Histone methylation machinery in gliomas: From enzymatic mechanisms to inhibitor development

Glioma is the most common primary malignant tumor of the central nervous system (CNS). Advances in molecular pathology have established a robust causal link between histone modifications and glioma genesis. In addition to prior findings, recent empirical evidence has unequivocally substantiated the intricate and close relationship between histone modifications and temozolomide (TMZ) resistance, thereby advancing our understanding in this field. This article systematically reviews the roles of histone methylation modifications in glioma pathogenesis and their implications for the mechanisms of therapeutic drug action. Moreover, the latest research advancements concerning histone methylation - related enzymes and their inhibitors in the diagnosis and treatment of glioma were elaborately described, highlighting their significant implications for the field. It is highly anticipated that this review will serve as a catalyst, offering a novel and insightful direction for the ongoing research endeavors, diagnostic approaches, and therapeutic strategies pertaining to glioma.