title: EZH2, an on-off valve in signal network of tumor cells.
abstract: Enhancer Zeste 2 (EZH2) is a histone methyltransferase catalyzing histone H3K27me3 to mediate gene silence. It is implicated in governing various biological behaviors of human malignancies. In this review, we over-review EZH2 serves as an "on-off valve"--not only as a critical epigenetic repressor, but as a brand-new activator for specific downstream targets as well. Time and space it "switching on-off" depends on the context and its cellular type. Moreover, EZH2 could act as a Tumor-Defender under certain circumstances. Moreover, the "Mutual-Inhibition" relationship between EZH2 and microRNAs is elaborated. In addition, we focus on different functions of phosphorylatied EZH2 in tumor cells. Finally, EZH2 inhibitors are summarized and newly-discovered strategies of targeting-EZH2 treatment are prospected.
authors.affiliation: The Maxillary Facial and Otorhinolaryngology Head & Neck Surgery, Tianjin Medical University Cancer Institute & Hospital, National Clinical Research Center for Cancer, Tianjin Key Laboratory of Cancer Prevention and Therapy, Huanhuxi Road, Tiyuanbei, Hexi District, Tianjin 300060, China.
authors.forename: Shanshan
authors.initials: S
authors.lastname: Sun
authors.affiliation: Department of Tumor Cell Biology, Key Laboratory of Cancer Prevention & Therapy of Tianjin, Tianjin Medical University Cancer Institute & Hospital, National Clinical Research Center for Cancer, Huanhu West Road, Hexi District, Tianjin 300060, China.
authors.forename: Feng
authors.initials: F
authors.lastname: Yu
authors.affiliation: The Maxillary Facial and Otorhinolaryngology Head & Neck Surgery, Tianjin Medical University Cancer Institute & Hospital, National Clinical Research Center for Cancer, Tianjin Key Laboratory of Cancer Prevention and Therapy, Huanhuxi Road, Tiyuanbei, Hexi District, Tianjin 300060, China. Electronic address: lunzhangchina@163.com.
authors.forename: Lun
authors.initials: L
authors.lastname: Zhang
authors.affiliation: The Maxillary Facial and Otorhinolaryngology Head & Neck Surgery, Tianjin Medical University Cancer Institute & Hospital, National Clinical Research Center for Cancer, Tianjin Key Laboratory of Cancer Prevention and Therapy, Huanhuxi Road, Tiyuanbei, Hexi District, Tianjin 300060, China. Electronic address: byron2000zhou@163.com.
authors.forename: Xuan
authors.initials: X
authors.lastname: Zhou
mesh_terms: D000818:Animals; D000071221:Enhancer of Zeste Homolog 2 Protein / Q000378:metabolism / Q000502:physiology*; D015972:Gene Expression Regulation, Neoplastic; D020868:Gene Silencing; D006801:Humans; D051379:Mice; D035683:MicroRNAs / Q000378:metabolism; D009369:Neoplasms / Q000235:genetics* / Q000378:metabolism; D010766:Phosphorylation; D015398:Signal Transduction; D015533:Transcriptional Activation
chemical_list: D035683:MicroRNAs; C498409:EZH2 protein, human; D000071221:Enhancer of Zeste Homolog 2 Protein
keywords: Double facet; EZH2; Histone modulation; Signaling; Tumor