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

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

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Author(s)

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

Detail(s)

Original languageEnglish
Pages (from-to)2597-2603
Journal / PublicationJournal of Medicinal Chemistry
Volume60
Issue number6
Publication statusPublished - 23 Mar 2017

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)

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; Li, Guodong; Vellaisamy, Kasipandi; Wong, Chun-Yuen; Ma, Dik-Lung; Leung, Chung-Hang.

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