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Epidrugs in cancer: mechanisms, applications, and future direction.

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Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico 📖 저널 OA 14.8% 2022: 0/2 OA 2023: 0/3 OA 2024: 4/7 OA 2025: 7/46 OA 2026: 31/223 OA 2022~2026 2026 Vol.28(4) p. 1085-1100
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Bibi R, Varshetha L, Lahary RK, Namburi J, Laskar FA, Sarkar K

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DNA methylation, histone modifications, and regulation of non-coding RNA are all epigenetic modifications affecting cancer cells of origin and progression.

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APA Bibi R, Varshetha L, et al. (2026). Epidrugs in cancer: mechanisms, applications, and future direction.. Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico, 28(4), 1085-1100. https://doi.org/10.1007/s12094-025-04064-z
MLA Bibi R, et al.. "Epidrugs in cancer: mechanisms, applications, and future direction.." Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico, vol. 28, no. 4, 2026, pp. 1085-1100.
PMID 41062905 ↗

Abstract

DNA methylation, histone modifications, and regulation of non-coding RNA are all epigenetic modifications affecting cancer cells of origin and progression. These changes lead to changed expression of genes, which in turn is the reason for cancer occurrence in the form of inhibition of tumor suppressor genes or activation of oncogenes. Epigenetic changes, as opposed to genetic mutations, are reversible; thus, they seem to be interesting targets for therapeutic interventions. Current review summarizes the various types of epidrugs -DNA methyltransferase inhibitors (DNMTis), histone deacetylase inhibitors (HDACis), histone methyltransferase inhibitors (HMTis), and BET inhibitors-are studied in this review. And the mechanisms of action, therapeutic potential, and clinical applications of epidrugs in several types of cancer, such as solid tumors (breast, lung, colorectal, and brain tumors) and hematological malignancies (acute myeloid leukemia (AML) and multiple myeloma). In addition, we address the challenges faced by epigenetic therapies, such as drug toxicity, off-target effects, and drug resistance. One of the rapidly evolving areas of cancer treatment is bringing new cancer treatments, and the use of epidrugs with conventional treatments, immunotherapy, and targeted therapy is an area. Epidrugs, drugs that control epigenetic pathways, have become substances that could be beneficial in cancer treatment. They can repress normal gene expression, reverse drug resistance, and make tumors penetrable to treatments that are already in place. Following instructions by tumor-specific epigenome analysis, personalized epigenetic therapy has the prospect to tailor the treatment schedule and to enhance medical outcome. Overcoming limitations and forming combination strategies to promote efficacy with less toxicity would foster the epigenetic treatment approach for cancer.

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