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Trp-Arg-Xaa tripeptides act as uncompetitive-type inhibitors of human dipeptidyl peptidase IV.

Abstract：

:Human dipeptidyl peptidase IV (hDPPIV, alternative name: CD26) inhibitors provide an effective strategy for the treatment of type 2 diabetes. Recently, our research group discovered a non substrate-mimic inhibitory dipeptide, Trp-Arg, by the systematic analysis of a dipeptide library. In the present study, a tripeptide library Trp-Arg-Xaa (where Xaa represents any amino acid) was analyzed to investigate the interactions of peptidergic inhibitors with hDPPIV. Trp-Arg-Glu showed the highest inhibitory effect toward hDPPIV (Ki=130 μM). All of the tested 19 Trp-Arg-Xaa tripeptides showed unique uncompetitive-type inhibition. The inhibition mechanism of Trp-Arg-Xaa is discussed based on the crystal structure of hDPPIV. The information obtained by this study suggests a novel concept for developing hDPPIV inhibitory peptides and drugs.

journal_name

Peptides

journal_title

Peptides

authors

Lan VT,Ito K,Ito S,Kawarasaki Y

doi

10.1016/j.peptides.2014.01.027

subject

Has Abstract

pub_date

2014-04-01 00:00:00

pages

166-70

eissn

0196-9781

issn

1873-5169

pii

S0196-9781(14)00041-2

journal_volume

54

pub_type

杂志文章

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