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Translating epigenetics into an anticancer drug pipeline for solid tumors

The latest genome-wide mapping techniques allow a comprehensive study of transcriptional activity and gene regulation. Epigenetic marks, such as DNA methylation and histone modifications, impact nucleosome properties and chromatin states, which are critical for regulating gene and noncoding RNA expression [1]. Genetic variation works in concert with epigenetic mechanisms to regulate gene expression in normal tissues. Perturbation of the structure and function of the genome can lead to cancer and all other diseases [2]. The advantage of the reversibility of epigenetic alterations has led to the development of several inhibitors of histone deacetylation or DNA methylation approved for the treatment of hematological malignancies by the US FDA, and efforts are underway to discover novel markers and drugs for solid cancer therapeutic management [3,4]. This article focuses on the latest advances, limitations and challenges for the integration of epigenetics in the research arena of novel biomarker and drug development in the combinatorial treatment of solid cancer.