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An Iridium(III) Complex Inhibits JMJD2 Activities and Acts as a Potential Epigenetic Modulator
Liu L.-J.1; Lu L.2; Zhong H.-J.1; He B.2; Kwong D.W.J.2; Ma D.-L.2; Leung C.-H.1
2015
Source PublicationJournal of Medicinal Chemistry
ISSN222623
Volume58Issue:16Pages:6697
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). © 2015 American Chemical Society.

DOI10.1021/acs.jmedchem.5b00375
URLView the original
Indexed BySCIE
Language英語English
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000360415800029
The Source to ArticleScopus
Scopus ID2-s2.0-84940539379
Fulltext Access
Citation statistics
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorMa D.-L.; Leung C.-H.
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Taipa, Macao P. R. China
2.Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong P. R. China
First Author AffilicationInstitute of Chinese Medical Sciences
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Liu L.-J.,Lu L.,Zhong H.-J.,et al. An Iridium(III) Complex Inhibits JMJD2 Activities and Acts as a Potential Epigenetic Modulator[J]. Journal of Medicinal Chemistry, 2015, 58(16), 6697.
APA Liu L.-J.., Lu L.., Zhong H.-J.., He B.., Kwong D.W.J.., Ma D.-L.., & Leung C.-H. (2015). An Iridium(III) Complex Inhibits JMJD2 Activities and Acts as a Potential Epigenetic Modulator. Journal of Medicinal Chemistry, 58(16), 6697.
MLA Liu L.-J.,et al."An Iridium(III) Complex Inhibits JMJD2 Activities and Acts as a Potential Epigenetic Modulator".Journal of Medicinal Chemistry 58.16(2015):6697.
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