Journal article
Identification and development of 2,3-dihydropyrrolo[1,2-a]quinazolin-5(1H)-one inhibitors targeting bromodomains within the switch/sucrose nonfermenting complex
- Abstract:
- Bromodomain containing proteins PB1, SMARCA4, and SMARCA2 are important components of SWI/SNF chromatin remodeling complexes. We identified bromodomain inhibitors that target these proteins and 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 KD values 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
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(Version of record, pdf, 3.4MB)
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- Publisher copy:
- 10.1021/acs.jmedchem.5b01997
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Authors
Funding
+ Cambridge Ph.D. Training Programme in Chemical Biology and Molecular Medicine
More from this funder
Funding agency for:
Sutherell, C
+ Engineering and Physical Sciences Research Council
More from this funder
Funding agency for:
Ley, S
Grant:
EP/K039520/1
Bibliographic Details
- Publisher:
- American Chemical Society Publisher's website
- Journal:
- Journal of medicinal chemistry Journal website
- Volume:
- 59
- Issue:
- 10
- Pages:
- 5095-5101
- Publication date:
- 2016-04-27
- DOI:
- EISSN:
-
1520-4804
- ISSN:
-
0022-2623
- Pmid:
-
27119626
- Source identifiers:
-
619949
Item Description
- Language:
- English
- Keywords:
- Pubs id:
-
pubs:619949
- UUID:
-
uuid:6a445819-669d-404b-aee8-804e03dfdff1
- Local pid:
- pubs:619949
- Deposit date:
- 2017-12-20
Terms of use
- Copyright holder:
- © 2016 American Chemical Society
- Copyright date:
- 2016
- Notes:
- 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.
- Licence:
- CC Attribution (CC BY)
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