An iridium(III) complex inhibits JMJD2 activities and acts as a potential epigenetic modulator
Department of Chemistry
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, L., Lu, L., Zhong, H., He, B., Kwong, W., Ma, D., & Leung, C. (2015). An iridium(III) complex inhibits JMJD2 activities and acts as a potential epigenetic modulator. Journal of Medicinal Chemistry, 58 (16). https://doi.org/10.1021/acs.jmedchem.5b00375