1.
Bioorg Med Chem Lett
; 26(5): 1365-70, 2016 Mar 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-26869194
RESUMEN
A phenotypic screening of thienodiazepines derived from a hit compound found through a binding assay targeting co-stimulatory molecules on T cells and antigen presenting cells successfully led to the discovery of a thienotriazolodiazepine compound (7f) possessing potent immunosuppressive activity. A chemical biology approach has succeeded in revealing that 7f is a first inhibitor of epigenetic bromodomain-containing proteins. 7f is expected to become an anti-cancer agent as well as an immunosuppressive agent.