Cancer epigenetics and the potential of epigenetic drugs for treating solid tumors

ABSTRACT

Introduction: Epigenetic modification without DNA sequence mutation plays an important role in cancer development. Some small molecular inhibitors targeting key epigenetic molecules have been approved by the Food and Drug Administration to treat hematological malignancies. However, the anticancer effects of these drugs on solid tumors are not satisfactory, and the mechanisms of action remain largely unknown.

Areas covered: The review summarizes the latest research on cancer epigenetics and discusses the potentials and limitations of using epigenetic drugs to treat solid tumors. An analysis of possible reasons for epigenetic drug treatment failure in solid tumors in some clinical trials is discussed along with prospects for future development.

Expert commentary: Next-generation small molecule inhibitors will target novel epigenetic regulators with high cancer specificity. Combined modalities exploiting epigenetic drugs with chemo-/radiotherapy, molecular-targeting drugs, and immunotherapy will be able to effectively treat solid tumors in the near future.

KEYWORDS:

• Epigenetics
• epigenetic drugs
• hematologic malignancies
• solid tumors
• combination therapy

Acknowledgments

We thank the members of the Hunan Key Laboratory of Viral Hepatitis and Center of Molecular Medicine, Xiangya Hospital, Central South University for constructive discussions.

Declaration of interest

The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This manuscript has received funds from the National Natural Science Foundation of China [NSFC, 81572542, NSFC, 81874196], the Doctoral Fund of the Ministry of Education of China (RFDP, 20130162110029), and Scientific Research Funds for Returned Overseas Chinese Scholars, Ministry of Education of China (SRF for ROCS, SEM, 2014-1685).