- 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...
Expand abstract - Publication status:
- Published
- Publisher copy:
- 10.1021/jm401582c
-
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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
- Language:
- English
- Keywords:
- Copyright date:
- 2013
Journal article
Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain.
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