Document Detail

Activation of human and rabbit prokallikrein by serine and metalloproteases.
MedLine Citation:
PMID:  3159929     Owner:  NLM     Status:  MEDLINE    
Human and rabbit kidney and urine contain an inactive form of kallikrein. Studies on the mRNA sequence suggested that the active form of the enzyme and the propeptide are linked by a peptide bond between a basic and hydrophobic amino acid. We studied the activation of prokallikrein by serine proteases and a neutral metalloproteinase, thermolysin, because serine proteases cleave the peptide chain after a basic amino acid and thermolysin before a hydrophobic amino acid. The activity of kallikrein was measured by RIA and with a fluorogenic peptide substrate. Trypsin was used as a standard reference activator. We found that human plasmin and plasminogen, activated by urokinase, activate prokallikrein. Pronase coupled to Sepharose also enhanced the activity of the renal kallikrein zymogen. On a molar basis, thermolysin was a more effective activator of prokallikrein than trypsin. The activation by thermolysin was blocked by the inhibitor phosphoramidon, but not by DFP or SBTI. These experiments indicate that, in addition to serine proteases, neutral metalloproteases of tissues may activate prokallikrein.
Y Noda; Y Takada; E G Erdös
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Publication Detail:
Type:  Journal Article; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Kidney international     Volume:  27     ISSN:  0085-2538     ISO Abbreviation:  Kidney Int.     Publication Date:  1985 Apr 
Date Detail:
Created Date:  1985-08-22     Completed Date:  1985-08-22     Revised Date:  2009-11-19    
Medline Journal Info:
Nlm Unique ID:  0323470     Medline TA:  Kidney Int     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  630-5     Citation Subset:  IM    
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MeSH Terms
Endopeptidases / pharmacology*
Enzyme Activation / drug effects
Fibrinolysin / pharmacology
Kallikreins / metabolism*
Kidney / enzymology*
Plasminogen / pharmacology
Prekallikrein / metabolism*,  urine
Pronase / pharmacology
Serine Endopeptidases
Thermolysin / pharmacology*
Grant Support
Reg. No./Substance:
9001-91-6/Plasminogen; 9055-02-1/Prekallikrein; EC 3.4.-/Endopeptidases; EC 3.4.21.-/Kallikreins; EC 3.4.21.-/Serine Endopeptidases; EC; EC 3.4.24.-/Pronase; EC

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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