Epigenetic Modulators As Therapeutic Agents in Cancer
Overview
Chemistry
Molecular Biology
Authors
Affiliations
Epigenetics play a crucial role in gene regulation and cellular processes. Most importantly, its dysregulation can contribute to the development of tumors. Epigenetic modifications, such as DNA methylation and histone acetylation, are reversible processes that can be utilized as targets for therapeutic intervention. DNA methylation inhibitors disrupt DNA methylation patterns by inhibiting DNA methyltransferases. Such inhibitors can restore normal gene expression patterns, and they can be effective against various forms of cancer. Histone deacetylase inhibitors increase histone acetylation levels, leading to altered gene expressions. Like DNA methylation inhibitors, histone methyltransferase inhibitors target molecules involved in histone methylation. Bromodomain and extra-terminal domain inhibitors target proteins involved in gene expression. They can be effective by inhibiting oncogene expression and inducing anti-proliferative effects seen in cancer. Understanding epigenetic modifications and utilizing epigenetic inhibitors will offer new possibilities for cancer research.
Kaltsas A, Markou E, Kyrgiafini M, Zikopoulos A, Symeonidis E, Dimitriadis F Genes (Basel). 2025; 16(1).
PMID: 39858640 PMC: 11765119. DOI: 10.3390/genes16010093.
Cao T, Shen X, Pei F, Jiang T, Zhang J, Zhou H Cancer Rep (Hoboken). 2024; 7(12):e70080.
PMID: 39676597 PMC: 11647173. DOI: 10.1002/cnr2.70080.
Hypoxia and aging: molecular mechanisms, diseases, and therapeutic targets.
Nisar A, Khan S, Li W, Hu L, Samarawickrama P, Gold N MedComm (2020). 2024; 5(11):e786.
PMID: 39415849 PMC: 11480526. DOI: 10.1002/mco2.786.
Deciphering Depression: Epigenetic Mechanisms and Treatment Strategies.
Aljabali A, Alkaraki A, Gammoh O, Tambuwala M, Mishra V, Mishra Y Biology (Basel). 2024; 13(8).
PMID: 39194576 PMC: 11351889. DOI: 10.3390/biology13080638.
GLP and G9a histone methyltransferases as potential therapeutic targets for lymphoid neoplasms.
Silva-Carvalho A, Filiu-Braga L, Bogea G, de Assis A, Pittella-Silva F, Saldanha-Araujo F Cancer Cell Int. 2024; 24(1):243.
PMID: 38997742 PMC: 11249034. DOI: 10.1186/s12935-024-03441-y.