Clinical advances in targeting epigenetics for cancer therapy. (18th February 2021)

• Record Type: Journal Article
• Authors: Feng, Shengrui; De Carvalho, Daniel D.
• Is Part Of: FEBS journal. Volume 289:Number 5(2022)
• Page Start: 1214
• Page End: 1239
• Publication Date: 2021-02-18
• Subjects: cancer therapy -- DNA methylation -- epigenetic therapy -- histone modification; Biochemistry -- Periodicals; Molecular biology -- Periodicals; Pathology, Molecular -- Periodicals; 572
• DOI: 10.1111/febs.15750
• Languages: English
• ISSNs: 1742-464X

Abstract

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. Abstract : Small molecules have been designed to target the epigenetic proteins including 'writers', 'readers', and 'erasers', many of which have entered clinical trials for cancer treatment. Here, we review the epigenetic drugs currently in preclinical and clinical investigations and highlight the opportunities and challenges in their implication to cancer treatment. We envision that combining epigenetic drugs with chemotherapies, targeted therapies, and immunotherapies as a promising strategy for cancer therapy.