Author/Authors :
Dominique Lesuisse، نويسنده , , Pierre Deprez، نويسنده , , Eva Albert، نويسنده , , Tran Thien Duc، نويسنده , , Benoit Sortais، نويسنده , , Dominique Gofflo، نويسنده , , Véronique Jean-Baptiste، نويسنده , , Jean-Pierre Marquette، نويسنده , , Bernard Schoot، نويسنده , , Edoardo Sarubbi، نويسنده , , Gudrun Lange، نويسنده , , Pierre Broto، نويسنده , , Eliane Mandine، نويسنده ,
Abstract :
The structure-based design and synthesis of new thioazepinones as ligands for Src SH2 protein is presented. From benzothioazepinones, ligands with somewhat unspecific binding properties, simpler thioazepinones were designed, the best ones demonstrated nanomolar affinity for Src SH2. A few of these new ligands were crystallized with the protein and demonstrated a specific binding mode with the protein.
