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

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

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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...

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Bibliographic Details
Main Authors: Sutherell, C, Tallant, C, Monteiro, O, Yapp, C, Fuchs, J, Fedorov, O, Siejka, P, Müller, S, Knapp, S, Brenton, J, Brennan, P, Ley, S
Format: Journal article
Language:English
Published: American Chemical Society 2016

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