Roshni Bibi, Lakshmi Varshetha, Rakshit Kamal Lahary, Jahnavi Namburi, Fardeen Ahmed Laskar, Koustav Sarkar
{"title":"Epidrugs in cancer: mechanisms, applications, and future direction.","authors":"Roshni Bibi, Lakshmi Varshetha, Rakshit Kamal Lahary, Jahnavi Namburi, Fardeen Ahmed Laskar, Koustav Sarkar","doi":"10.1007/s12094-025-04064-z","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":50685,"journal":{"name":"Clinical & Translational Oncology","volume":" ","pages":""},"PeriodicalIF":2.5000,"publicationDate":"2025-10-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Clinical & Translational Oncology","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1007/s12094-025-04064-z","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"ONCOLOGY","Score":null,"Total":0}
引用次数: 0
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.
期刊介绍:
Clinical and Translational Oncology is an international journal devoted to fostering interaction between experimental and clinical oncology. It covers all aspects of research on cancer, from the more basic discoveries dealing with both cell and molecular biology of tumour cells, to the most advanced clinical assays of conventional and new drugs. In addition, the journal has a strong commitment to facilitating the transfer of knowledge from the basic laboratory to the clinical practice, with the publication of educational series devoted to closing the gap between molecular and clinical oncologists. Molecular biology of tumours, identification of new targets for cancer therapy, and new technologies for research and treatment of cancer are the major themes covered by the educational series. Full research articles on a broad spectrum of subjects, including the molecular and cellular bases of disease, aetiology, pathophysiology, pathology, epidemiology, clinical features, and the diagnosis, prognosis and treatment of cancer, will be considered for publication.