Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 60, Issue 6, Pages 2597-2603Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b00133
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Funding
- Hong Kong Baptist University [FRG2/15-16/002]
- Health and Medical Research Fund [HMRF/14130522]
- Research Grants Council [HKBU/12301115, HKBU/204612,, HKBU/201913]
- French National Research Agency/Research Grants Council Joint Research Scheme [A-HKBU201/12]
- National Natural Science Foundation of China [21575121, 21628502]
- Guangdong Province Natural Science Foundation [2015A030313816]
- Hong Kong Baptist University Century Club Sponsorship Scheme
- Interdisciplinary Research Matching Scheme [RCIRMS/15-16/03]
- Science and Technology Development Fund
- Macao SAR [098/2014/A2]
- University of Macau [MYRG2015-00137-ICMS-ARCM, MYRG2016-00151-ICMS-ARCM, MRG044/LCH/2015/ ICMS]
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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.
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