title: Development of potent and selective dipeptidyl peptidase II inhibitors.
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.
authors.affiliation: Department of Medicinal Chemistry, University of Antwerp (UIA), Universiteitsplein 1, Antwerpen, Belgium.
authors.forename: Kristel
authors.initials: K
authors.lastname: Senten
authors.forename: Pieter
authors.initials: P
authors.lastname: Van der Veken
authors.forename: Gunther
authors.initials: G
authors.lastname: Bal
authors.forename: Ingrid
authors.initials: I
authors.lastname: De Meester
authors.forename: Anne-Marie
authors.initials: AM
authors.lastname: Lambeir
authors.forename: Simon
authors.initials: S
authors.lastname: Scharpé
authors.forename: Brigitte
authors.initials: B
authors.lastname: Bauvois
authors.forename: Achiel
authors.initials: A
authors.lastname: Haemers
authors.forename: Koen
authors.initials: K
authors.lastname: Augustyns
mesh_terms: 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
chemical_list: D010880:Piperidines; D011480:Protease Inhibitors; D011759:Pyrrolidines; D004152:Dipeptidyl-Peptidases and Tripeptidyl-Peptidases; C100151:dipeptidyl peptidase II; D018819:Dipeptidyl Peptidase 4