Development of potent and selective dipeptidyl peptidase II inhibitors.
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.
Senten
Kristel
K
Department of Medicinal Chemistry, University of Antwerp (UIA), Universiteitsplein 1, Antwerpen, Belgium.
Van der Veken
Pieter
P
Bal
Gunther
G
De Meester
Ingrid
I
Lambeir
Anne-Marie
AM
Scharpé
Simon
S
Bauvois
Brigitte
B
Haemers
Achiel
A
Augustyns
Koen
K
D018819:Dipeptidyl Peptidase 4 / Q000378:metabolism; D004152:Dipeptidyl-Peptidases and Tripeptidyl-Peptidases / Q000037:antagonists & inhibitors*; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D012661:Semen / Q000201:enzymology; D013329:Structure-Activity Relationship
D010880:Piperidines; D011480:Protease Inhibitors; D011759:Pyrrolidines; D004152:Dipeptidyl-Peptidases and Tripeptidyl-Peptidases; C100151:dipeptidyl peptidase II; D018819:Dipeptidyl Peptidase 4