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Updated: Nov 11, 2025
An Integrated Platform for Genome-wide Mapping of Chromatin States Using High-throughput ChIP-sequencing in Tumor Tissues
Published on: April 5, 2018
Current paradigms in epigenetic anticancer therapeutics and future challenges
Manoj Singh1, Vikas Kumar1, Nirmala Sehrawat1
1Department of Biotechnology, Maharishi Markandeshwar (Deemed to be University), Mullana-Ambala, 133207, Haryana, India.
Abstract:
Any alteration at the genetic or epigenetic level, may result in multiplex of diseases including tumorigenesis which ultimately results in the cancer development. Restoration of the normal epigenome by reversing the epigenetic alterations have been reported in tumors paving the way for development of an effective epigenetic treatment in cancer. However, delineating various epigenetic events has been a challenging task so far despite substantial progress in understanding DNA methylation and histone modifications during transcription of genes. Many inhibitors in the form of epigenetic drugs mostly targeting chromatin and histone modifying enzymes including DNA methyltransferase (DNMT) enzyme inhibitors and a histone deacetylases (HDACs) inhibitor, have been in use subsequent to the approval by FDA for cancer treatment. Similarly, other inhibitory drugs, such as FK228, suberoylanilide hydroxamic acid (SAHA) and MS-275, have been successfully tested in clinical studies. Despite all these advancements, still we see a hazy view as far as a promising epigenetic anticancer therapy is concerned. The challenges are to have more specific and effective inhibitors with negligible side effects. Moreover, the alterations seen in tumors are not well understood for which one has to gain deeper insight into the tumor pathology as well. Current review focusses on such epigenetic alterations occurring in cancer and the effective strategies to utilize such alterations for potential therapeutic use and treatment in cancer.
Insights
Epigenetic alterations drive cancer development. This review explores reversing these changes with epigenetic drugs for effective cancer treatment, focusing on challenges and future strategies.
Area of Science:
- Oncology
- Epigenetics
- Molecular Biology
Background:
- Genetic and epigenetic alterations are key drivers of tumorigenesis and cancer development.
- Epigenetic modifications, including DNA methylation and histone modifications, play crucial roles in gene transcription.
- Reversing epigenetic alterations in tumors offers a promising avenue for developing effective epigenetic cancer treatments.
Purpose of the Study:
- To review epigenetic alterations in cancer.
- To discuss strategies for utilizing these alterations for therapeutic benefit.
- To highlight challenges and future directions in epigenetic cancer therapy.
Main Methods:
- Review of current literature on epigenetic alterations in cancer.
- Analysis of epigenetic drugs targeting DNA methyltransferase (DNMT) and histone deacetylases (HDACs).
- Discussion of clinical studies involving epigenetic inhibitors like FK228, SAHA, and MS-275.
Main Results:
- Epigenetic drugs targeting DNMT and HDACs are FDA-approved and show promise in clinical studies.
- Despite progress, challenges remain in developing specific, effective inhibitors with minimal side effects.
- Deeper understanding of tumor pathology and epigenetic alterations is needed for optimized therapy.
Conclusions:
- Epigenetic therapy holds significant potential for cancer treatment by reversing aberrant epigenetic modifications.
- Further research is required to overcome challenges related to inhibitor specificity, efficacy, and understanding tumor-specific epigenetic landscapes.
- Developing more targeted and effective epigenetic strategies is crucial for advancing cancer therapy.
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