Rhodium(III)-Based Inhibitor of the JMJD3-H3K27me3 Interaction and Modulator of the Inflammatory Response

Tian Shu Kang, Chung Nga Ko, Jia Tong Zhang, Chun Wu, Chun Yuen Wong, Edmond Dik Lung MA, Chung Hang Leung*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

7 Citations (Scopus)

Abstract

We describe in this study a rhodium(III) complex 1 as a new JMJD3 inhibitor and proinflammatory mediator. Complex 1 selectively inhibited the demethylation of H3K27me3 over other similar substrates, indicating its selectivity for JMJD3 over other histone demethylases, including JMJD2D and KDM5A. In terms of mechanism, complex 1 inhibited the JMJD3-H3K27me3 interaction in mouse macrophage cells and down-regulated the expression of TNF-α. To our knowledge, complex 1 is the first metal-based inhibitor of JMJD3 activity and only the second class of JMJD3 inhibitor reported overall.

Original languageEnglish
Pages (from-to)14023-14026
Number of pages4
JournalInorganic Chemistry
Volume57
Issue number22
DOIs
Publication statusPublished - 19 Nov 2018

Scopus Subject Areas

  • Physical and Theoretical Chemistry
  • Inorganic Chemistry

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