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. 2014 Aug;24(8):899-900.
doi: 10.1038/cr.2014.90. Epub 2014 Jul 8.

BETs abet Tam-R in ER-positive breast cancer

Prasanna G Alluri  1 , Irfan A Asangani  2 , Arul M Chinnaiyan  3
Affiliations

BETs abet Tam-R in ER-positive breast cancer

Prasanna G Alluri et al. Cell Res. 2014 Aug.

Abstract

Epigenetic modifications such as histone acetylation play a central role in the transcriptional regulation of many oncogenic drivers. Accumulating evidence suggests that pharmacological modulation of certain key epigenetic reader proteins such as BRD2/3/4 may serve as an attractive strategy for treatment of many cancers, including tamoxifen-resistant breast cancer.

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Figures

Figure 1
Figure 1
Context-dependent roles of BRD proteins in breast and prostate cancers. Bromodomain proteins play a key role in transcriptional regulation by interacting with acetylated histones and oncogenic drivers such as WHSC1, AR and TWIST. BET inhibitors cause preferential loss of BRD proteins at “super-enhancers” associated with key oncogenic drivers and may have therapeutic benefit in the treatment of tamoxifen-resistant breast cancer, triple negative breast cancer and castration-resistant prostate cancer.
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