Discovery of thioazepinone ligands for Src SH2: From non-specific to specific binding

Authors
Lesuisse, D Deprez, P Albert, E Duc, TT Sortais, B Gofflo, D Jean-Baptiste, V Marquette, JP Schoot, B Sarubbi, E Lange, G Broto, P Mandine, E
Citation
D. Lesuisse et al., Discovery of thioazepinone ligands for Src SH2: From non-specific to specific binding, BIOORG MED, 11(16), 2001, pp. 2127-2131
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
16
Year of publication
2001
Pages
2127 - 2131
Database
ISI
SICI code
0960-894X(20010820)11:16<2127:DOTLFS>2.0.ZU;2-9
Abstract
The structure-based design and synthesis of new thioazepinones as ligands f or Src SH2 protein is presented. From benzothioazepinones, ligands with som ewhat unspecific binding properties, simpler thioazepinones were designed, the best ones demonstrated nanomolar affinity for Src SH2. A few of these n ew ligands were crystallized with the protein and demonstrated a specific b inding mode with the protein. (C) 2001 Elsevier Science Ltd. All rights res erved.