Genta Sofia, Pirosa Maria Cristina, Stathis Anastasios
Medical Oncology, Oncology Institute of Southern Switzerland, Ospedale San Giovanni, 6500, Bellinzona, Switzerland.
Curr Oncol Rep. 2019 Feb 4;21(2):13. doi: 10.1007/s11912-019-0762-x.
Increasing evidence suggests that epigenome plays a central role in cancer development making it a promising target for anticancer treatments. Here, we review two new classes of epigenome-targeting agents: the bromodomain and extraterminal domain proteins (BET) inhibitors and the enhancer of zeste homolog (EZH2) inhibitors.
Clinical research evaluating BET and EZH2 inhibitors is still at an early stage; however, both classes of drugs have demonstrated activity among different hematologic malignancies and solid tumors. Several studies on BETi and EZH2i are ongoing to better define their potential role in cancer treatment, which patients are most likely to benefit and if the association with other drugs can improve their efficacy.
越来越多的证据表明表观基因组在癌症发展中起核心作用，使其成为抗癌治疗的一个有前景的靶点。在此，我们综述两类新型的表观基因组靶向药物：溴结构域和额外末端结构域蛋白（BET）抑制剂以及zeste同源增强子（EZH2）抑制剂。
评估BET和EZH2抑制剂的临床研究仍处于早期阶段；然而，这两类药物在不同血液系统恶性肿瘤和实体瘤中均已显示出活性。关于BETi和EZH2i的多项研究正在进行中，以更好地确定它们在癌症治疗中的潜在作用、哪些患者最可能从中获益以及与其他药物联合使用是否能提高其疗效。
