Clinical advances in targeting epigenetics for cancer therapy
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Updated: Nov 18, 2025

An Integrated Platform for Genome-wide Mapping of Chromatin States Using High-throughput ChIP-sequencing in Tumor Tissues
Published on: April 5, 2018
Shengrui Feng1,2, Daniel D De Carvalho1,2
1Princess Margaret Cancer Centre, University Health Network, Toronto, ON, Canada.
Abstract:
The appropriate coordination between epigenetic regulators is essential for spatial and temporal regulation of gene expression and maintenance of cell identity. Cancer is a disease driven by both genetic and epigenetic alterations. The widespread dysregulation and reversible nature of epigenetic alterations confer cancer cells with vulnerabilities for therapeutic interventions. Over the past decades, remarkable progress has been made in developing drugs that target epigenetic regulators, with many drugs under evaluation in clinical trials. Here, we summarize the epigenetic drugs currently in clinical investigations and highlight the potentials and challenges in their implication to treat cancer. We also discuss the preclinical and clinical results of combination therapies with epigenetic drugs and other therapies such as targeted and immune-based therapies.
Insights
Epigenetic regulators control gene expression and cell identity. Epigenetic drugs offer cancer treatment potential by targeting reversible epigenetic alterations, with ongoing clinical trials exploring combination therapies.
Area of Science:
- Molecular Biology
- Cancer Biology
- Pharmacology
Background:
- Epigenetic regulators are crucial for gene expression and cell identity.
- Cancer involves genetic and epigenetic alterations, offering therapeutic vulnerabilities.
- Epigenetic dysregulation is reversible, presenting opportunities for drug development.
Purpose of the Study:
- To review epigenetic drugs in clinical investigation for cancer treatment.
- To highlight the potential and challenges of epigenetic therapies.
- To discuss combination therapies involving epigenetic drugs.
Main Methods:
- Literature review of epigenetic drugs in clinical trials.
- Analysis of preclinical and clinical data for combination therapies.
- Synthesis of current research on epigenetic regulators in cancer.
Main Results:
- Numerous epigenetic drugs are under clinical investigation.
- Combination therapies show promise when integrating epigenetic drugs with other treatments.
- Challenges remain in optimizing epigenetic drug efficacy and delivery.
Conclusions:
- Epigenetic drugs represent a promising therapeutic avenue for cancer.
- Combination strategies are key to overcoming resistance and enhancing treatment outcomes.
- Further research is needed to fully realize the potential of epigenetic therapies in oncology.
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