Targeting epigenetic regulators for cancer therapy: mechanisms and advances in clinical trials

By Yuan Cheng, Cai He, Manni Wang, Xuelei Ma, Fei Mo, Sheng-yong Yang, Junhong Han, Xiawei Wei. Signal Transduction and Targeted Therapy, 2019

873 citations recorded by the source corpus.

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.

Subfields: Molecular Biology

View Paper: https://www.semanticscholar.org/paper/8a9da7f124bcf0c94fbf60c55c35977dcaa3e2ca

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In Molecular Biology

1. Ping Gao
2. Huafeng Zhang
3. Linchong Sun

Citations in the corpus

• Metabolic reprogramming and epigenetic modifications on the path to cancer (2021, background): “…SAM cycle inhibitors and other inhibitors or activators of epigenetic modulation in cancer, please see the excellent reviews by Falkenberg et al., Eckschlager et al., Wong et al. and Cheng et al. (Falkenberg and Johnstone, 2014; Eckschlager et al., 2017; Wong et al., 2017; Cheng et al., 2019).”