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, Edmond Dik Lung MA*, Chung Hang Leung

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

38 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)2597-2603
Number of pages7
JournalJournal of Medicinal Chemistry
Volume60
Issue number6
DOIs
Publication statusPublished - 23 Mar 2017

Scopus Subject Areas

  • Molecular Medicine
  • Drug Discovery

Fingerprint

Dive into the research topics of 'A Rhodium(III)-Based Inhibitor of Lysine-Specific Histone Demethylase 1 as an Epigenetic Modulator in Prostate Cancer Cells'. Together they form a unique fingerprint.

Cite this