Slow-tight binding inhibition of pepsin by an aspartic protease inhibitor from streptomyces sp MBR04

TitleSlow-tight binding inhibition of pepsin by an aspartic protease inhibitor from streptomyces sp MBR04
Publication TypeJournal Article
Year of Publication2012
AuthorsMenon, V, Rao, M
JournalInternational Journal of Biological Macromolecules
Volume51
Issue1-2
Pagination165-174
Date PublishedJUL
ISSN0141-8130
KeywordsAspartic protease inhibitor, Low molecular weight, Slow-tight binding inhibition
Abstract

The present article reports a low molecular weight aspartic protease inhibitor from a Streptomyces sp. MBR04 exhibiting a two-step inhibition mechanism against pepsin. The kinetic interactions revealed a reversible, competitive, slow-tight binding inhibition with an IC50 and K-i values of 4.5 nM and 4 nM respectively. The conformational changes induced upon inhibitor binding to pepsin was monitored by far and near UV analysis, demonstrated that the inhibitor binds to the active site and causes inactivation. Chemical modification of the inhibitor with WRK and TNBS abolished the antiproteolytic activity of the inhibitor. (c) 2012 Elsevier B.V. All rights reserved.

DOI10.1016/j.ijbiomac.2012.04.002
Type of Journal (Indian or Foreign)Foreign
Impact Factor (IF)2.596
Divison category: 
Biochemical Sciences