Histone Demethylase Modulation: Epigenetic Strategy to Combat Cancer Progression

Epigenomes

article

Rashmi Srivastava¹  Rubi Singh²  Shaurya Jauhari³  Niraj Lodhi⁴  Rakesh Srivastava⁵ 

[1] Department of Zoology, Babasaheb Bhimrao Ambedkar University;Department of Hematology, Bioreference Laboratories;Division of Education, Training, and Assessment, Global Education Center, Infosys Limited;Clinical Research ,(Research and Development Division) Mirna Analytics LLC;Molecular Biology and Microbiology, GenTox Research and Development

关键词: epigenetics;    transcription;    histone demethylases;    cancer;    histone demethylase inhibitors;    cancer epitherapy;   

DOI  :  10.3390/epigenomes7020010

学科分类：分子生物学，细胞生物学和基因

来源: mdpi

【 摘 要 】

Epigenetic modifications are heritable, reversible changes in histones or the DNA that control gene functions, being exogenous to the genomic sequence itself. Human diseases, particularly cancer, are frequently connected to epigenetic dysregulations. One of them is histone methylation, which is a dynamically reversible and synchronously regulated process that orchestrates the three-dimensional epigenome, nuclear processes of transcription, DNA repair, cell cycle, and epigenetic functions, by adding or removing methylation groups to histones. Over the past few years, reversible histone methylation has become recognized as a crucial regulatory mechanism for the epigenome. With the development of numerous medications that target epigenetic regulators, epigenome-targeted therapy has been used in the treatment of malignancies and has shown meaningful therapeutic potential in preclinical and clinical trials. The present review focuses on the recent advances in our knowledge on the role of histone demethylases in tumor development and modulation, in emphasizing molecular mechanisms that control cancer cell progression. Finally, we emphasize current developments in the advent of new molecular inhibitors that target histone demethylases to regulate cancer progression.

【 授权许可】

CC BY