Yang Hua, Wei Li, Xun Yang, Yang Anping, You Hua
Department of Basic Medicine and Biomedical Engineering, School of Medicine, Foshan University, Foshan 528000, Guangdong Province, China.
Affiliated Cancer Hospital & Institute of Guangzhou Medical University, Guangzhou 510095, Guangdong Province, China.
Mol Ther Oncolytics. 2021 Mar 5;21:1-14. doi: 10.1016/j.omto.2021.03.005. eCollection 2021 Jun 25.
Despite advances in treatment, the prognosis for glioma patients remains poor. Bromodomain-containing protein 4 (BRD4), a member of the bromodomain and extraterminal (BET) protein family, plays an important role in controlling oncogene expression and genome stability. In recent years, numerous BRD4 inhibitors have entered clinical trials and achieved exciting results in tumor treatment. Recent clinical studies have shown that BRD4 expression in glioma is significantly higher than in the adjacent normal brain tissue. BRD4 inhibitors effectively penetrate the blood-brain barrier and target glioma tumor tissues but have little effect on normal brain tissues. Thus, BRD4 is a target for the treatment of glioma. In this study, we discuss the progress in the use of BRD4 inhibitors for glioma treatment, their mechanism of action, and their broad potential clinical application.
尽管治疗方面取得了进展，但胶质瘤患者的预后仍然很差。含溴结构域蛋白4（BRD4）是溴结构域和额外末端（BET）蛋白家族的成员，在控制癌基因表达和基因组稳定性方面发挥着重要作用。近年来，众多BRD4抑制剂已进入临床试验，并在肿瘤治疗中取得了令人振奋的成果。最近的临床研究表明，胶质瘤中BRD4的表达明显高于相邻的正常脑组织。BRD4抑制剂能有效穿透血脑屏障并靶向胶质瘤肿瘤组织，但对正常脑组织影响很小。因此，BRD4是治疗胶质瘤的一个靶点。在本研究中，我们讨论了使用BRD4抑制剂治疗胶质瘤的进展、其作用机制以及广泛的潜在临床应用。
