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Rhodium(III)-Based Inhibitor of the JMJD3-H3K27me3 Interaction and Modulator of the Inflammatory Response
Kang, Tian-Shu1; Ko, Chung-Nga2; Zhang, Jia-Tong1; Wu, Chun2; Wong, Chun-Yuen; Ma, Dik-Lung2; Leung, Chung-Hang1,3
2018-11-19
Source PublicationINORGANIC CHEMISTRY
ISSN0020-1669
Volume57Issue:22Pages:14023-14026
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-alpha. To our knowledge, complex 1 is the first metal-based inhibitor of JMJD3 activity and only the second class of JMJD3 inhibitor reported overall.

DOI10.1021/acs.inorgchem.8b02256
URLView the original
Indexed BySCI
Language英语
WOS Research AreaChemistry
WOS SubjectChemistry, Inorganic & Nuclear
WOS IDWOS:000451244700003
PublisherAMER CHEMICAL SOC
Fulltext Access
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Cited Times [WOS]:3   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Res Chinese Med, Macau 519020, Peoples R China;
2.Hong Kong Baptist Univ, Dept Chem, Kowloon Tong 518000, Hong Kong, Peoples R China;
3.City Univ Hong Kong, Dept Chem, Tat Chee Ave, Hong Kong 518000, Hong Kong, Peoples R China
First Author AffilicationUniversity of Macau
Recommended Citation
GB/T 7714
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[J]. INORGANIC CHEMISTRY,2018,57(22):14023-14026.
APA Kang, Tian-Shu.,Ko, Chung-Nga.,Zhang, Jia-Tong.,Wu, Chun.,Wong, Chun-Yuen.,...&Leung, Chung-Hang.(2018).Rhodium(III)-Based Inhibitor of the JMJD3-H3K27me3 Interaction and Modulator of the Inflammatory Response.INORGANIC CHEMISTRY,57(22),14023-14026.
MLA Kang, Tian-Shu,et al."Rhodium(III)-Based Inhibitor of the JMJD3-H3K27me3 Interaction and Modulator of the Inflammatory Response".INORGANIC CHEMISTRY 57.22(2018):14023-14026.
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