Department of Chemistry
An iridium(III) complex inhibits JMJD2 activities and acts as a potential epigenetic modulator
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–H3K9me3 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.
Source Publication Title
Journal of Medicinal Chemistry
American Chemical Society
Link to Publisher's Edition
Liu, Li-Juan, Lihua Lu, Hai-Jing Zhong, Bingyong He, Wei Jing Daniel Kwong, Dik Lung Ma, and Chung-Hang Leung. "An iridium(III) complex inhibits JMJD2 activities and acts as a potential epigenetic modulator." Journal of Medicinal Chemistry 58.16 (2015): 6697-6703.