The dipeptidyl peptidase IV family in cancer and cell biology

FEBS J. 2010 Mar;277(5):1126-44. doi: 10.1111/j.1742-4658.2009.07526.x. Epub 2010 Jan 13.


Of the 600+ known proteases identified to date in mammals, a significant percentage is involved or implicated in pathogenic and cancer processes. The dipeptidyl peptidase IV (DPIV) gene family, comprising four enzyme members [DPIV (EC, fibroblast activation protein, DP8 and DP9] and two nonenzyme members [DP6 (DPL1) and DP10 (DPL2)], are interesting in this regard because of their multiple diverse functions, varying patterns of distribution/localization and subtle, but significant, differences in structure/substrate recognition. In addition, their engagement in cell biological processes involves both enzymatic and nonenzymatic capabilities. This article examines, in detail, our current understanding of the biological involvement of this unique enzyme family and their overall potential as therapeutic targets.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Biomarkers, Tumor / classification
  • Dipeptidyl-Peptidases and Tripeptidyl-Peptidases / classification
  • Dipeptidyl-Peptidases and Tripeptidyl-Peptidases / genetics*
  • Dipeptidyl-Peptidases and Tripeptidyl-Peptidases / metabolism*
  • Disease Models, Animal
  • Drug Delivery Systems
  • Humans
  • Models, Molecular
  • Neoplasms / drug therapy
  • Neoplasms / enzymology*
  • Neoplasms / genetics*
  • Neoplasms / immunology


  • Biomarkers, Tumor
  • Dipeptidyl-Peptidases and Tripeptidyl-Peptidases