期刊
NATURE REVIEWS DRUG DISCOVERY
卷 13, 期 5, 页码 339-358出版社
NATURE PUBLISHING GROUP
DOI: 10.1038/nrd4286
关键词
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资金
- Structural Genomics Consortium (SGC)
- Canadian Institutes for Health Research [1097737]
- Canada Foundation for Innovation
- Genome Canada
- GlaxoSmithKline
- Pfizer
- Eli Lilly
- Takeda
- AbbVie
- Novartis Research Foundation
- Bayer
- Ontario Ministry of Research and Innovation
- Wellcome Trust [092809/Z/10/Z]
- Wellcome Trust Career-Development Fellowship [095751/Z/11/Z]
Lysine acetylation is a key mechanism that regulates chromatin structure; aberrant acetylation levels have been linked to the development of several diseases. Acetyl-lysine modifications create docking sites for bromodonnains, which are small interaction modules found on diverse proteins, some of which have a key role in the acetylation-dependent assembly of transcriptional regulator complexes. These complexes can then initiate transcriptional programmes that result in phenotypic changes. The recent discovery of potent and highly specific inhibitors for the BET (bromodonnain and extra-terminal) family of bromodomains has stimulated intensive research activity in diverse therapeutic areas, particularly in oncology, where BET proteins regulate the expression of key oncogenes and anti-apoptotic proteins. In addition, targeting BET bromodonnains could hold potential for the treatment of inflammation and viral infection. Here, we highlight recent progress in the development of bromodomain inhibitors, and their potential applications in drug discovery.
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