DNA methylation inhibitors: Retrospective and perspective view

Md Gias Uddin; Tamer E Fandy

doi:10.1016/bs.acr.2021.03.007

DNA methylation inhibitors: Retrospective and perspective view

Adv Cancer Res. 2021:152:205-223. doi: 10.1016/bs.acr.2021.03.007. Epub 2021 May 4.

Authors

Md Gias Uddin¹, Tamer E Fandy²

Affiliations

¹ Department of Pharmaceutical & Administrative Sciences, School of Pharmacy, University of Charleston, Charleston, WV, United States.
² Department of Pharmaceutical & Administrative Sciences, School of Pharmacy, University of Charleston, Charleston, WV, United States. Electronic address: tamerfandy@ucwv.edu.

Abstract

DNA methylation is an epigenetic modification that contributes to essential biological processes such as retrotransposon silencing, cell differentiation, genomic imprinting and X-chromosome inactivation. DNA methylation generates a stable epigenetic mark associated with silencing of gene expression. Aberrant DNA methylation is associated with the development of different tumor types. Reversing DNA methylation is a rational strategy to restore gene re-expression and induce cell differentiation in cancer. DNA hypomethylating agents is a class of drugs that demonstrated efficacy in different tumors. In this chapter, the classification of DNA hypomethylating agents, their pharmacodynamics and their potential drawbacks will be discussed.

Keywords: 5-Azacytidine; Cancer; DNA hypomethylating agents; DNA methylation; Decitabine; RG108.

MeSH terms

Antineoplastic Agents* / therapeutic use
Azacitidine / therapeutic use
DNA Methylation
Humans
Neoplasms* / drug therapy
Neoplasms* / genetics
Retrospective Studies

Substances

Antineoplastic Agents
Azacitidine

Grants and funding

P20 GM103434/GM/NIGMS NIH HHS/United States