Discovery of Thioazepinone Ligands for Src SH2: From Non-specific to Specific Binding

Autor:	Eliane Mandine, Pierre Broto, Gudrun Lange, Tran Thien Duc, Pierre Deprez, Dominique Gofflo, Bernard Schoot, Eva Albert, Edoardo Sarubbi, Véronique Jean-Baptiste, Dominique Lesuisse, Jean-Pierre Marquette, Benoit Sortais
Rok vydání:	2001
Předmět:	Models Molecular chemistry.chemical_classification Binding Sites Molecular model Stereochemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science Azepines Ligands SH2 domain Biochemistry Chemical synthesis Oncogene Protein pp60(v-src) src Homology Domains Enzyme chemistry Drug Discovery Chemical specificity Molecular Medicine Signal transduction Binding site Molecular Biology Proto-oncogene tyrosine-protein kinase Src
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 11:2127-2131
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::60270c2b32c45e9ce59ba104204305c2 https://doi.org/10.1016/s0960-894x(01)00386-9 Zobrazit plný text záznamu Full Text from ScienceDirect