溴尿嘧啶
BRD4
BET抑制剂
表观遗传学
药物发现
计算生物学
药理学
医学
癌症研究
生物
生物信息学
生物化学
基因
作者
Imran Ali,Gildon Choi,Kwang-Ho Lee
出处
期刊:Recent Patents on Anti-cancer Drug Discovery
[Bentham Science]
日期:2017-11-20
卷期号:12 (4)
被引量:21
标识
DOI:10.2174/1574892812666170808121228
摘要
Background: Bromodomain and Extra Terminal (BET) family of bromodomain proteins (BRDs), comprised of four members in humans (BRD2, BRD3, BRD4, and BRDT), has emerged as a promising new cancer target class for small-molecule drug discovery. Objective: This review discusses the patent literature of BET inhibitors (2010-2017) for the treatment of cancer and other related diseases. Method: BET proteins act as ‘epigenetic readers' and bind to acetylated lysine residues on the tails of histones H3 and H4. Inhibition of BET proteins for a wide array of therapeutic applications has led to the discovery and development of various BET inhibitors. Results: The increasing significance of BET inhibitors as a potential anticancer therapeutic has led to an extensive patent activity both from academia and pharmaceutical industry. Several of the BET inhibitors are under clinical development for the treatment of various kinds of cancers. Conclusion: The unmet needs and challenges associated with BET inhibition for cancer treatment have been portrayed in this review. An insight into the current developments and future prospects has been described as well. Keywords: BET, BET inhibitors, BRDs, cancer, epigenetics, patent, therapeutic potential.
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