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

Yuan Cheng, He Cai, Manni Wang, Xuelei Ma, Fei Mo, Shengyong Yang, Junhong Han, Xiawei Wei

Signal Transduction and Targeted Therapy · 2019 · ▲ 1,100 citations

Epigenetic alterations Human Preclinical / animal Review

Abstract

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.

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Provenance

Source: OpenAlex
DOI: 10.1038/s41392-019-0095-0
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Fetched: 2026-06-14 MST

Cite this

APA

Cheng, Y., Cai, H., Wang, M., Ma, X., Mo, F., Yang, S., Han, J., & Wei, X. (2019). Targeting epigenetic regulators for cancer therapy: mechanisms and advances in clinical trials. <em>Signal Transduction and Targeted Therapy</em>. https://doi.org/10.1038/s41392-019-0095-0

Vancouver

Cheng Y, Cai H, Wang M, Ma X, Mo F, Yang S, et al. Targeting epigenetic regulators for cancer therapy: mechanisms and advances in clinical trials. Signal Transduction and Targeted Therapy. 2019. doi:10.1038/s41392-019-0095-0.

BibTeX

@article{yuan2019Target, title = {Targeting epigenetic regulators for cancer therapy: mechanisms and advances in clinical trials}, author = {Yuan Cheng and He Cai and Manni Wang and Xuelei Ma and Fei Mo and Shengyong Yang and Junhong Han and Xiawei Wei}, journal = {Signal Transduction and Targeted Therapy}, year = {2019}, doi = {10.1038/s41392-019-0095-0}, }