Bromodomain and extraterminal (BET) proteins: biological functions, diseases, and targeted therapy
作者机构：Department of Gynecology OncologyHarbin Medical University Cancer HospitalHarbin 150086China School of Optometry and Ophthalmology and Eye HospitalWenzhou Medical UniversityWenzhouChina Department of Colorectal SurgeryHarbin Medical University Cancer HospitalHarbinChina
出 版 物：《Signal Transduction and Targeted Therapy》 (信号转导与靶向治疗（英文）)
年 卷 期：2023年第8卷第12期
页 面：5631-5656页
核心收录：
学科分类：0710[理学-生物学] 1002[医学-临床医学] 100214[医学-肿瘤学] 10[医学]
基 金：supported by the National Natural Science Foundation of China(nos.81872507 and 82173238) the Heilongjiang Provincial Natural Science Foundation Key Projects(ZD2020H007) the Harbin Medical University Cancer Hospital(CN)Nn10 Project(Nn10py2017-01) the China Postdoctoral Science Foundation(296266) the Heilongjiang Province Doctoral Post-doctoral Fund(LBH-Z21177) the Fundamental Research Funds for the Provincial Universities(2022-KYYWF-0291) the Harbin Medical University Haiyan Youth Fund(JJQN2022-3).
主 题：drugs holds meaningful
摘 要：BET proteins,which influence gene expression and contribute to the development of cancer,are epigenetic interpreters.Thus,BET inhibitors represent a novel form of epigenetic anticancer treatment.Although preliminary clinical trials have shown the anticancer potential of BET inhibitors,it appears that these drugs have limited effectiveness when used alone.Therefore,given the limited monotherapeutic activity of BET inhibitors,their use in combination with other drugs warrants attention,including the meaningful variations in pharmacodynamic activity among chosen drug combinations.In this paper,we review the function of BET proteins,the preclinical justification for BET protein targeting in cancer,recent advances in small-molecule BET inhibitors,and preliminary clinical trial findings.We elucidate BET inhibitor resistance mechanisms,shed light on the associated adverse events,investigate the potential of combining these inhibitors with diverse therapeutic agents,present a comprehensive compilation of synergistic treatments involving BET inhibitors,and provide an outlook on their future prospects as potent antitumor agents.We conclude by suggesting that combining BET inhibitors with other anticancer drugs and innovative next-generation agents holds great potential for advancing the effective targeting of BET proteins as a promising anticancer strategy.
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