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

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

SUBMITTER: Liao Q 

PROVIDER: S-EPMC9999304 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature