GLP and G9a Histone Methyltransferases As Potential Therapeutic Targets for Lymphoid Neoplasms

Overview

Journal Cancer Cell Int

Publisher Biomed Central

Date 2024 Jul 12

PMID 38997742

Authors

Amandda Evelin Silva-Carvalho

Luma Dayane Carvalho Filiu-Braga

Gabriela Muller Reche Bogea

Alan Jhones Barbosa de Assis

Fabio Pittella-Silva

Felipe Saldanha-Araujo

Affiliations

Soon will be listed here.

Abstract

Histone methyltransferases (HMTs) are enzymes that regulate histone methylation and play an important role in controlling transcription by altering the chromatin structure. Aberrant activation of HMTs has been widely reported in certain types of neoplastic cells. Among them, G9a/EHMT2 and GLP/EHMT1 are crucial for H3K9 methylation, and their dysregulation has been associated with tumor initiation and progression in different types of cancer. More recently, it has been shown that G9a and GLP appear to play a critical role in several lymphoid hematologic malignancies. Importantly, the key roles played by both enzymes in various diseases made them attractive targets for drug development. In fact, in recent years, several groups have tried to develop small molecule inhibitors targeting their epigenetic activities as potential anticancer therapeutic tools. In this review, we discuss the physiological role of GLP and G9a, their oncogenic functions in hematologic malignancies of the lymphoid lineage, and the therapeutic potential of epigenetic drugs targeting G9a/GLP for cancer treatment.

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