An Iridium(III) Complex Inhibits JMJD2 Activities and Acts as a Potential Epigenetic Modulator

Li Juan Liu, Lihua Lu, Hai Jing Zhong, Bingyong He, Daniel W J KWONG, Edmond Dik Lung MA*, Chung Hang Leung

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

47 Citations (Scopus)

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 languageEnglish
Pages (from-to)6697-6703
Number of pages7
JournalJournal of Medicinal Chemistry
Volume58
Issue number16
DOIs
Publication statusPublished - 27 Aug 2015

Scopus Subject Areas

  • Molecular Medicine
  • Drug Discovery

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