溴结构域蛋白4的抑制策略及其在肿瘤治疗中的研究进展

刘晓庆; 梁爽; 刘永军; 张娜

doi:10.11665/j.issn.1000-5048.20210302

溴结构域蛋白4的抑制策略及其在肿瘤治疗中的研究进展

山东大学药学院，天然产物化学生物学教育部重点实验室，济南 250012

基金项目: 国家自然科学基金资助项目(No.81974498)

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出版历程
- 收稿日期: 2020-05-22
- 修回日期: 2021-02-02
- 刊出日期: 2021-06-24

Progress of research on inhibition strategy of bromodomain-containing protein 4 and its application in tumor therapy

Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Ji'nan 250012, China

Funds: This study was supported by the National Natural Science Foundation of China (No. 81974498)

摘要

摘要: 溴结构域蛋白4（bromodomain-containing protein 4，BRD4）是溴结构域和超末端结构域家族中最重要的蛋白，其过度表达与多种肿瘤的发生发展密切相关，成为肿瘤治疗的新靶点。BRD4的抑制策略主要包括BRD4抑制剂和BRD4降解剂，其单独用药或与化学治疗、光热治疗、免疫治疗等治疗手段联合使用均显示出良好的抗肿瘤效果，为肿瘤治疗开辟了新的方向。本文介绍了BRD4的结构及其在肿瘤发生发展中的作用，综述了BRD4的抑制策略、在肿瘤联合治疗中应用以及耐药性的研究进展，为以BRD4为靶点的肿瘤治疗提供理论参考。
- BRD4 /
- 抑制剂 /
- 降解剂 /
- 肿瘤联合治疗 /
- 耐药性
Abstract: Bromodomain-containing protein 4 (BRD4), a new target for tumor therapy, is the most important member of the bromodomain and extra-terminal family. The overexpression of BRD4 is associated with genesis and development of various cancers.Used either alone or in combination with other treatments such as chemotherapy, photothermal therapy and immunotherapy, the BRD4 inhibitors or degraders exhibited excellent antitumor effects, providing a new direction in tumor treatment. In this review, the structure and function of BRD4, the inhibition strategies of BRD4, the application in tumor combination therapy and drug resistance are introduced, which provides reference for targeting BRD4 in tumor therapy.
- BRD4 /
- inhibitor /
- degrader /
- tumor combination therapy /
- drug resistance

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参考文献(51)

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