@article{22ba5625bd5e420fb43b8937fb3dc045,
title = "An Iridium(III) Complex Inhibits JMJD2 Activities and Acts as a Potential Epigenetic Modulator",
abstract = "A novel iridium(III) complex was synthesized and evaluated for its ability to target JMJD2 enzymatic activity. The iridium(III) complex 1 can inhibit JMJD2 activity and was selective for JMJD2 activity over JARID, JMJD3, and HDAC activities. Moreover, 1 suppressed the trimethylation of the p21 promoter on H3K9me3 and interrupted the JMJD2D-H3K9me3 interactions in human cells, suggesting that it could act as an epigenetic modulator. To our knowledge, 1 represents the first metal-based JMJD2 inhibitor reported in the literature. (Figure Presented).",
author = "Liu, {Li Juan} and Lihua Lu and Zhong, {Hai Jing} and Bingyong He and Kwong, {Daniel W. J.} and Ma, {Dik Lung} and Leung, {Chung Hang}",
note = "Funding information: This work is supported by Hong Kong Baptist University (FRG2/14-15/004), Centre for Cancer and Inflammation Research, School of Chinese Medicine (CCIR-SCM, HKBU), the Health and Medical Research Fund (HMRF/13121482 and HMRF/14130522), the Research Grants Council (HKBU/201811, HKBU/204612, and HKBU/201913), the French National Research Agency/Research Grants Council Joint Research Scheme (A-HKBU201/12 - Oligoswitch), Interdisciplinary Research Matching Scheme (RC-IRMS/14-15/06), the Science and Technology Development Fund, Macao SAR (103/2012/A3 and 098/2014/A2), and the University of Macau (MYRG091(Y3-L2)-ICMS12-LCH, MYRG2015-00137-ICMS-QRCM, and MRG023/LCH/2013/ICMS). Publisher copyright: {\textcopyright} 2015 American Chemical Society",
year = "2015",
month = aug,
day = "27",
doi = "10.1021/acs.jmedchem.5b00375",
language = "English",
volume = "58",
pages = "6697--6703",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "16",
}
