- 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 binds the fifth bromodomain of PB1 with a KD of 124 nM, SMARCA2B and SMARCA4 with KDs of 262 and 417 nM respectively, and displays excellent selectivity over bromodomains other than PB1, SMARCA2, and SMARCA4
- Publication status:
- Peer review status:
- Peer reviewed
- Publisher's version
- American Chemical Society Publisher's website
- Journal of Medicinal Chemistry Journal website
- Publication date:
- Acceptance date:
- Source identifiers:
- Local pid:
- Copyright holder:
- American Chemical Society
- Copyright date:
- Copyright © 2016 American Chemical Society. This is an open access article published under a Creative Commons Attribution (CC-BY) License, which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
Identification and development of 2,3-dihydropyrrolo[1,2-a]quinazolin-5(1H)-one inhibitors targeting bromodomains within the switch/sucrose non-fermenting complex.
Cambridge PhD Training Programme in Chemical Biology and Molecular Medicine More from this funder
+ Engineering and Physical Sciences Research Council More from this funder
AbbVie More from this funder
Bayer Pharma AG More from this funder
Boehringer Ingelheim More from this funderExpand funders...