TY - JOUR
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 - http://www.scopus.com/inward/record.url?scp=85016291193&partnerID=8YFLogxK
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 -
