EZH2: The roles in targeted therapy and mechanisms of resistance in breast cancer

Yun Chen; Hongyan Zhu; Yi Luo; Shuangmei Tong; Yan Liu

doi:10.1016/j.biopha.2024.116624

EZH2: The roles in targeted therapy and mechanisms of resistance in breast cancer

Biomed Pharmacother. 2024 Apr 25:175:116624. doi: 10.1016/j.biopha.2024.116624. Online ahead of print.

Authors

Yun Chen¹, Hongyan Zhu², Yi Luo³, Shuangmei Tong⁴, Yan Liu⁵

Affiliations

¹ Department of Clinical Pharmacy, Xinhua Hospital Affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai 200092, PR China; Clinical Pharmacy Innovation Institute, Shanghai Jiao Tong University School of Medicine, Shanghai 200092, PR China. Electronic address: chenyun0313@sjtu.edu.cn.
² Department of Clinical Pharmacy, Xinhua Hospital Affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai 200092, PR China; Clinical Pharmacy Innovation Institute, Shanghai Jiao Tong University School of Medicine, Shanghai 200092, PR China. Electronic address: zhuhongyan@shsmu.edu.cn.
³ Clinical Pharmacy Innovation Institute, Shanghai Jiao Tong University School of Medicine, Shanghai 200092, PR China; Biotheus Inc., Guangdong Province, Zhuhai 519080, PR China. Electronic address: yluo.sz@gmail.com.
⁴ Department of Clinical Pharmacy, Xinhua Hospital Affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai 200092, PR China; Clinical Pharmacy Innovation Institute, Shanghai Jiao Tong University School of Medicine, Shanghai 200092, PR China. Electronic address: tongshuangmei@xinhuamed.com.cn.
⁵ Department of Clinical Pharmacy, Xinhua Hospital Affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai 200092, PR China; Clinical Pharmacy Innovation Institute, Shanghai Jiao Tong University School of Medicine, Shanghai 200092, PR China. Electronic address: liuyan@shsmu.com.cn.

PMID: 38670045
DOI: 10.1016/j.biopha.2024.116624

Abstract

Drug resistance presents a formidable challenge in the realm of breast cancer therapy. Accumulating evidence suggests that enhancer of zeste homolog 2 (EZH2), a component of the polycomb repressive complex 2 (PRC2), may serve as a key regulator in controlling drug resistance. EZH2 overexpression has been observed in breast cancer and many other malignancies, showing a strong correlation with poor outcomes. This review aims to summarize the mechanisms by which EZH2 regulates drug resistance, with a specific focus on breast cancer, in order to provide a comprehensive understanding of the underlying molecular processes. Additionally, we will discuss the current strategies and outcomes of targeting EZH2 using both single agents and combination therapies, with the goal of offering improved guidance for the clinical treatment of breast cancer patients who have developed drug resistance.

Keywords: Breast cancer; EZH2; Resistance; Targeted therapy.

Publication types

Review