In the past few years, it has become clear that mutations in epigenetic regulatory genes are common in human cancers. Therapeutic strategies are now being developed to target cancers with mutations in these genes using specific chemical inhibitors. In addition, a complementary approach based on the concept of synthetic lethality, which allows exploitation of loss-of-function mutations in cancers that are not targetable by conventional methods, has gained traction. Both of these approaches are now being tested in several clinical trials. In this Review, we present recent advances in epigenetic drug discovery and development, and suggest possible future avenues of investigation to drive progress in this area.

在过去的几年中，很明显，表观遗传调控基因的突变在人类癌症中很常见。现在正在开发治疗策略，以使用特定的化学抑制剂靶向这些基因中突变的癌症。此外，一种基于合成致死性概念的补充方法已广受欢迎，该方法可利用传统方法无法靶向的癌症中的功能丧失突变。这两种方法现在都在一些临床试验中进行测试。在本综述中，我们介绍了表观遗传药物发现和开发的最新进展，并提出了可能的未来研究途径，以推动这一领域的进展。