Novel insights toward histone lysine methyltransferases in cancer therapy: from epigenetic regulation to selective drugs

Journal of Pharmaceutical Analysis

Available online 30 November 2022

Journal of Pharmaceutical AnalysisAuthor links open overlay panelHighlights•

We provide an updated overview of the regulatory roles of several KMT activities in oncogenesis, tumor suppression and immune regulation.

We summarize the current targeting strategies in different cancer types and multiple ongoing clinical trials of combination therapy with KMT inhibitors.

We endeavor to depict the regulation of KMT-mediated epigenetic landscape of and provide potential epigenetic targets in the treatment of cancers.

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 KMT 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 therapy with KMT inhibitors. In summary, we endeavor to depict the regulation of KMT-mediated epigenetic landscape of and provide potential epigenetic targets in the treatment of cancers.

Keywords

Cancer

epigenetics

histone lysine methyltransferase

epigenetic inhibitors

combined therapeutic strategy

clinical application

© 2022 Published by Elsevier B.V. on behalf of Xi’an Jiaotong University.

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