| Literature DB >> 30628724 |
Qipeng Liu1,2,3, Guangyu Wang4,5, Qiaqia Li1,2,6,7, Weihua Jiang1, Jung-Sun Kim1, Rui Wang1, Sen Zhu1, Xiaoju Wang8,9, Lin Yan1,2, Yang Yi1,7,10,11, Lili Zhang1, Qingshu Meng1,7, Chao Li1,6,7, Dongyu Zhao4,5, Yuanyuan Qiao8,9, Yong Li8,9, Demirkan B Gursel12,13, Arul M Chinnaiyan8,9,14,15,16, Kaifu Chen4,5,17, Qi Cao1,7,18.
Abstract
Polycomb group proteins are important epigenetic regulators for cell proliferation and differentiation, organ development, as well as initiation and progression of lethal diseases, including cancer. Upregulated Polycomb group proteins, including Enhancer of zeste homolog 2 (EZH2), promote proliferation, migration, invasion and metastasis of cancer cells, as well as self-renewal of cancer stem cells. In our study, we report that EZH2 and embryonic ectoderm development (EED) indicate respective direct interaction with androgen receptor (AR). In the context of AR-positive prostate cancer, EZH2 and EED regulate AR expression levels and AR downstream targets. More importantly, we demonstrate that targeting EZH2 with the small-molecule inhibitor astemizole in cancer significantly represses the EZH2 and AR expression as well as the neoplastic capacities. These results collectively suggest that pharmacologically targeting EZH2 might be a promising strategy for advanced prostate cancer.Entities:
Keywords: EED; EZH2; androgen receptor; astemizole; prostate cancer
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Year: 2019 PMID： 30628724 DOI： 10.1002/ijc.32118
Source DB: PubMed Journal: Int J Cancer ISSN： 0020-7136 Impact factor: 7.396