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Published on: August 5, 2022
Epigenetic inhibitors for cancer treatment
Hongchao Yuan1, Yuanjun Lu1, Yibin Feng1
1School of Chinese Medicine, The University of Hong Kong, Pokfulam, Hong Kong.
Abstract:
Epigenetics is a heritable and reversible modification that occurs independent of the alteration of primary DNA sequence but remarkably affects genetic expression. Aberrant epigenetic regulators are frequently observed in cancer progression not only influencing the behavior of tumor cells but also the tumor-associated microenvironment (TME). Increasing evidence has shown their great potential as biomarkers to predict clinical outcomes and chemoresistance. Hence, targeting the deregulated epigenetic regulators would be a compelling strategy for cancer treatment. So far, current epigenetic drugs have shown promising efficacy in both preclinical trials and clinical treatment of cancer, which encourages research discoveries on the development of novel epigenetic inhibitors either from natural compounds or artificial synthesis. However, only a few have been approved by the FDA, and more effort needs to be put into the related research. This chapter will update the applications and latest progress of epigenetic inhibitors in cancer treatment and provide prospects for the future development of epigenetic drugs.
Insights
Epigenetic regulators influence cancer progression and chemoresistance. Targeting these aberrant regulators with epigenetic drugs offers a promising strategy for cancer treatment, with ongoing research for novel inhibitors.
Area of Science:
- Molecular Biology
- Oncology
- Pharmacology
Background:
- Epigenetics involves heritable, reversible modifications impacting gene expression without altering DNA sequence.
- Aberrant epigenetic regulators are implicated in cancer progression, affecting tumor cells and the tumor microenvironment (TME).
- Epigenetic regulators show potential as biomarkers for predicting clinical outcomes and chemoresistance.
Purpose of the Study:
- To review the applications and latest advancements of epigenetic inhibitors in cancer therapy.
- To explore the potential of targeting deregulated epigenetic regulators for cancer treatment.
- To discuss the future prospects of epigenetic drug development.
Main Methods:
- Review of current literature on epigenetic inhibitors in cancer treatment.
- Analysis of preclinical and clinical trial data for epigenetic drugs.
- Exploration of natural compounds and synthetic molecules as epigenetic inhibitors.
Main Results:
- Current epigenetic drugs demonstrate promising efficacy in preclinical and clinical cancer studies.
- Targeting epigenetic regulators is a compelling strategy for cancer treatment.
- Few epigenetic drugs are FDA-approved, highlighting the need for further research and development.
Conclusions:
- Epigenetic inhibitors represent a significant therapeutic strategy for cancer.
- Continued research is crucial for developing novel and effective epigenetic drugs.
- The field holds promise for improving cancer treatment outcomes and overcoming chemoresistance.
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