Identification and development of 2,3-dihydropyrrolo[1,2-a]quinazolin-5(1H)-one inhibitors targeting bromodomains within the switch/sucrose non-fermenting complex.

Bromodomain containing proteins PB1, SMARCA4, and SMARCA2 are important components of SWI/SNF chromatin remodeling complexes. We identified bromodomain inhibitors targeting these proteins, which display unusual binding modes involving water displacement from the KAc binding site. The best compound b...

Полное описание

Библиографические подробности
Главные авторы: Sutherell, C, Tallant, C, Monteiro, O, Yapp, C, Fuchs, J, Fedorov, O, Siejka, P, Müller, S, Knapp, S, Brenton, J, Brennan, P, Ley, S
Формат: Journal article
Язык:English
Опубликовано: American Chemical Society 2016