Ali Imran, Choi Gildon, Lee Kwangho
Bio-Organic Science Division, Korea Research Institute of Chemical Technology, Daejeon 34114, Korea.
Recent Pat Anticancer Drug Discov. 2017 Nov 20;12(4):340-364. doi: 10.2174/1574892812666170808121228.
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.
This review discusses the patent literature of BET inhibitors (2010-2017) for the treatment of cancer and other related diseases.
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.
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.
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.
含溴结构域蛋白（BRD）的溴结构域与额外末端（BET）家族在人类中由四个成员组成（BRD2、BRD3、BRD4和BRDT），已成为小分子药物研发中一个有前景的新癌症靶点类别。
本综述讨论了2010年至2017年用于治疗癌症及其他相关疾病的BET抑制剂的专利文献。
BET蛋白作为“表观遗传阅读器”，与组蛋白H3和H4尾部的乙酰化赖氨酸残基结合。对BET蛋白的抑制作用在广泛的治疗应用中促使了各种BET抑制剂的发现和开发。
BET抑制剂作为一种潜在的抗癌治疗方法的重要性日益增加，这导致了学术界和制药行业广泛的专利活动。几种BET抑制剂正在进行治疗各种癌症的临床试验。
本综述描述了与BET抑制用于癌症治疗相关的未满足需求和挑战。同时也介绍了对当前进展和未来前景的洞察。
