Highly potent inhibitors of the Grb2-SH2 domain

Authors
Schoepfer, J Fretz, H Gay, B Furet, P Garcia-Echeverria, C End, N Caravatti, G
Citation
J. Schoepfer et al., Highly potent inhibitors of the Grb2-SH2 domain, BIOORG MED, 9(2), 1999, pp. 221-226
Citations number
23
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
2
Year of publication
1999
Pages
221 - 226
Database
ISI
SICI code
0960-894X(19990118)9:2<221:HPIOTG>2.0.ZU;2-7
Abstract
Highly potent inhibitors of the Grb2-SH2 domain have been synthesized. They share the common sequence: Ac-Pmp-Ac(6)c-Asn-NH-(3-indolyl-propyl). Differ ent substituents at the 3-indolyl-propylamine C-terminal group were explore d to further improve the activity. This is the first example of inhibitors of SH2 domains with sub-nanomolar affinity reported to date. (C) 1999 Elsev ier Science Ltd. All rights reserved.