Abstract
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. (Figure Presented).
Original language | English |
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Pages (from-to) | 6697-6703 |
Number of pages | 7 |
Journal | Journal of Medicinal Chemistry |
Volume | 58 |
Issue number | 16 |
DOIs | |
Publication status | Published - 27 Aug 2015 |
Scopus Subject Areas
- Molecular Medicine
- Drug Discovery