Available online 30 November 2022
Author 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.
AbstractThe 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.
KeywordsCancer
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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