Dipeptidyl peptidase-IV (DPP-IV) (EC 18.104.22.168) is а 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.
Keywords: Dipeptidyl peptidase-IV inhibitors, Pharmacokinetic properties, Physico-chemical properties, SAR, Toxicological
properties, Type 2 diabetes mellitus.
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