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Development of potent and selective dipeptidyl peptidase II inhibitors
Kristel Senten1, Pieter Van der Veken, Gunther Bal
1Department of Medicinal Chemistry, University of Antwerp (UIA), Universiteitsplein 1, Antwerpen, Belgium.
Bioorganic & Medicinal Chemistry Letters
|September 25, 2002
Abstract:
Structure-activity investigations of product-like dipeptide analogues lacking the C-terminal carbonyl function resulted in potent and selective dipeptidyl peptidase II (DPP II) inhibitors. Dab-Pip has an IC(50)=0.13 microM for DPP II and a 7600-fold selectivity with respect to DPP IV. This compound will be highly valuable for the investigation of the biochemical function of DPP II.