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Nat Rev Cancer. 2012 Jun 22;12(7):465-77. doi: 10.1038/nrc3256.

BET domain co-regulators in obesity, inflammation and cancer.

Author information

1
Cancer Research Center, Nutrition Obesity Research Center, Departments of Medicine and Pharmacology, Boston University School of Medicine, 72 East Concord Street, Boston, MA 02118, USA.

Abstract

The bromodomain is a highly conserved motif of 110 amino acids that is bundled into four anti-parallel α-helices and found in proteins that interact with chromatin, such as transcription factors, histone acetylases and nucleosome remodelling complexes. Bromodomain proteins are chromatin 'readers'; they recruit chromatin-regulating enzymes, including 'writers' and 'erasers' of histone modification, to target promoters and to regulate gene expression. Conventional wisdom held that complexes involved in chromatin dynamics are not 'druggable' targets. However, small molecules that inhibit bromodomain and extraterminal (BET) proteins have been described. We examine these developments and discuss the implications for small molecule epigenetic targeting of chromatin networks in cancer.

PMID:
22722403
PMCID:
PMC3934568
DOI:
10.1038/nrc3256
[Indexed for MEDLINE]
Free PMC Article

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