Bromodomain and extra-terminal (BET) family proteins: New therapeutic targets in major diseases.
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Date
2016-06
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Abstract
The bromodomains and extra-terminal domain (BET) family proteins recognize acetylated chromatin through their
bromodomains (BDs) and help in regulating gene expression. BDs are chromatin ‘readers’: by interacting with
acetylated lysines on the histone tails, they recruit chromatin-regulating proteins on the promoter region to regulate
gene expression and repression. Extensive efforts have been employed by scientific communities worldwide to
identify and develop potential inhibitors of BET family BDs to regulate protein expression by inhibiting acetylated
histone (H3/H4) interactions. Several small molecule inhibitors have been reported, which not only have high affinity
but also have high specificity to BET BDs. These developments make BET family proteins an important therapeutic
targets for major diseases such as cancer, neurological disorders, obesity and inflammation. Here, we review and
discuss the structural biology of BET family BDs and their applications in major diseases.
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Keywords
BET family bromodomains, drug targets, epigenetics, structural biology, transcription regulation
Citation
Padmanabhan Balasundaram, Mathur Shruti, Ramu Manjula, Tripathi Shailesh. Bromodomain and extra-terminal (BET) family proteins: New therapeutic targets in major diseases. Journal of Biosciences. 2016 June; 41(2): 295-311.