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Updated: May 4, 2026

An Integrated Platform for Genome-wide Mapping of Chromatin States Using High-throughput ChIP-sequencing in Tumor Tissues
Published on: April 5, 2018
Cancer epigenetics drug discovery and development: the challenge of hitting the mark
Abstract:
Over the past several years, there has been rapidly expanding evidence of epigenetic dysregulation in cancer, in which histone and DNA modification play a critical role in tumor growth and survival. These findings have gained the attention of the drug discovery and development community, and offer the potential for a second generation of cancer epigenetic agents for patients following the approved "first generation" of DNA methylation (e.g., Dacogen, Vidaza) and broad-spectrum HDAC inhibitors (e.g., Vorinostat, Romidepsin). This Review provides an analysis of prospects for discovery and development of novel cancer agents that target epigenetic proteins. We will examine key examples of epigenetic dysregulation in tumors as well as challenges to epigenetic drug discovery with emerging biology and novel classes of drug targets. We will also highlight recent successes in cancer epigenetics drug discovery and consider important factors for clinical success in this burgeoning area.
Insights
Novel cancer therapies targeting epigenetic proteins are emerging, offering a second generation of treatments beyond DNA methylation and HDAC inhibitors. This review explores epigenetic dysregulation, drug discovery challenges, and future clinical success factors.
Area of Science:
- Oncology
- Epigenetics
- Drug Discovery
Background:
- Epigenetic dysregulation, including histone and DNA modification, is increasingly recognized as critical in cancer progression.
- Approved epigenetic drugs (e.g., DNA methyltransferase inhibitors, histone deacetylase inhibitors) represent the first generation of cancer epigenetic agents.
Purpose of the Study:
- To analyze the prospects for discovering and developing novel cancer agents targeting epigenetic proteins.
- To review key examples of epigenetic dysregulation in tumors and challenges in epigenetic drug discovery.
Main Methods:
- Literature review of epigenetic dysregulation in cancer.
- Analysis of emerging biological insights and novel drug targets in cancer epigenetics.
- Examination of recent successes and factors for clinical advancement.
Main Results:
- Expanding evidence links epigenetic dysregulation to tumor growth and survival.
- Development of a second generation of cancer epigenetic agents is a key focus.
- Novel drug targets and emerging biology present both challenges and opportunities.
Conclusions:
- Targeting epigenetic proteins holds significant promise for next-generation cancer therapies.
- Overcoming drug discovery challenges is crucial for clinical success in cancer epigenetics.
- Continued research into epigenetic dysregulation will drive the development of innovative cancer treatments.
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