Volume 13 Issue 2
Mar.  2023
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Article Navigation >  Journal of Pharmaceutical Analysis  > 2023  >  13(2): 127-141
Qili Liao, Jie Yang, Shengfang Ge, Peiwei Chai, Jiayan Fan, Renbing Jia. Novel insights into histone lysine methyltransferases in cancer therapy: From epigenetic regulation to selective drugs[J]. Journal of Pharmaceutical Analysis, 2023, 13(2): 127-141. doi: 10.1016/j.jpha.2022.11.009
Citation: Qili Liao, Jie Yang, Shengfang Ge, Peiwei Chai, Jiayan Fan, Renbing Jia. Novel insights into histone lysine methyltransferases in cancer therapy: From epigenetic regulation to selective drugs[J]. Journal of Pharmaceutical Analysis, 2023, 13(2): 127-141. doi: 10.1016/j.jpha.2022.11.009
shu

Novel insights into histone lysine methyltransferases in cancer therapy: From epigenetic regulation to selective drugs

doi: 10.1016/j.jpha.2022.11.009

  • a. Department of Ophthalmology, Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, 200001, China;

  • b. Shanghai Key Laboratory of Orbital Diseases and Ocular Oncology, Shanghai, 200001, China

Funds:

This work was supported by the Science and Technology Commission of Shanghai, China (Grant Nos.: 20DZ2270800 and 19JC1410200), Innovative Research Team of High-Level Local Universities in Shanghai, China (Grant No.: SHSMU-ZDCX20210900), and the National Natural Science Foundation of China (Grant No.: 82073889).

  • Received Date: Jul. 25, 2022
  • Accepted Date: Nov. 27, 2022
  • Rev Recd Date: Nov. 24, 2022
  • Publish Date: Mar. 07, 2023
    Abstract
  • The reversible and precise temporal and spatial regulation of histone lysine methyltransferases (KMTs) is essential for epigenome homeostasis. The dysregulation of KMTs is associated with tumor initiation, metastasis, chemoresistance, invasiveness, and the immune microenvironment. Therapeutically, their promising effects are being evaluated in diversified preclinical and clinical trials, demonstrating encouraging outcomes in multiple malignancies. In this review, we have updated recent understandings of KMTs' functions and the development of their targeted inhibitors. First, we provide an updated overview of the regulatory roles of several KMT activities in oncogenesis, tumor suppression, and immune regulation. In addition, we summarize the current targeting strategies in different cancer types and multiple ongoing clinical trials of combination therapies with KMT inhibitors. In summary, we endeavor to depict the regulation of KMT-mediated epigenetic landscape and provide potential epigenetic targets in the treatment of cancers.
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