Jumonji histone demethylases as emerging therapeutic targets

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• 作者：Sung Yeon Park^a ; Jong-Wan Park^a ; ^b ; Yang-Sook Chun^a ; ^b ; ^c ; ^{chunys@snu.ac.kr" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Jumonji histone demethylases ; Epigenetic regulator ; Cancer ; p53
• 刊名：Pharmacological Research
• 出版年：2016
• 出版时间：March 2016
• 年：2016
• 卷：105
• 期：Complete
• 页码：146-151
• 全文大小：948 K

文摘

The methylation status of lysine residues in histones determines the transcription of surrounding genes by modulating the chromatin architecture. Jumonji domain-containing histone-lysine demethylases (Jmj-KDMs) remove the methyl moiety from lysine residues in histones by utilizing Fe²⁺ and α-ketoglutarate. Since genetic alterations in Jmj-KDMs occur in various human cancers, the roles of Jmj-KDMs in cancer development and progression have been investigated, but still controversial. The KDM7 subfamily, which belongs to the Jmj-KDM family, is an emerging class of transcriptional coactivators because its members erase the repressive marks H3K9me2/1, H3K27me2/1, and H4K20 me1. Recently, KDM7C (alternatively named PHF2) was discovered as a new KDM7 member and identified to play a tumor-suppressive role through the reinforcement of p53-driven growth arrest and apoptosis. In this article, we generally reviewed the roles of Jmj-KDMs in human cancers and more discussed the molecular functions and the clinical significances of KDM7C.