一种铱（III）配合物抑制JMJD2活性并作为潜在的表观遗传调节剂。
An Iridium(III) Complex Inhibits JMJD2 Activities and Acts as a Potential Epigenetic Modulator.
作者信息
Liu Li-Juan, Lu Lihua, Zhong Hai-Jing, He Bingyong, Kwong Daniel W J, Ma Dik-Lung, Leung Chung-Hang
机构信息
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau , Taipa, Macao P. R. China.
Department of Chemistry, Hong Kong Baptist University , Kowloon Tong, Hong Kong P. R. China.
出版信息
J Med Chem. 2015 Aug 27;58(16):6697-703. doi: 10.1021/acs.jmedchem.5b00375. Epub 2015 Aug 11.
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.
合成了一种新型铱（III）配合物，并对其靶向JMJD2酶活性的能力进行了评估。铱（III）配合物1能够抑制JMJD2活性，并且相对于JARID、JMJD3和HDAC活性而言，对JMJD2活性具有选择性。此外，1抑制了人细胞中p21启动子在H3K9me3位点的三甲基化，并中断了JMJD2D与H3K9me3之间的相互作用，这表明它可以作为一种表观遗传调节剂。据我们所知，1是文献中报道的首个基于金属的JMJD2抑制剂。
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