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Peptidyl epoxides as inhibitors of α-chymotrypsin: Remarkable change from irreversible to reversible competitive inhibitor as a consequence of the improvement of binding affinity

✍ Scribed by Dong H. Kim; Zhi-Hong Li; Soo Suk Lee

Book ID: 104364682
Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 200 KB
Volume: 6
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(96)00536-7

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✦ Synopsis

The replacement of the ester group in (23,3R)-2-benzyl-3,4-epoxybutanoic acid methyl ester (1) with a N-benzoyl-2-pyrrolidylcarboxamide moiety changes the mode of inhibition for a-chymotrypsin from an active site directed inactivator to a reversible competitive inhibitor.