Article
A phenotypic drug discovery study on thienodiazepine derivatives as inhibitors of T cell proliferation induced by CD28 co-stimulation leads to the discovery of a first bromodomain inhibitor.
Bioorganic & medicinal chemistry letters - 1 Mar 2016
Endo Junichi, Hikawa Hidemasa, Hamada Maiko, Ishibuchi Seigo, Fujie Naoto, Sugiyama Naoki, Tanaka Minoru, Kobayashi Haruhito, Sugahara Kunio, Oshita Koichi, Iwata Kazunori, Ooike Shinsuke, Murata Meguru, Sumichika Hiroshi, Chiba Kenji, Adachi Kunitomo
Abstract excerpt
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...
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