BET 蛋白影响基因表达并促进癌症的发展，是表观遗传学的解释者。因此，BET 抑制剂代表了一种新型的表观遗传抗癌治疗。尽管初步临床试验已显示 BET 抑制剂的抗癌潜力，但这些药物单独使用时的效果似乎有限。因此，鉴于 BET 抑制剂的单一治疗活性有限，其与其他药物的联合使用值得关注，包括所选药物组合之间药效活性的有意义的变化。在本文中，我们回顾了 BET 蛋白的功能、BET 蛋白靶向癌症的临床前理由、小分子 BET 抑制剂的最新进展以及初步临床试验结果。我们阐明了 BET 抑制剂的耐药机制，阐明了相关的不良事件，研究了这些抑制剂与不同治疗药物相结合的潜力，提出了涉及 BET 抑制剂的协同治疗的综合汇编，并对其作为有效抗肿瘤药物的未来前景进行了展望。我们的结论是，将 BET 抑制剂与其他抗癌药物和创新的下一代药物相结合，对于推进 BET 蛋白的有效靶向作为一种有前途的抗癌策略具有巨大的潜力。© 2023。作者。

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.© 2023. The Author(s).