Characterization and comparative evaluation of a novel PAI-1 inhibitor

Thrombosis and Haemostasis

Volumn 88, Issue 1, 2002, Pages 137-143

  Gils, Ann ^a   Stassen, Jean Marie ^a   Nar, Herbert ^a   Kley, Joerg T ^a   Wienen, Wolfgang ^a   Ries, Uwe J ^a   Declerck, Paul J ^a  

^a UNIVERSITY OF LEUVEN   (Belgium)

Author keywords

PAI 1; PAI 1 inhibitor; Serpin; Thrombosis

Indexed keywords

ANTICOAGULANT AGENT; AR H 029953XX; HP 129; PEPTIDE TV ASS; PLASMIN; PLASMINOGEN ACTIVATOR INHIBITOR 1; PLASMINOGEN ACTIVATOR INHIBITOR 1 INHIBITOR; TISSUE PLASMINOGEN ACTIVATOR; UNCLASSIFIED DRUG; UROKINASE; XR 1853; XR 5118; AR H029953XX; AR-H029953XX; CHLORPHENAMIDINE; CHROMOGENIC SUBSTRATE; FENDOSAL; NITRO DERIVATIVE; PIPERAZINE DERIVATIVE; SALICYLIC ACID DERIVATIVE; SERINE PROTEINASE INHIBITOR;

ARTICLE; ASSAY; CHROMOGENIC ASSAY; COMPARATIVE STUDY; COMPLEX FORMATION; CONTROLLED STUDY; DRUG INACTIVATION; DRUG MECHANISM; DRUG POTENCY; DRUG SCREENING; ENZYME LINKED IMMUNOSORBENT ASSAY; ENZYME SUBSTRATE; HUMAN; IC 50; INHIBITION KINETICS; METHODOLOGY; POLYACRYLAMIDE GEL ELECTROPHORESIS; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN STRUCTURE; QUANTITATIVE ANALYSIS; RISK FACTOR; SCREENING TEST; SURFACE PLASMON RESONANCE; METABOLISM;

ANTICOAGULANTS; CHLORPHENAMIDINE; CHROMOGENIC COMPOUNDS; DRUG EVALUATION, PRECLINICAL; ENZYME-LINKED IMMUNOSORBENT ASSAY; HUMANS; INHIBITORY CONCENTRATION 50; NITRO COMPOUNDS; PIPERAZINES; PLASMINOGEN ACTIVATOR INHIBITOR 1; SALICYLIC ACIDS; SERINE PROTEINASE INHIBITORS; SURFACE PLASMON RESONANCE;

EID: 0036301837     PISSN: 03406245     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0037-1613166     Document Type: Article

References (50)

1. Demonstration of a fast-acting inhibitor of plasminogen activators in human plasma
2. Plasminogen activator inhibitor-1 is a major determinant of arterial thrombolysis resistance
3. Plasmin activation system in restenosis: Role in pathogenesis and clinical prediction?
4. Plasminogen activator inhibitor type-1 (PAI-1) and its role in cardiovascular disease
5. Thrombogenic and fibrinolytic factors and cardiovascular risk in non-insulin-dependent diabetes mellitus
6. Clinical implications of elevated PAI-1 revisited: Multiple arterial thromboses in a patient with essential thrombocythemia and elevated plasminogen activator inhibitor-1 (PAI-1) levels: A case report and review of the literature
7. The urokinase type plasminogen activator system in cancer metastasis: A review
8. Multifunctional potential of the plasminogen activation system in tumor invasion and metastasis
9. Plasminogen activator inhibitor type-1: Reactive center and amino-terminal heterogeneity determined by protein and cDNA sequencing
10. cDNA cloning of human plasminogen activator-inhibitor from endothelial cells
11. Cloning and sequence of a cDNA coding for the human beta-migrating endothelial-cell-type plasminogen activator inhibitor
12. Endothelial plasminogen activator inhibitor (PAI): A new member of the Serpin gene family
13. Structure-function relationship in serpins: Current concepts and controversies
14. On the size of the active site in proteases
15. Protein inhibitors of proteinases
16. Implications of the three-dimensional structure of alpha 1-antitrypsin for structure and function of serpins
17. Endothelial cells produce a latent inhibitor of plasminogen activators that can be activated by denaturants
18. Identification of a conformationally distinct form of plasminogen activator inhibitor-1, acting as a noninhibitory substrate for tissue-type plasminogen activator
19. A substrate-like form of plasminogen-activator-inhibitor type 1. Conversion between different forms by sodium dodecyl sulphate
20. Interconversions between active, inert and substrate forms of denatured/refolded type-1 plasminogen activator inhibitor
21. Conversion of plasminogen activator inhibitor-1 from inhibitor to substrate by point mutations in the reactive-site loop
22. Serpin reactive center loop mobility is required for inhibitor function but not for enzyme recognition
23. Proteinase specificity and functional diversity in point mutants of plasminogen activator inhibitor 1
24. Characterization of plasminogen activator inhibitor 1 mutants containing the p13 to p10 region of ovalbumin or antithrombin iii: Evidence that the p13 residue contributes significantly to the active to substrate transition
25. Engineering of conformations of plasminogen activator inhibitor-1 - A crucial role of beta-strand 5A residues in the transition of active form to latent and substrate forms
26. Modulation of plasminogen activator inhibitor 1 by Triton X-100 - Identification of two consecutive conformational transitions
27. Inhibition of plasminogen activator inhibitor-1 activity results in promotion of endogenous thrombolysis and inhibition of thrombus extension in models of experimental thrombosis
28. Thrombolysis and reocclusion in experimental jugular vein and coronary artery thrombosis. Effects of a plasminogen activator inhibitor type 1-neutralizing monoclonal antibody
29. Anti thrombotic effect of a pai 1 inhibitor in rats given endotoxin
30. Neutralization of plasminogen activator inhibitor-1 inhibitory properties: Identification of two different mechanisms
31. Antithrombotic activity of a monoclonal antibody inducing the substrate form of plasminogen activator inhibitor type 1 in rat models of venous and arterial thrombosis
32. Suppression of plasminogen activator inhibitor 1 (PAI-1) activity levels in rats by monoclonal antibodies
33. The acid stabilization of plasminogen activator inhibitor-1 depends on protonation of a single group that affects loop insertion into beta-sheet A
34. Peptide-mediated inactivation of recombinant and platelet plasminogen activator inhibitor-1 in vitro
35. 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
36. Selection of peptides that bind to plasminogen activator inhibitor 1 (PAI-1) using random peptide phage-display libraries
37. Inhibition of plasminogen activator inhibitor 1 activity by two diketopiperazines, xr330 and xr334 produced by streptomyces sp
38. Evaluation of a low molecular weight modulator of human plasminogen activator inhibitor-1 activity
39. Xr5118, a novel modulator of plasminogen activator inhibitor 1 (pai 1), increases endogenous tpa activity in the rat
40. Detergent between 80 modifies the specific activity of pai 1
41. Novel low molecular weight inhibitor of pai 1 (xr5118) promotes endogenous fibrinolysis and reduces postthrombolysis thrombus growth in rabbits
42. Identification of the binding site for a low-molecular-weight inhibitor of plasminogen activator inhibitor type 1 by site-directed mutagenesis
43. Inhibition of plasminogen activator inhibitor-1 by 11-keto-9(E), 12(E)-octadecadienoic acid, a novel fatty acid produced by Trichoderma sp
44. Synthesis and in vitro evaluation of a series of diketopiperazine inhibitors of plasminogen activator inhibitor-1
45. A regulatory hydrophobic area in the flexible joint region of plasminogen activator inhibitor-1, defined with fluorescent activity-neutralizing ligands - Ligand-induced serpin polymerization
46. Stereodependent inhibition of plasminogen activator inhibitor type 1 by phosphorothioate oligonucleotides: Proof of sequence specificity in cell culture and in vivo rat experiments
47. The cytotoxicity of anti-PAI-I oligonucleotides and their conjugates
48. Fendosal (HP 129): A potent anti-inflammatory and analgesic compound
49. Introducing a biosensor based technology for real-time biospecific interaction analysis
50. Predictive value of fibrinolytic factors in coronary heart disease