Inhibition of dipeptidyl peptidase IV (CD26) by peptide boronic acid dipeptides

被引：7
|
作者：
Pargellis, CA
Campbell, SJ
Pav, S
Graham, ET
Pitner, TP
机构：
[1] BOEHRINGER INGELHEIM PHARMACEUT INC,DEPT ANALYT SCI,RIDGEFIELD,CT 06877
[2] BOEHRINGER INGELHEIM PHARMACEUT INC,DEPT INFORMAT SYST,RIDGEFIELD,CT 06877
来源：
JOURNAL OF ENZYME INHIBITION | 1997年 / 11卷 / 03期
关键词：
dipeptidyl peptidase IV; DPPIV; peptide boronates; val-boroPro; CD26;
D O I：
10.3109/14756369709027647
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Peptide boronic acid dipeptide compounds were analyzed for their ability to inhibit recombinant human dipeptidylpeptidase IV (CD26, DPPIV). Rate constants for the peptide boronates are difficult to obtain because the active boronic acid dipeptide exists in equilibrium with a cyclic inactive species in aqueous solution. Rate constants were determined for the inhibition of DPPIV using several peptide boronates at different pH values. Val-boroPro forms the most tightly bound complex with DPPIV; the first order half life for dissociation of the inactive enzyme/inhibitor complex at 23 degrees C is approximately 27 days.
引用
收藏
页码：151 / 169
页数：19
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