title: The Roles of Histone Demethylase UTX and JMJD3 (KDM6B) in Cancers: Current Progress and Future Perspectives.
abstract: Aberrant epigenetic reprogramming occurs frequently in the development of tumors. Histone H3 lysine 27 trimethylation (H3K27me3) exerts a repressive epigenetic mark on a large number of genes. UTX and JMJD3 are the only two histone demethylases which activate gene expression via demethylating H3K27me3 to H3K27me2 or H3K27me1. Current studies show that dysregulation of these two proteins are heavily linked to oncogenesis in various tissue types. Accumulating evidence suggested that there is remarkable therapeutic potential of targeting JMJD3 or UTX in different types of cancer. Herein, we shall give a brief review on the functional roles of JMJD3 and UTX in cancers and evaluate the available compounds and agents targeting UTX and JMJD3. Finally, we also discuss the several modalities that target UTX and JMJD3 for cancer therapy. This review will help to develop novel strategies to abolish or restore effects of UTX and JMJD3 in the pathogenesis of cancer.
authors.affiliation: Laboratory of Molecular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou, 646000, Sichuan, P.R. China. xzg555898@hotmail.com.
authors.forename: Zhan Gang
authors.initials: ZG
authors.lastname: Xiao
authors.forename: Jing
authors.initials: J
authors.lastname: Shen
authors.forename: Lin
authors.initials: L
authors.lastname: Zhang
authors.forename: Long Fei
authors.initials: LF
authors.lastname: Li
authors.forename: Ming Xing
authors.initials: MX
authors.lastname: Li
authors.forename: Wei
authors.initials: W
authors.lastname: Hu
authors.forename: Zhi Jie
authors.initials: ZJ
authors.lastname: Li
authors.affiliation: Rm 521A, School of Biomedical Sciences, Faculty of Medicine, The Chinese University of Hong Kong, Shatin, N.T., Hong Kong, China. chcho@cuhk.edu.hk.
authors.forename: Chi Hin
authors.initials: CH
authors.lastname: Cho