A new structural class of selective and non-covalent inhibitors of the chymotrypsin-like activity of the 20S proteasome

Authors
Garcia-Echevarria, C Imbach, P France, D Furst, P Lang, M Noorani, M Scholz, D Zimmermann, J Furet, P
Citation
C. Garcia-echevarria et al., A new structural class of selective and non-covalent inhibitors of the chymotrypsin-like activity of the 20S proteasome, BIOORG MED, 11(10), 2001, pp. 1317-1319
Citations number
21
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
10
Year of publication
2001
Pages
1317 - 1319
Database
ISI
SICI code
0960-894X(20010521)11:10<1317:ANSCOS>2.0.ZU;2-P
Abstract
We describe the identification and in vitro characterization of a series of 2-aminobenzylstatine derivatives that inhibit non-covalently the chymotryp sin-like activity of the 20S proteasome. Our initial SAR data demonstrate t hat the 2-aminobenzylstatine core structure can effectively serve as the ba sis for designing potent, selective and non-covalent inhibitors of the chym otrypsin-like activity of the 20S proteasome. (C) 2001 Elsevier Science Ltd . All rights reserved.