Helen Diller Family Comprehensive Cancer Center, University of California, San Francisco, California 94158, USA.
Nat Rev Drug Discov. 2017 Apr;16(4):241-263. doi: 10.1038/nrd.2016.256. Epub 2017 Mar 10.
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，人们已经清楚地认识到，表观遗传调控基因的突变在人类癌症中很常见。目前正在开发治疗策略，使用特定的化学抑制剂来靶向这些基因发生突变的癌症。此外，一种基于合成致死性概念的互补方法也逐渐受到关注，该方法可以利用传统方法无法靶向的癌症中的功能丧失突变。这两种方法目前都在几项临床试验中进行测试。在这篇综述中，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方向，以推动该领域的进展。
