Natural and synthetic inhibitors of the tumor-associated serine protease urokinase-type plasminogen activator

Advances in Experimental Medicine and Biology

Volumn 477, Issue , 2000, Pages 331-341

  Magdolen, Viktor ^a   De, Nuria Arroyo ^a   Sperl, Stefan ^a,b   Muehlenweg, Bernd ^a   Luther, Thomas ^c   Wilhelm, Olaf G ^a,d   Magdolen, Ulla ^a   Graeff, Henner ^a   Reuning, Ute ^a   Schmitt, Manfred ^a  

^a TECHNICAL UNIVERSITY OF MUNICH   (Germany)

^b MAX PLANCK INSTITUTE OF BIOCHEMISTRY   (Germany)

^c DRESDEN UNIVERSITY OF TECHNOLOGY   (Germany)

^d Wilex Biotechnology GmbH   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

5 AMIDINOBENZIMIDAZOLE DERIVATIVE; AMIDINOINDOLE DERIVATIVE; B 428; B 623; BENZAMIDINE DERIVATIVE; BENZO[B]THIOPHENE 2 CARBOXAMIDINE DERIVATIVE; BETA NAPHTHAMIDINE DERIVATIVE; PHENYLGUANIDINE DERIVATIVE; PLASMINOGEN ACTIVATOR INHIBITOR; PLASMINOGEN ACTIVATOR INHIBITOR 1; PLASMINOGEN ACTIVATOR INHIBITOR 2; TAMOXIFEN; UNCLASSIFIED DRUG;

ANGIOGENESIS; ANIMAL CELL; ANTINEOPLASTIC ACTIVITY; CONFERENCE PAPER; DRUG MECHANISM; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; INHIBITION KINETICS; MOUSE; NONHUMAN; PLASMINOGEN ACTIVATION; PRIORITY JOURNAL; PROTEINASE INHIBITION; STRUCTURE ACTIVITY RELATION;

AMIDINES; AMILORIDE; ANIMALS; BENZAMIDINES; GUANIDINES; MICE; MICE, KNOCKOUT; MODELS, BIOLOGICAL; MOLECULAR STRUCTURE; NEOPLASM INVASIVENESS; NEOPLASM PROTEINS; PHENOTYPE; PLASMINOGEN ACTIVATOR INHIBITOR 1; PLASMINOGEN ACTIVATOR INHIBITOR 2; RECEPTORS, CELL SURFACE; SERINE PROTEINASE INHIBITORS; SERPINS; STRUCTURE-ACTIVITY RELATIONSHIP; THIOPHENES; URINARY PLASMINOGEN ACTIVATOR;

ANIMALIA;

EID: 0034470252     PISSN: 00652598     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (44)

1. Effects of synthetic urokinase inhibitors on local invasion and metastasis in a routine mammary tumor model
2. Inhibition of mammary tumor cell adhesion, migration, and invasion by the selective synthetic urokinase inhibitor B428
3. The urokinase-type plasminogen activator system in cancer metastasis: A review
4. Significance of the plasminogen activator inhibitor of placental type (PAI-2) in pregnancy
5. Absence of host plasminogen activator inhibitor I prevents cancer invasion and vascularization
6. Molecular evolution of plasminogen activator inhibitor-1 functional stability
7. The urokinase inhibitor p-aminobenzamidine inhibits growth of a human prostate tumor in SCID mice
8. uPA, uPAR, PAI-1: Key intersection of proteolytic, adhesive and chemotactic highways?
9. Plasminogen activator inhibitor-1 gene-deficient mice I. Generation by homologous recombination and characterization
10. Plasminogen activator inhibitor-1 gene-deficient mice. II. Effects on hemostasis, thrombosis, and thrombolysis
11. Degradation of urokinase plasminogen activator (uPA) in endometrial stromal cells requires both the uPA receptor and the low-density lipoprotein receptor-related protein/alpha2-macroglobulin receptor
12. Urokinase/urokinase receptor system: Internalization/degradation of urokinase-serpin complexes: Mechanism and regulation
13. The plasminogen activator inhibitor-2 gene is not required for normal murine development or survival
14. Type-1 plasminogen-activator inhibitor -conformational differences between latent, active, reactive-centre-cleaved and plasminogen- activator-complexed forms, as probed by proteolytic susceptibility
15. Of mice and men. The function of plasminogen activator inhibitors (PAIs) in vivo
16. Plasminogen binding to cell surfaces
17. Plasminogen activator inhibitor-2: Prognostic relevance in 1012 patients with primary breast cancer
18. Effective activation of the proenzyme form of the urokinase-type plasminogen activator (pro-uPA) by the cysteine protease cathepsin L
19. Activation of proMMP-9 by a plasmin/MMP-3 cascade in a tumor cell model. Regulation by tissue inhibitors of metalloproteinases
20. The crystal structure of plasminogen activator inhibitor 2 at 2.0 Å resolution: Implications for serpin function
21. Synthetic inhibitors of thrombin and factor Xa: From bench to bedside
22. Inhibitors of urokinase reduce size of prostate cancer xenografts in severe combined immunodeficient mice
23. The urokinase receptor is a major vitronectin-binding protein on endothelial cells
24. Plasminogen activator inhibitor-1 represses integrin- and vitronectin-mediated cell migration independently of its function as an inhibitor of plasminogen activation
25. Cathepsin B efficiently activates the soluble and the tumor cell receptor-bound form of the proenzyme urokinase-type plasminogen activator (pro-uPA)
26. Clinical relevance of the urokinase plasminogen activator system in breast cancer
27. Regulation of cell adhesion by PAI-1
28. Evaluation of some newer matrix metalloproteinases
29. Plasminogen activator inhibitor type-2. A spontaneously polymerizing serpin that exists in two topological forms
30. Recycling of the urokinase receptor upon internalization of the uPA:serpin complexes
31. Prevention of prostate-cancer metastasis in vivo by a novel synthetic inhibitor of urokinase-type plasminogen activator (uPA)
32. Urokinase-type plasminogen activator/type-2 plasminogen-activator inhibitor complexes are not internalized upon binding to the urokinase- type-plasminogen-activator receptor in THP-1 cells. Interaction of urokinase-type plasminogen activator/type-2 plasminogen-activator inhibitor complexes with the cell surface
33. Processing of complex between urokinase and its type-2 inhibitor on the cell surface. A possible regulatory mechanism of urokinase activity
34. Multifunctional potential of the plasminogen activation system in tumor invasion and metastasis
35. Clinical impact of the plasminogen activation system in tumor invasion and metastasis: Prognostic relevance and target for therapy
36. The active conformation of plasminogen activator inhibitor 1, a target for drugs to control fibrinolysis and cell adhesion
37. Plasminogen activator inhibitors
38. Synthetic inhibitors of serine proteinases. 17. The effect of benzamidine derivatives on the activity of urokinase and the reduction of fibrinolysis
39. Angiostatic activity of synthetic inhibitors of urokinase type plasminogen activator
40. Aromatic amidines: Comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin
41. Inhibition of urokinase by 4-substituted benzo[b]thiophene-2- carboxamidines: An important new class of selective synthetic urokinase inhibitor
42. Amiloride selectively inhibits the urokinase-type plasminogen activator
43. Prevention of breast cancer growth, invasion, and metastasis by antiestrogen tamoxifen alone or in combination with urokinase inhibitor B-428
44. Selective inhibition of urokinase by substituted phenylguanidines: Quantitative structure-activity relationship analyses