Structure-based design of a non-peptidic antagonist of the SH2 domain of Grb2

Authors
Caravatti, G Rahuel, J Gay, B Furet, P
Citation
G. Caravatti et al., Structure-based design of a non-peptidic antagonist of the SH2 domain of Grb2, BIOORG MED, 9(14), 1999, pp. 1973-1978
Citations number
13
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
14
Year of publication
1999
Pages
1973 - 1978
Database
ISI
SICI code
0960-894X(19990719)9:14<1973:SDOANA>2.0.ZU;2-8
Abstract
The structure-based design and synthesis of a completely non-peptidic, micr omolar antagonist of the SH2 domain of Grb2 is presented. The compound mimi cs the two main pharmacophores of the natural ligand, the phenylphosphate o f the phosphotyrosine residue and the beta-carboxamide of the X+2 asparagin e, which are linked by a rigid aromatic spacer. (C) 1999 Elsevier Science L td. All rights reserved.