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A Rhodium(III)-Based Inhibitor of Lysine-Specific Histone Demethylase 1 as an Epigenetic Modulator in Prostate Cancer Cells
Yang, Chao1; Wang, Wanhe2; Liang, Jia-Xin1; Li, Guodong1; Vellaisamy, Kasipandi2; Wong, Chun-Yuen3; Ma, Dik-Lung2; Leung, Chung-Hang1
2017-03-23
Source PublicationJOURNAL OF MEDICINAL CHEMISTRY
ISSN0022-2623
Volume60Issue:6Pages:2597-2603
Abstract

We report herein a novel rhodium(III) complex 1 as a new LSD1 targeting agent and epigenetic modulator. Complex 1 disrupted the interaction of LSD1-H3K4me2 in human prostate carcinoma cells and enhanced the amplification of p21, FOXA2, and BMP2 gene promoters. Complex 1 was selective for LSD1 over other histone demethylases, such as KDM2b, KDM7, and MAO activities, and also showed antiproliferative activity toward human cancer cells. To date, complex 1 is the first metal-based inhibitor of LSD1 activity.

DOI10.1021/acs.jmedchem.7b00133
URLView the original
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000397546000031
PublisherAMER CHEMICAL SOC
The Source to ArticleWOS
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Cited Times [WOS]:28   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorMa, Dik-Lung
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau, China
2.Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong, China
3.Department of Biology and Chemistry, City University of Hong Kong, Tat Chee Avenue, Kowloon, Hong Kong SAR, China
First Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Yang, Chao,Wang, Wanhe,Liang, Jia-Xin,et al. A Rhodium(III)-Based Inhibitor of Lysine-Specific Histone Demethylase 1 as an Epigenetic Modulator in Prostate Cancer Cells[J]. JOURNAL OF MEDICINAL CHEMISTRY,2017,60(6):2597-2603.
APA Yang, Chao.,Wang, Wanhe.,Liang, Jia-Xin.,Li, Guodong.,Vellaisamy, Kasipandi.,...&Leung, Chung-Hang.(2017).A Rhodium(III)-Based Inhibitor of Lysine-Specific Histone Demethylase 1 as an Epigenetic Modulator in Prostate Cancer Cells.JOURNAL OF MEDICINAL CHEMISTRY,60(6),2597-2603.
MLA Yang, Chao,et al."A Rhodium(III)-Based Inhibitor of Lysine-Specific Histone Demethylase 1 as an Epigenetic Modulator in Prostate Cancer Cells".JOURNAL OF MEDICINAL CHEMISTRY 60.6(2017):2597-2603.
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