Department of Surgery, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
J Med Chem. 2022 Jul 28;65(14):9564-9579. doi: 10.1021/acs.jmedchem.2c00680. Epub 2022 Jul 15.
The histone lysine demethylase 4 (KDM4) family plays an important role in regulating gene transcription, DNA repair, and metabolism. The dysregulation of KDM4 functions is associated with many human disorders, including cancer, obesity, and cardiovascular diseases. Selective and potent KDM4 inhibitors may help not only to understand the role of KDM4 in these disorders but also to provide potential therapeutic opportunities. Here, we provide an overview of the field and discuss current status, challenges, and opportunities lying ahead in the development of KDM4-based anticancer therapeutics.
组蛋白赖氨酸去甲基酶 4（KDM4）家族在调节基因转录、DNA 修复和代谢方面发挥着重要作用。KDM4 功能的失调与许多人类疾病有关，包括癌症、肥胖和心血管疾病。选择性和有效的 KDM4 抑制剂不仅有助于了解 KDM4 在这些疾病中的作用，而且还为提供潜在的治疗机会。在这里，我们提供了该领域的概述，并讨论了在开发基于 KDM4 的抗癌治疗方法方面的当前现状、挑战和机遇。
