Development of potent and selective dipeptidyl peptidase II inhibitors

Kristel Senten; Pieter Van der Veken; Gunther Bal; Ingrid De Meester; Anne-Marie Lambeir; Simon Scharpé; Brigitte Bauvois; Achiel Haemers; Koen Augustyns

doi:10.1016/s0960-894x(02)00603-0

Development of potent and selective dipeptidyl peptidase II inhibitors

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2825-8. doi: 10.1016/s0960-894x(02)00603-0.

Authors

Kristel Senten¹, Pieter Van der Veken, Gunther Bal, Ingrid De Meester, Anne-Marie Lambeir, Simon Scharpé, Brigitte Bauvois, Achiel Haemers, Koen Augustyns

Affiliation

¹ Department of Medicinal Chemistry, University of Antwerp (UIA), Universiteitsplein 1, Antwerpen, Belgium.

PMID: 12270155
DOI: 10.1016/s0960-894x(02)00603-0

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Dipeptidyl Peptidase 4 / metabolism
Dipeptidyl-Peptidases and Tripeptidyl-Peptidases / antagonists & inhibitors*
Humans
In Vitro Techniques
Kinetics
Male
Piperidines / chemical synthesis*
Piperidines / pharmacology*
Protease Inhibitors / chemical synthesis*
Protease Inhibitors / pharmacology*
Pyrrolidines / chemical synthesis*
Pyrrolidines / pharmacology*
Semen / enzymology
Structure-Activity Relationship

Substances

Piperidines
Protease Inhibitors
Pyrrolidines
Dipeptidyl-Peptidases and Tripeptidyl-Peptidases
dipeptidyl peptidase II
Dipeptidyl Peptidase 4