Epigenetic alternations concern heritable yet reversible changes in histone or DNA modifications that regulate gene activity beyond the underlying sequence. Epigenetic dysregulation is often linked to human disease, notably cancer. With the development of various drugs targeting epigenetic regulators, epigenetic-targeted therapy has been applied in the treatment of hematological malignancies and has exhibited viable therapeutic potential for solid tumors in preclinical and clinical trials. In this review, we summarize the aberrant functions of enzymes in DNA methylation, histone acetylation and histone methylation during tumor progression and highlight the development of inhibitors of or drugs targeted at epigenetic enzymes.
Keywords: Cancer epidemiology; Drug development.
© The Author(s) 2019.
Conflict of interest statement
Conflict of interestThe authors declare that they have no conflict of interest.
Epigenetic Targets and Their Inhibitors in Cancer TherapyL Zhao et al. Curr Top Med Chem 18 (28), 2395-2419. PMID 30582481. - ReviewEpigenetics is defined as the stable and heritable alternations in gene expression without changing the DNA nucleotide sequence. The initiation and progression of cancer …
Epigenetic Enzyme Mutations: Role in Tumorigenesis and Molecular InhibitorsM Han et al. Front Oncol 9, 194. PMID 30984620. - ReviewEpigenetic modifications, such as DNA methylation and histone modification, result in heritable changes in gene expression without changing the DNA sequence. Epigenetic r …
Insights Into Novel Emerging Epigenetic Drugs in Myeloid MalignanciesNS Chandhok et al. Ther Adv Hematol 10, 2040620719866081. PMID 31431820. - ReviewEpigenetics has been defined as 'a stably heritable phenotype resulting from changes in a chromosome without alterations in the DNA sequence' and several epigenetic regul …
Targeting Epigenetic DNA and Histone Modifications to Treat Kidney DiseaseM Fontecha-Barriuso et al. Nephrol Dial Transplant 33 (11), 1875-1886. PMID 29534238. - ReviewEpigenetics refers to heritable changes in gene expression patterns not caused by an altered nucleotide sequence, and includes non-coding RNAs and covalent modifications …
Current and Upcoming Approaches to Exploit the Reversibility of Epigenetic Mutations in Breast CancerF Falahi et al. Breast Cancer Res 16 (4), 412. PMID 25410383. - ReviewDNA methylation and histone modifications are important epigenetic modifications associated with gene (dys)regulation. The epigenetic modifications are balanced by epigen …