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EZH1/2 as targets for cancer therapy

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Abstract

The enhancer of zeste homolog 2 (EZH2) and its highly related homolog EZH1 are considered to be epigenetic silencing factors, and they play key roles in the growth and differentiation of cells as the core components of polycomb repressive complex 2 (PRC2). EZH1 and EZH2 are known to have a role in human malignancies, and alterations in these two genes have been implicated in transformation of human malignancies. Inhibition of EZH1/2 has been shown to result in tumor regression in humans and has been studied and evaluated in the preclinical setting and in multiple clinical trials at various levels. Our work thus contributes to the understanding of the relationship between regulatory molecules associated with EZH1/2 proteins and tumor progression, and may provide new insights for mechanism-based EZH1/2-targeted therapy in tumors.

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Fig. 1: The structure of EZH1 and EZH2.
Fig. 2: The function of EZH1 and EZH2.
Fig. 3: Expression levels of EZH1 in TCGA database.
Fig. 4: EZH1 in oncology.
Fig. 5: Expression levels of EZH2 in human tumors.
Fig. 6: EZH2 in oncology.
Fig. 7: EZH2 inhibitors in early studies.
Fig. 8: EZH1/2 inhibitors in early studies.

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Acknowledgements

This study was supported by research funding from National Natural Science Foundation of China (No. 82073895, 82073864), Science and Technology Planning Project of Guangzhou (No. 202002030294), Basic and Applied Basic Research Foundation of Guangdong (No. 2021A1515220126, 2018B030311020). In addition, thanks are given to all contributors in this field.

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RA was responsible for writing and revising the paper. RA, Y-QL and Y-LL contributed to data collection. Specially, all TCGA data analysis was provided by Y-QL. ZL was responsible for reviewing and directing the writing of the article. All authors approved the final manuscript for submission.

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Correspondence to Zhong Liu.

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An, R., Li, YQ., Lin, YL. et al. EZH1/2 as targets for cancer therapy. Cancer Gene Ther (2022). https://doi.org/10.1038/s41417-022-00555-1

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