Institut Curie, Paris Sciences et Lettres Research University, Paris, France; INSERM U934/CNRS UMR3215, Paris, France.
Institut Curie, Paris Sciences et Lettres Research University, Paris, France; INSERM U934/CNRS UMR3215, Paris, France.
Curr Opin Chem Biol. 2020 Jun;56:51-62. doi: 10.1016/j.cbpa.2019.11.009. Epub 2020 Jan 23.
Targeting chromatin-modifying enzymes is a promising strategy for cancer treatment. The antitumor effectivity of compounds inhibiting histone methyltransferases - mainly EZH2 - is currently being tested in phase I/II clinical trials, some of them showing positive results in hematological malignancies and solid tumors of specific mutational background. In this review, we aim at highlighting the recent advances in the field of histone methyltransferase inhibitors and describing the challenges that need to be addressed for their successful implementation in the clinics.
靶向染色质修饰酶是癌症治疗的一种有前途的策略。目前正在进行 I/II 期临床试验，以测试抑制组蛋白甲基转移酶（主要是 EZH2）的化合物的抗肿瘤效果，其中一些在血液恶性肿瘤和具有特定突变背景的实体瘤中显示出积极的结果。在这篇综述中，我们旨在强调组蛋白甲基转移酶抑制剂领域的最新进展，并描述在临床中成功实施它们所需要解决的挑战。
