256656-31-2Relevant academic research and scientific papers
Discovery of thioazepinone ligands for Src SH2: From non-specific to specific binding
Lesuisse, Dominique,Deprez, Pierre,Albert, Eva,Duc, Tran Thien,Sortais, Benoit,Gofflo, Dominique,Jean-Baptiste, Veronique,Marquette, Jean-Pierre,Schoot, Bernard,Sarubbi, Edoardo,Lange, Gudrun,Broto, Pierre,Mandine, Eliane
, p. 2127 - 2131 (2007/10/03)
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.
