Beyond regulations at DNA levels: A review of epigenetic therapeutics targeting cancer stem cells

• Published in: Cell proliferation Vol. 54; no. 2; pp. e12963 - n/a
• Main Authors: Zhang, Shunhao, Gong, Yanji, Li, Chunjie, Yang, Wenbin, Li, Longjiang
• Format: Journal Article
• Language: English
• Published: England John Wiley & Sons, Inc 01.02.2021; Wiley-Blackwell; John Wiley and Sons Inc
• Subjects: Angiogenesis; Antagomirs - metabolism; Antagomirs - pharmacology; Antagomirs - therapeutic use; Apoptosis; Cancer; cancer stem cells; Cancer therapies; Cell proliferation; Chemoresistance; Chemotherapy; Deoxyribonucleic acid; DNA; DNA (Cytosine-5-)-Methyltransferases - antagonists & inhibitors; DNA (Cytosine-5-)-Methyltransferases - metabolism; DNA methylation; DNA methyltransferase; Drug resistance; Enzyme Inhibitors - pharmacology; Enzyme Inhibitors - therapeutic use; Epigenesis, Genetic; epigenetic therapeutics; Epigenetics; Epithelial-Mesenchymal Transition; Gene expression; Histone deacetylase; Histone Deacetylase Inhibitors - pharmacology; Histone Deacetylase Inhibitors - therapeutic use; Humans; Inhibitors; Kinases; Leukemia; Metastases; Metastasis; MicroRNAs - antagonists & inhibitors; MicroRNAs - genetics; MicroRNAs - metabolism; miRNA; Mutation; Neoplasms - drug therapy; Neoplasms - pathology; Neoplastic Stem Cells - cytology; Neoplastic Stem Cells - drug effects; Neoplastic Stem Cells - metabolism; Phosphorylation; Plastic foam; Proteins; Review; Reviews; Ribonucleic acid; RNA; Stem cells; Tumorigenesis; Tumors; DNA methyltransferase; miRNA; cancer stem cells; histone deacetylase; epigenetic therapeutics
• ISSN: 0960-7722; 1365-2184
• DOI: 10.1111/cpr.12963

In the past few years, the paramount role of cancer stem cells (CSCs), in terms of cancer initiation, proliferation, metastasis, invasion and chemoresistance, has been revealed by accumulating studies. However, this level of cellular plasticity cannot be entirely explained by genetic mutations. Research on epigenetic modifications as a complementary explanation for the properties of CSCs has been increasing over the past several years. Notably, therapeutic strategies are currently being developed in an effort to reverse aberrant epigenetic alterations using specific chemical inhibitors. In this review, we summarize the current understanding of CSCs and their role in cancer progression, and provide an overview of epigenetic alterations seen in CSCs. Importantly, we focus on primary cancer therapies that target the epigenetic modification of CSCs by the use of specific chemical inhibitors, such as histone deacetylase (HDAC) inhibitors, DNA methyltransferase (DNMT) inhibitors and microRNA‐based (miRNA‐based) therapeutics. Epigenetic therapeutics targeting cancer stem cells.