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

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^*

^*Corresponding author for this work

Department of Chemistry

Research output: Contribution to journal › Journal article › peer-review

73 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 language	English
Pages (from-to)	2597-2603
Number of pages	7
Journal	Journal of Medicinal Chemistry
Volume	60
Issue number	6
Early online date	1 Mar 2017
DOIs	https://doi.org/10.1021/acs.jmedchem.7b00133
Publication status	Published - 23 Mar 2017

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10.1021/acs.jmedchem.7b00133

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

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.",

author = "Chao Yang and Wanhe Wang and Liang, \{Jia Xin\} and Guodong Li and Kasipandi Vellaisamy and Wong, \{Chun Yuen\} and Ma, \{Dik Lung\} and Leung, \{Chung Hang\}",

note = "Funding Information: This work is supported by Hong Kong Baptist University (Grant FRG2/15-16/002), the Health and Medical Research Fund (Grant HMRF/14130522), the Research Grants Council (Grants HKBU/12301115, HKBU/204612, and HKBU/201913), the French National Research Agency/Research Grants Council Joint Research Scheme (Grant A-HKBU201/12, Oligoswitch), National Natural Science Foundation of China (Grant 21575121), Guangdong Province Natural Science Foundation (Grant 2015A030313816), Hong Kong Baptist University Century Club Sponsorship Scheme 2016, Interdisciplinary Research Matching Scheme (Grant RC-IRMS/15-16/03), the Science and Technology Development Fund, Macao SAR (Grant 098/2014/A2), the University of Macau (Grants MYRG2015-00137-ICMS-QRCM, MYRG2016-00151-ICMS-QRCM, and MRG044/LCH/2015/ICMS), and National Natural Science Foundation of China (Grant 21628502). Publisher copyright: {\textcopyright} 2017 American Chemical Society",

year = "2017",

month = mar,

day = "23",

doi = "10.1021/acs.jmedchem.7b00133",

language = "English",

volume = "60",

pages = "2597--2603",

journal = "Journal of Medicinal Chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

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T1 - A Rhodium(III)-Based Inhibitor of Lysine-Specific Histone Demethylase 1 as an Epigenetic Modulator in Prostate Cancer Cells

AU - Yang, Chao

AU - Wang, Wanhe

AU - Liang, Jia Xin

AU - Li, Guodong

AU - Vellaisamy, Kasipandi

AU - Wong, Chun Yuen

AU - Ma, Dik Lung

AU - Leung, Chung Hang

N1 - Funding Information: This work is supported by Hong Kong Baptist University (Grant FRG2/15-16/002), the Health and Medical Research Fund (Grant HMRF/14130522), the Research Grants Council (Grants HKBU/12301115, HKBU/204612, and HKBU/201913), the French National Research Agency/Research Grants Council Joint Research Scheme (Grant A-HKBU201/12, Oligoswitch), National Natural Science Foundation of China (Grant 21575121), Guangdong Province Natural Science Foundation (Grant 2015A030313816), Hong Kong Baptist University Century Club Sponsorship Scheme 2016, Interdisciplinary Research Matching Scheme (Grant RC-IRMS/15-16/03), the Science and Technology Development Fund, Macao SAR (Grant 098/2014/A2), the University of Macau (Grants MYRG2015-00137-ICMS-QRCM, MYRG2016-00151-ICMS-QRCM, and MRG044/LCH/2015/ICMS), and National Natural Science Foundation of China (Grant 21628502). Publisher copyright: © 2017 American Chemical Society

PY - 2017/3/23

Y1 - 2017/3/23

N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/85016291193

U2 - 10.1021/acs.jmedchem.7b00133

DO - 10.1021/acs.jmedchem.7b00133

M3 - Journal article

C2 - 28219005

AN - SCOPUS:85016291193

SN - 0022-2623

VL - 60

SP - 2597

EP - 2603

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 6

ER -

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

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