EZH2 in Cancer Progression and Potential Application in Cancer Therapy: A Friend or Foe?

Ke-Sin Yan; Chia-Yuan Lin; Tan-Wei Liao; Cheng-Ming Peng; Shou-Chun Lee; Yi-Jui Liu; Wing P Chan; Ruey-Hwang Chou

doi:10.3390/ijms18061172

EZH2 in Cancer Progression and Potential Application in Cancer Therapy: A Friend or Foe?

Int J Mol Sci. 2017 May 31;18(6):1172. doi: 10.3390/ijms18061172.

Authors

Ke-Sin Yan¹, Chia-Yuan Lin², Tan-Wei Liao³, Cheng-Ming Peng⁴, Shou-Chun Lee⁵, Yi-Jui Liu^{6

7}, Wing P Chan⁸, Ruey-Hwang Chou^{9

10

11}

Affiliations

¹ Graduate Institute of Biomedical Sciences, China Medical University, No.91, Hsueh-Shih Rd., North Dist., Taichung 40402, Taiwan. n79927@yahoo.com.tw.
² Graduate Institute of Biomedical Sciences, China Medical University, No.91, Hsueh-Shih Rd., North Dist., Taichung 40402, Taiwan. a8760752@hotmail.com.
³ Center for Molecular Medicine, China Medical University Hospital, No. 2, Yude Rd., North Dist., Taichung 40402, Taiwan. dawn770501@hotmail.com.
⁴ Da Vinci Minimally Invasive Surgery Center, Chung Shan Medical University Hospital, No. 110, Sec. 1, Chien-Kuo N. Rd., Taichung 40201, Taiwan. jimy5989@gmail.com.
⁵ Master's Program of Biomedical Informatics and Biomedical Engineering, Feng Chia University, No. 100, Wenhwa Rd., Seatwen Dist., Taichung 40724, Taiwan. cxz82282@gmail.com.
⁶ Master's Program of Biomedical Informatics and Biomedical Engineering, Feng Chia University, No. 100, Wenhwa Rd., Seatwen Dist., Taichung 40724, Taiwan. erliu@fcu.edu.tw.
⁷ Department of Automatic Control Engineering, Feng Chia University, No.100, Wenhwa Rd., Seatwen Dist., Taichung 40724, Taiwan. erliu@fcu.edu.tw.
⁸ Department of Radiology, Wan Fang Hospital, Taipei Medical University, No. 111, Sec. 3, Singlong Rd., Taipei 11696, Taiwan. wingchan@w.tmu.edu.tw.
⁹ Graduate Institute of Biomedical Sciences, China Medical University, No.91, Hsueh-Shih Rd., North Dist., Taichung 40402, Taiwan. rhchou@mail.cmu.edu.tw.
¹⁰ Center for Molecular Medicine, China Medical University Hospital, No. 2, Yude Rd., North Dist., Taichung 40402, Taiwan. rhchou@mail.cmu.edu.tw.
¹¹ Department of Biotechnology, Asia University, No. 500, Lioufeng Rd., Wufeng Dist., Taichung 41354, Taiwan. rhchou@mail.cmu.edu.tw.

Abstract

Enhancer of zeste homolog 2 (EZH2), a histone methyltransferase, catalyzes tri-methylation of histone H3 at Lys 27 (H3K27me3) to regulate gene expression through epigenetic machinery. EZH2 functions as a double-facet molecule in regulation of gene expression via repression or activation mechanisms, depending on the different cellular contexts. EZH2 interacts with both histone and non-histone proteins to modulate diverse physiological functions including cancer progression and malignancy. In this review article, we focused on the updated information regarding microRNAs (miRNAs) and long non coding RNAs (lncRNAs) in regulation of EZH2, the oncogenic and tumor suppressive roles of EZH2 in cancer progression and malignancy, as well as current pre-clinical and clinical trials of EZH2 inhibitors.

Keywords: EZH2; EZH2 inhibitors; cancer; epigenetic regulation; lncRNAs; microRNAs.

Publication types

Review

MeSH terms

Disease Progression
Enhancer of Zeste Homolog 2 Protein / antagonists & inhibitors
Enhancer of Zeste Homolog 2 Protein / genetics*
Enzyme Inhibitors / therapeutic use
Gene Expression Regulation, Neoplastic*
Humans
MicroRNAs / genetics*
Mutation
Neoplasms / drug therapy
Neoplasms / genetics*
Neoplasms / pathology
RNA, Long Noncoding / genetics*
Tumor Suppressor Proteins / genetics

Substances

Enzyme Inhibitors
MicroRNAs
RNA, Long Noncoding
Tumor Suppressor Proteins
EZH2 protein, human
Enhancer of Zeste Homolog 2 Protein