Document Detail

Inhibition of receptor-bound urokinase by plasminogen-activator inhibitors.
MedLine Citation:
PMID:  2161846     Owner:  NLM     Status:  MEDLINE    
Urokinase-type plasminogen activator (uPA) binds to a specific receptor on various cell types, the bound molecule retaining its enzymatic activity against plasminogen. We have now investigated whether receptor-bound uPA also retains the ability to react with and be inhibited by plasminogen activator inhibitors (PAI-1 and PAI-2). uPA bound to its receptor on human U937 monocyte-like cells was inhibited by PAI-1 (in its active form in the presence of vitronectin fragments) with an association rate constant of 4.5 x 10(6) M-1 s-1, which was 40% lower than that obtained for uPA in solution (7.9 x 10(6) M-1 s-1). The inhibition of uPA by PAI-2 was decreased to a similar extent by receptor binding, falling from 5.3 x 10(5) to 3.3 x 10(5) M-1 s-1. Stimulation of U937 cells with phorbol 12-myristate 13-acetate was accompanied by a further reduction in receptor-bound uPA inhibition by PAI-1 and PAI-2 to 1.7 x 10(6) and 1.1 x 10(5) M-1 s-1, respectively. These constants although lower than those for uPA in solution still represent rather rapid inhibition of the enzyme, and demonstrate that uPA bound to its specific cellular receptor remains available for efficient inhibition by PAI's, which may therefore play a major role in controlling cell-surface plasminogen activation and extracellular proteolytic activity.
V Ellis; T C Wun; N Behrendt; E Rønne; K Danø
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  The Journal of biological chemistry     Volume:  265     ISSN:  0021-9258     ISO Abbreviation:  J. Biol. Chem.     Publication Date:  1990 Jun 
Date Detail:
Created Date:  1990-07-16     Completed Date:  1990-07-16     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  2985121R     Medline TA:  J Biol Chem     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  9904-8     Citation Subset:  IM    
Finsen Laboratory, Rigshospitalet, Copenhagen, Denmark.
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MeSH Terms
Antigen-Antibody Complex
Cell Line
Enzyme Precursors / metabolism*
Plasminogen / metabolism
Plasminogen Activators / metabolism*
Plasminogen Inactivators / pharmacology*
Receptors, Cell Surface / drug effects,  metabolism*
Receptors, Urokinase Plasminogen Activator
Tetradecanoylphorbol Acetate / pharmacology
Tumor Cells, Cultured / metabolism
Urokinase-Type Plasminogen Activator / metabolism*
Reg. No./Substance:
0/Antibodies; 0/Antigen-Antibody Complex; 0/Enzyme Precursors; 0/PLAUR protein, human; 0/Plasminogen Inactivators; 0/Receptors, Cell Surface; 0/Receptors, Urokinase Plasminogen Activator; 16561-29-8/Tetradecanoylphorbol Acetate; 9001-91-6/Plasminogen; EC 3.4.21.-/Plasminogen Activators; EC Plasminogen Activator

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