Interdependence of kallikrein-related peptidases in proteolytic networks

Biol Chem. 2010 May;391(5):581-7. doi: 10.1515/BC.2010.055.

Abstract

Human kallikrein-related peptidases (KLKs) are 15 homologous serine proteases involved in several (patho)physiological processes, including cancer. Secreted as precursors, they are activated upon proteolytic release of a short pro-peptide. We searched for interconnection of KLKs within extracellular proteolytic networks leading to activation of protease zymogens and found that (i) pro-KLK activation by other KLKs is scarce, with the exception of pro-KLK11, which is efficiently activated by KLK4 and 5; (ii) pro-KLK4 is activated by matrix metalloproteinase 3; and (iii) trypsin-like KLKs efficiently activate the serine protease urokinase. Our observations provide new insights into the regulation of these important tumor-associated proteases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Enzyme Activation
  • Enzyme Precursors / metabolism*
  • Gene Expression Regulation, Enzymologic
  • Humans
  • Kallikreins / genetics
  • Kallikreins / metabolism*
  • Matrix Metalloproteinase 3 / metabolism
  • Neoplasms / enzymology
  • Serine Endopeptidases / metabolism
  • Urokinase-Type Plasminogen Activator

Substances

  • Enzyme Precursors
  • trypsin-like serine protease
  • KLK5 protein, human
  • Kallikreins
  • Serine Endopeptidases
  • kallikrein 4
  • Urokinase-Type Plasminogen Activator
  • Matrix Metalloproteinase 3