Systematic analysis of a dipeptide library for inhibitor development using human dipeptidyl peptidase IV produced by a Saccharomyces cerevisiae expression system

► A recombinant production system of human dipeptidyl peptidase IV (hDPPIV) was established. ► A dipeptide library was analyzed systematically to develop hDPPIV inhibitors. ► Some dipeptides having hDPPIV inhibitory effects were identified. ► The most effective inhibitory dipeptide was Trp-Pro (Ki = 0.04 mM). ► The inhibitory mode was well explained by some amino acid indices and by the structure of hDPPIV.