Published in:

Open Access 01-03-2025 | Epigenetics | REVIEW

Epigenetic drugs in cancer therapy

Authors: Amila Suraweera, Kenneth J. O’Byrne, Derek J. Richard

Published in: Cancer and Metastasis Reviews | Issue 1/2025

Abstract

Genetic and epigenetic modifications of DNA are involved in cancer initiation and progression. Epigenetic modifications change chromatin structure and DNA accessibility and thus affect DNA replication, DNA repair and transcription. Epigenetic modifications are reversible and include DNA methylation, histone acetylation and histone methylation. DNA methylation is catalysed by DNA methyltransferases, histone acetylation and deacetylation are catalysed by histone acetylases and deacetylases, while histone methylation is catalysed by histone methyltransferases. Epigenetic modifications are dysregulated in several cancers, making them cancer therapeutic targets. Epigenetic drugs (epi-drugs) which are inhibitors of epigenetic modifications and include DNA methyltransferase inhibitors (DNMTi), histone deacetylase inhibitors (HDACi), histone methyltransferase inhibitors (HMTi) and bromodomain and extra-terminal motif protein inhibitors (BETi), have demonstrated clinical success as anti-cancer agents. Furthermore, the combination of epi-drugs with standard chemotherapeutic agents has demonstrated promising anti-cancer effects in pre-clinical and clinical settings. In this review, we discuss the role of epi-drugs in cancer therapy and explore their current and future use in combination with other anti-cancer agents used in the clinic. We further highlight the side effects and limitations of epi-drugs. We additionally discuss novel delivery methods and novel tumour epigenetic biomarkers for the screening, diagnosis and development of personalised cancer treatments, in order to reduce off-target toxicity and improve the specificity and anti-tumour efficacy of epi-drugs.

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Title: Epigenetic drugs in cancer therapy
Authors: Amila Suraweera
Kenneth J. O’Byrne
Derek J. Richard
Publication date: 01-03-2025
Publisher: Springer US
Keywords: Epigenetics
Cancer Therapy
Checkpoint Inhibitors
Solid Tumor
Hematologic Cancer
Published in: Cancer and Metastasis Reviews / Issue 1/2025
Print ISSN: 0167-7659
Electronic ISSN: 1573-7233
DOI: https://doi.org/10.1007/s10555-025-10253-7

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