A Rhodium(III)-Based Inhibitor of Lysine-Specific Histone Demethylase 1 as an Epigenetic Modulator in Prostate Cancer Cells

Chao Yang; Wanhe Wang; Jia-Xin Liang; Guodong Li; Kasipandi Vellaisamy; Chun-Yuen Wong; Dik-Lung Ma; Chung-Hang Leung

doi:10.1021/acs.jmedchem.7b00133

Author(s)

Chao Yang
Wanhe Wang
Jia-Xin Liang
Guodong Li
Kasipandi Vellaisamy
Dik-Lung Ma
Chung-Hang Leung

Detail(s)

Original language	English
Pages (from-to)	2597-2603
Journal / Publication	Journal of Medicinal Chemistry
Volume	60
Issue number	6
Publication status	Published - 23 Mar 2017

Link(s)

DOI	DOI https://doi.org/10.1021/acs.jmedchem.7b00133 Final Published version
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Link to Scopus	https://www.scopus.com/record/display.uri?eid=2-s2.0-85016291193&origin=recordpage
Permanent Link	https://scholars.cityu.edu.hk/en/publications/publication(6ae7f7ea-a5ed-420a-b264-ac3c214ef03d).html

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.

Citation Format(s)

[ RIS ] [ BibTeX ]

A Rhodium(III)-Based Inhibitor of Lysine-Specific Histone Demethylase 1 as an Epigenetic Modulator in Prostate Cancer Cells. / Yang, Chao; Wang, Wanhe; Liang, Jia-Xin et al.
In: Journal of Medicinal Chemistry, Vol. 60, No. 6, 23.03.2017, p. 2597-2603.

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

Yang, C, Wang, W, Liang, J-X, Li, G, Vellaisamy, K, Wong, C-Y, Ma, D-L & Leung, C-H 2017, 'A Rhodium(III)-Based Inhibitor of Lysine-Specific Histone Demethylase 1 as an Epigenetic Modulator in Prostate Cancer Cells', Journal of Medicinal Chemistry, vol. 60, no. 6, pp. 2597-2603. https://doi.org/10.1021/acs.jmedchem.7b00133

Yang, C., Wang, W., Liang, J-X., Li, G., Vellaisamy, K., Wong, C-Y., Ma, D-L., & Leung, C-H. (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. https://doi.org/10.1021/acs.jmedchem.7b00133

Yang C, Wang W, Liang J-X, Li G, Vellaisamy K, Wong C-Y 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. 2017 Mar 23;60(6):2597-2603. doi: 10.1021/acs.jmedchem.7b00133

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. In: Journal of Medicinal Chemistry. 2017 ; Vol. 60, No. 6. pp. 2597-2603.