

^e UNIVERSITÉ CATHOLIQUE DE LOUVAIN   (Belgium)

^f TOHOKU UNIVERSITY SCHOOL OF MEDICINE   (Japan)

Author keywords

Anticoagulation; Antifibrosis; Plasminogen activator inhibitor 1 inhibitor; Serpin; Virtual screening

Indexed keywords

ANTICOAGULANT AGENT; BLEOMYCIN; FERRIC CHLORIDE; PLASMINOGEN ACTIVATOR INHIBITOR 1; SERINE PROTEINASE INHIBITOR; TICLOPIDINE; TIROFIBAN; TISSUE PLASMINOGEN ACTIVATOR; TM 5007; WARFARIN; FERRIC ION; SERPINE2 PROTEIN, MOUSE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTICOAGULATION; ARTERY; ARTERY THROMBOSIS; ARTICLE; BETA SHEET; BLOOD CLOTTING; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG EFFICACY; DRUG MECHANISM; EXPERIMENTAL MODEL; EXPERIMENTAL MOUSE; EXPERIMENTAL RAT; FIBRINOLYSIS; IN VITRO STUDY; IN VIVO STUDY; LUNG FIBROSIS; MALE; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN STRUCTURE; RAT; SCREENING; TESTIS ARTERY; ANIMAL; ARTERIOVENOUS SHUNT; BINDING SITE; C57BL MOUSE; CHEMICAL STRUCTURE; CHEMICALLY INDUCED DISORDER; CHEMISTRY; COMPUTER INTERFACE; COMPUTER SIMULATION; DRUG EFFECT; DRUG SCREENING; METHODOLOGY; PATHOLOGY; PHYSIOLOGY; PROTEIN CONFORMATION; TESTIS; THROMBOSIS; VASCULARIZATION;

ANIMALS; ANTICOAGULANTS; ARTERIOVENOUS SHUNT, SURGICAL; BINDING SITES; BLEOMYCIN; BLOOD COAGULATION; COMPUTER SIMULATION; DRUG EVALUATION, PRECLINICAL; FERRIC COMPOUNDS; MALE; MICE; MICE, INBRED C57BL; MODELS, MOLECULAR; PLASMINOGEN ACTIVATOR INHIBITOR 1; PROTEIN CONFORMATION; PULMONARY FIBROSIS; RATS; SERPINS; TESTIS; THROMBOSIS; USER-COMPUTER INTERFACE;

EID: 42249111398     PISSN: 10795642     EISSN: None     Source Type: Journal    
DOI: 10.1161/ATVBAHA.107.157479     Document Type: Article

References (32)

1. Carrell RW, Boswell DR. Serpins: the superfamily of plasma serine protease inhibitors. In: Barrett, Salvesen, eds. Proteinase Inhibitors. Elsevier Science. 1986; 403-420.
2. Gils A, Declerck PJ. The structural basis for the pathophysiological relevance of PAI-1 in cardiovascular diseases and the development of potential PAI-1 inhibitors. Thromb Haemost. 2004;91:425-437.
3. Elokdah H, Abou-Gharbia M, Hennan JK, McFarlane G, Mugford CP, Krishnamurthy G, Crandall DL. Tiplaxtinin, a novel, orally efficacious inhibitor of plasminogen activator inhibitor-1: design, synthesis, and preclinical characterization. J Med Chem. 2004;47:3491-3494.
4. Crandall DL, Elokdah H, Di L, Hennan JK, Gorlatova NV, Lawrence DA. Characterization and comparative evaluation of a structurally unique PAI-1 inhibitor exhibiting oral in-vivo efficacy. J Thromb Haemost. 2004;2:1422-1428.
5. Liang A, Wu F, Tran K, Jones SW, Deng G, Ye B, Zhao Z, Snider RM, Dole WP, Morser J, Wu Q. Characterization of a small molecule PAI-1 inhibitor, ZK4044. Thromb Res. 2005;115:341-350.
6. Dellas C, Loskutoff DJ. Historical analysis of PAI-1 from its discovery to its potential role in cell motility and disease. Thromb Haemost. 2005;93:631-640.
7. Bajou K, Noël A, Gerard RD, Masson V, Brunner N, Holst-Hansen C, Skobe M, Fusenig NE, Carmeliet P, Collen D, Foidart JM. Absent of host plasminogen activator inhibitor 1 prevents cancer invasion and vascularization. Nature Med. 1998;4:923-928.
8. Carmeliet P, Stassen JM, Schoonjans L, Ream B, van den Oord JJ, De Mol M, Mulligan RC, Collen D. Plasminogen activator inhibitor-1 gene-deficient mice: II Effects on hemostasis, thrombosis, and thrombolysis. J Clin Invest. 1993;92:2756-2760.
9. Eitzman DT, McCoy RD, Zheng X, Fay WP, Shen T, Ginsburg D, Simon RH. Bleomycin-induced pulmonary fibrosis in transgenic mice that either lack or overexpress the murine plasminogen activator inhibitor-1 gene. J Clin Invest. 1996;97:232-237.
10. Eitzman DT, Westrick RJ, Xu Z, Tyson J, Ginsburg D. Plasminogen activator inhibitor-1 deficiency protects against atherosclerosis progression in the mouse carotid artery. Blood. 2000;96:4212-4215.
11. Weisberg AD, Albornoz F, Griffin JP, Crandall DL, Elokdah H, Fogo AB, Vaughan DE, Brown NJ. Pharmacological inhibition and genetic deficiency of plasminogen activator inhibitor-1 attenuates angiotensin II/salt-induced aortic remodeling. Arterioscler Thromb Vasc Biol. 2005;25:365-371.
12. Nicholas SB, Aguiniga E, Ren Y, Kim J, Wong J, Govindarajan N, Noda M, Wang W, Kawano Y, Collins A, Hsueh WA. Plasminogen activator inhibitor-1 deficiency retards diabetic nephropathy. Kidney Int. 2005;67:1297-1307.
13. ab-fragment of a PAI-1 inhibiting antibody reduces thrombus size and restores blood flow in a rat model of arterial thrombosis. Thromb Haemost. 1997;77:964-969.
14. Wu Q, Zhao Z. Inhibition of PAI-1: A new anti-thrombotic approach. Cur Drug Targets-Cardiovas & Haemat Dis. 2002;2:27-42.
15. MOE (Molecular Operating Environment), version 2004.04; Chemical Computing Group Inc.: Montreal, Quebec, Canada, 2004.
16. Egelund R, Einholm AP, Pedersen KE, Nielsen RW, Christensen A, Deinum J, Andreasen PA. A regulatory hydrophobic area in the flexible joint region of plasminogen activator inhibitor-1: defined with fluorescent activity- neutralizing ligands. J Biol Chem. 2001;276:13077-13086.
17. Xue Y, Bjorquist P, Inghardt T, Linschoten M, Musil D, Sjolin L, Deinum J. Interfering with the inhibitory mechanism of serpins: crystal structure of a complex formed between cleaved plasminogen activator inhibitor type 1 and a reactive-centre loop peptide. Structure. 1998;6:627-636.
18. Horio K, Goto J. Hirayama N. A simple method to improve the odds in finding 'lead-like' compounds from the chemical library. Chem Pharm Bull. 2007;55:980-984.
19. Goto J, Kataoka R, Hirayama N. Ph4Dock-Pharmacophore-based protein-ligand docking. J Med Chem. 2004;47:6804-6811.
20. Bernstein FC, Koetzle TF, Williams GJ, Meyer EF Jr, Brice MD, Rodgers JR, Kennard O, Shimanouchi T, Tasumi M. The protein data bank: a computer-based archival file for macromolecular structures. J Mol Biol. 1997;112:535-542.
21. Edelsbrunner H, Facello M, Fu P, Liang J Measuring Proteins and Voids in Proteins. Proceedings of the 28th Hawaii International Conference on Systems Science. 1995; 256-264.
22. Halgren TA. Merck molecular force field. I. Basis, form, scope, parameterization, and performance of MMFF94. J Comp Chem. 1996;17:490-519.
23. Morishima Y, Tanabe K, Terada Y, Hara T, Kunitada S. Antithrombotic and hemorrhagic effects of DX-9065a, a direct and selective factor Xa inhibitor: comparison with a direct thrombin inhibitor and antithombin III-dependent anticoagulants. Thromb Haemost. 1997;78:1366-1371.
24. Goto S, Tamura B. S, Ishida H. Ability of anti-GP IIb/IIIa agents to dissolve platelet thrombi formed on a collagen surface under blood flow conditions. J Am Coll Cardiol. 2004;44:316-323.
25. Kivirikko KI, Laitinen O, Prockop D. J. Modifications of a specific assay for hydroxyproline in urine. Anal Biochem. 1967;19:249-255.
26. Ashcroft T, Simpson JM, Timbrell V. Simple method of estimating severity of pulmonary fibrosis on a numerical scale. J Clin Pathol. 1988;41:467-470.
27. 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;95:2416-2420.
28. 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;75:808-815.
29. Friederich PW, Levi M, Biemond BJ, Charlton P, Templeton D, van Zonneveld AJ, Bevan P, Pannekoek H, and ten Cate JW. Novel low-molecular-weight inhibitor of PAI-1 (XR5118) promotes endogenous fibrinolysis and reduces postthrombolysis thrombus growth in rabbits. Circulation. 1997;96:916-921.
30. Gorlatova NV, Cale JM, Elokdah H, Li D, Fan K, Warnock M, Crandall DL, Lawrence DA. Mechanism of inactivation of plasminogen activator inhibitor-1 by a small molecule inhibitor. J Biol Chem. 2007;282:9288-9296.
31. Smith LH, Dixon JD, Stringham JR, Eren M, Elokdah H, Crandall DL, Washington K, Vaughan DE. Pivotal role of PAI-1 in a murine model of hepatic vein thrombosis. Blood. 2006;107:132-134.
32. Vaughan DE, De Taeve BM, Eren M. PAI-1 Antagonists: predictable indications and unconventional applications. Curr Drug Targets. 2007;8:962-970.