期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 8, 期 8, 页码 869-874出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.7b00220
关键词
Epigenetics; histone demethylase; KDM4; JMJD2; synthesis; cancer
Histone lysine demethylases (KDMs) play a vital role in the regulation of chromatin-related processes. Herein, we describe our discovery of a series of potent KDM4 inhibitors that are both cell permeable and antiproliferative in cancer models. The modulation of histone H3K9me3 and H3K36me3 upon compound treatment was verified by homogeneous time-resolved fluorescence assay and by mass spectroscopy detection. Optimization of the series using structure-based drug design led to compound 6 (QC6352), a potent KDM4 family inhibitor that is efficacious in breast and colon cancer PDX models.
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