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含有Bromodomain蛋白4 (BRD4) 的蛋白质和癌症治疗:对双重目标药物开发的一

Zixiang Li¹, Haoyou Wang², Bo Liu³

¹Department of Thoracic Surgery, Liaoning Cancer Hospital & Institute, Cancer Hospital of China Medical University, 110042 Shenyang, China; Department of Thoracic Surgery, Cancer Hospital of Dalian University of Technology, Liaoning Cancer Hospital & Institute, 110042 Shenyang, China; Department of Biotherapy, Cancer Center and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, China; Institute of Precision Drug Innovation and Cancer Center, Second Affiliated Hospital of Dalian Medical University, Dalian 116023, China.

Biochemical pharmacology

|October 13, 2025

概括

含有odomain的蛋白4 (BRD4) 驱动癌症的进展,但耐药性限制了治疗方法. 双位抑制剂通过将BRD4抑制与其他增强癌症治疗策略相结合,显示出有前途.

科学领域:

在瘤学瘤学.
表观遗传学在表观遗传学中,表观遗传学是指表观遗传学.
分子生物学分子生物学

背景情况:

含有odomain的蛋白4 (BRD4) 是一个关键的表观遗传调节器,参与癌症的发展.
BRD4促进瘤基因转录,细胞周期进展,DNA修复,免疫抑制和端粒维护.
早期的BRD4抑制剂如 (+) -JQ1显示了临床前的有效性,但面临临临床耐药性挑战.

研究的目的:

审查瘤对BRD4向疗法的耐药性机制.
探索双目标抑制剂作为克服耐药性和改善癌症治疗的战略.

主要方法:

关于BRD4功能,抵抗机制和新治疗策略的文献综述.
对结合BRD4抑制与其他途径的双抑制剂方法的分析.

主要成果:

瘤对BRD4抑制剂的耐药性涉及BRD4蛋白稳定性,酸化和替代信号通路.
双位抑制剂通过同时向BRD4和其他瘤途径或表观遗传调节剂,提供了一个有希望的策略.
利用合成致死性,表观遗传调节和细胞循环中断的方法可以提高治疗疗效.

结论:

了解BRD4耐药机制对于开发有效的癌症疗法至关重要.
双位BRD4抑制剂是克服耐药性和改善患者治疗结果的有希望的策略.
预计进一步优化和临床翻译的双重目标疗法将推进精确和高效的癌症治疗.

关键词:

BRD4 抑制抑制 BRD4 的抑制癌症治疗癌症治疗药物开发药物开发双重目标药物双重目标药物表观遗传法规表观遗传法规表观遗传法规

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