Dipeptidyl peptidase inhibitors, an emerging drug class for inflammatory disease?

Trends Pharmacol Sci. 2009 Nov;30(11):600-7. doi: 10.1016/j.tips.2009.08.003.


Dipeptidyl peptidase (DPP)-4 is a member of the S9b serine protease family, which also includes DPP8 and DPP9. DPP4 cleaves a number of regulatory factors, including chemokines and growth factors. DPP4 inhibitors have recently emerged as an effective treatment option for type 2 diabetes. Early in vitro studies demonstrated that DPP4 inhibitors inhibit T-cell proliferation and cytokine production, leading to their investigation in numerous pre-clinical models of inflammatory diseases, including arthritis, multiple sclerosis and inflammatory bowel disease. Recent data suggest that the early DPP4-specific inhibitors might also bind DPP8 and DPP9, thus exerting their effects through non-specific binding. This review highlights recent insights into the applicability of DPP inhibitors as novel pharmacological agents for inflammatory disease.

Publication types

  • Review

MeSH terms

  • Animals
  • Clinical Trials as Topic
  • Dipeptidases / antagonists & inhibitors
  • Dipeptidyl Peptidase 4
  • Dipeptidyl-Peptidase IV Inhibitors / pharmacology*
  • Dipeptidyl-Peptidases and Tripeptidyl-Peptidases / antagonists & inhibitors
  • Drug Delivery Systems*
  • Drug Evaluation, Preclinical
  • Humans
  • Inflammation / drug therapy*
  • Inflammation / physiopathology


  • Dipeptidyl-Peptidase IV Inhibitors
  • Dipeptidases
  • DPP9 protein, human
  • Dipeptidyl-Peptidases and Tripeptidyl-Peptidases
  • DPP4 protein, human
  • DPP8 protein, human
  • Dipeptidyl Peptidase 4