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

Abstract:
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:
Published
Peer review status:
Peer reviewed
Version:
Publisher's version

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Publisher copy:
10.1021/acs.jmedchem.5b01997

Authors


Sutherell, CL More by this author
Tallant, C More by this author
Monteiro, OP More by this author
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Cambridge PhD Training Programme in Chemical Biology and Molecular Medicine More from this funder
Bayer Pharma AG More from this funder
Boehringer Ingelheim More from this funder
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Publisher:
American Chemical Society Publisher's website
Journal:
Journal of Medicinal Chemistry Journal website
Volume:
59
Issue:
10
Pages:
5095–5101
Publication date:
2016-04-05
Acceptance date:
2016-04-26
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
URN:
uuid:7c6b255b-6dfd-4d53-b16e-5645e06ac024
Source identifiers:
619949
Local pid:
pubs:619949
Language:
English

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