An Iridium(III) Complex Inhibits JMJD2 Activities and Acts as a Potential Epigenetic Modulator
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- 作者：Li-Juan Liu ; Lihua Lu ; Hai-Jing Zhong ; Bingyong He ; Daniel W. J. Kwong ; Dik-Lung Ma ; Chung-Hang Leung
- 刊名：Journal of Medicinal Chemistry
- 出版年：2015
- 出版时间：August 27, 2015
- 年：2015
- 卷：58
- 期：16
- 页码：6697-6703
- 全文大小：293K
- ISSN：1520-4804
文摘
A novel iridium(III) complex was synthesized and evaluated for its ability to target JMJD2 enzymatic activity. The iridium(III) complex 1 can inhibit JMJD2 activity and was selective for JMJD2 activity over JARID, JMJD3, and HDAC activities. Moreover, 1 suppressed the trimethylation of the p21 promoter on H3K9me3 and interrupted the JMJD2D鈥揌3K9me3 interactions in human cells, suggesting that it could act as an epigenetic modulator. To our knowledge, 1 represents the first metal-based JMJD2 inhibitor reported in the literature.