INHIBITION OF DIPEPTIDYL PEPTIDASE-IV (CD26) BY PEPTIDE BORONIC ACID DIPEPTIDES

Authors
PARGELLIS CA CAMPBELL SJ PAV S GRAHAM ET PITNER TP
Citation
Ca. Pargellis et al., INHIBITION OF DIPEPTIDYL PEPTIDASE-IV (CD26) BY PEPTIDE BORONIC ACID DIPEPTIDES, Journal of enzyme inhibition, 11(3), 1997, pp. 151-169
Citations number
26
Categorie Soggetti
Biology
Journal title
Journal of enzyme inhibition → ACNP
ISSN journal
87555093
Volume
11
Issue
3
Year of publication
1997
Pages
151 - 169
Database
ISI
SICI code
8755-5093(1997)11:3<151:IODP(B>2.0.ZU;2-C
Abstract
Peptide boronic acid dipeptide compounds were analyzed for their abili ty to inhibit recombinant human dipeptidylpeptidase IV (CD26, DPPIV). Rate constants for the peptide boronates are difficult to obtain becau se the active boronic acid dipeptide exists in equilibrium with a cycl ic inactive species in aqueous solution. Rate constants were determine d for the inhibition of DPPIV using several peptide boronates at diffe rent pH values. Val-boroPro forms the most tightly bound complex with DPPIV; the first order half life for dissociation of the inactive enzy me/inhibitor complex at 23 degrees C is approximately 27 days.