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; Dik-Lung Ma; Chung-Hang Leung

doi:10.1021/acs.inorgchem.8b02256

Author(s)

Tian-Shu Kang
Chung-Nga Ko
Jia-Tong Zhang
Chun Wu
Dik-Lung Ma
Chung-Hang Leung

Related Research Unit(s)

Department of Chemistry

Detail(s)

Original language	English
Pages (from-to)	14023-14026
Journal / Publication	Inorganic Chemistry
Volume	57
Issue number	22
Online published	30 Oct 2018
Publication status	Published - 19 Nov 2018

Link(s)

DOI	DOI https://doi.org/10.1021/acs.inorgchem.8b02256 Final Published version
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Link to Scopus	https://www.scopus.com/record/display.uri?eid=2-s2.0-85056174663&origin=recordpage
Permanent Link	https://scholars.cityu.edu.hk/en/publications/publication(0058944a-c5a7-4af7-8007-a4da896ac8f2).html

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.

Citation Format(s)

[ RIS ] [ BibTeX ]

Rhodium(III)-Based Inhibitor of the JMJD3-H3K27me3 Interaction and Modulator of the Inflammatory Response. / Kang, Tian-Shu; Ko, Chung-Nga; Zhang, Jia-Tong et al.

In: Inorganic Chemistry, Vol. 57, No. 22, 19.11.2018, p. 14023-14026.

Research output: Journal Publications and Reviews (RGC: 21, 22, 62) › 21_Publication in refereed journal › peer-review

Kang, T-S, Ko, C-N, Zhang, J-T, Wu, C, Wong, C-Y, Ma, D-L & Leung, C-H 2018, 'Rhodium(III)-Based Inhibitor of the JMJD3-H3K27me3 Interaction and Modulator of the Inflammatory Response', Inorganic Chemistry, vol. 57, no. 22, pp. 14023-14026. https://doi.org/10.1021/acs.inorgchem.8b02256

Kang, T-S., Ko, C-N., Zhang, J-T., Wu, C., Wong, C-Y., Ma, D-L., & Leung, C-H. (2018). Rhodium(III)-Based Inhibitor of the JMJD3-H3K27me3 Interaction and Modulator of the Inflammatory Response. Inorganic Chemistry, 57(22), 14023-14026. https://doi.org/10.1021/acs.inorgchem.8b02256

Kang T-S, Ko C-N, Zhang J-T, Wu C, Wong C-Y, Ma D-L et al. Rhodium(III)-Based Inhibitor of the JMJD3-H3K27me3 Interaction and Modulator of the Inflammatory Response. Inorganic Chemistry. 2018 Nov 19;57(22):14023-14026. Epub 2018 Oct 30. doi: 10.1021/acs.inorgchem.8b02256

Kang, Tian-Shu ; Ko, Chung-Nga ; Zhang, Jia-Tong et al. / Rhodium(III)-Based Inhibitor of the JMJD3-H3K27me3 Interaction and Modulator of the Inflammatory Response. In: Inorganic Chemistry. 2018 ; Vol. 57, No. 22. pp. 14023-14026.