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Protein & Peptide Letters

Editor-in-Chief

ISSN (Print): 0929-8665
ISSN (Online): 1875-5305

Low-Molecular-Weight Aldehyde Inhibitors of Cathepsin G

Author(s): Adam Lesner, Magdalena Wysocka, Marta Solek, Anna Legowska and Krzysztof Rolka

Volume 16 , Issue 4 , 2009

Page: [408 - 410] Pages: 3

DOI: 10.2174/092986609787848144

Price: $65

Abstract

A series of aldehyde inhibitors with the general formula Ac-Phe-Val-Thr-X-CHO, where X = Lys, Arg, Phe, Tyr, p-nitro-L-phenylalanine (Nif), p-amino-L-phenylalanine (Amf), p-guanidine-L-phenylalanine (Gnf), pyridyl-L-alanine (Pal), was synthesized. The starting structure of this series based on our previous work on cathepsin G chromogenic substrates. The synthesis of all compounds was performed in solid phase applying Fmoc chemistry. We investigated the inhibitory potency of the obtained compounds against cathepsin G and bovine α-chymotrypsin and evaluated their dissociation constants (Ki). The studied peptides displayed different inhibition profiles and potency. As a result, a potent and selective inhibitor of cathepsin G with the sequence Ac-Phe-Val-Thr-Gnf-CHO, displaying Ki = 22 nM was obtained.

Keywords: Cathepsin G, chymotrypsin, peptide aldehydes, peptidomimetics


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