An Overview of Recent Dipeptidyl Peptidase-IV Inhibitors: Linking their Structure and Physico-Chemical Properties with SAR, Pharmacokinetics and Toxicity

Dipeptidyl peptidase-IV (DPP-IV) (EC 3.4.14.5) is. member of the broad class of hydrolytic enzymes which is responsible for degradation of the incretin peptide hormones regulating blood glucose levels. In this article we review the literature on natural and synthetic DPP-IV inhibitors, focusing their chemical structure and mechanism of action. Further, physico-chemical, pharmacokinetic and toxicological properties of DPP-IV inhibitors are calculated and compared. On the basis of literature data we selected the DPP-IV inhibitors with IC50 values below 1 nM and discussed their possible application in therapy of type 2 diabetes mellitus.