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Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain.

Abstract:

Bromodomains are epigenetic reader domains that have recently become popular targets. In contrast to BET bromodomains, which have proven druggable, bromodomains from other regions of the phylogenetic tree have shallower pockets. We describe successful targeting of the challenging BAZ2B bromodomain using biophysical fragment screening and structure-based optimization of high ligand-efficiency fragments into a novel series of low-micromolar inhibitors. Our results provide attractive leads for d...

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Publication status:
Published

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Publisher copy:
10.1021/jm401582c

Authors


Ferguson, FM More by this author
Fedorov, O More by this author
Chaikuad, A More by this author
Philpott, M More by this author
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Journal:
Journal of medicinal chemistry
Volume:
56
Issue:
24
Pages:
10183-10187
Publication date:
2013-12-13
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
URN:
uuid:401bd886-aeaf-4cbe-b0e5-00b24f2c04fe
Source identifiers:
441660
Local pid:
pubs:441660

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