A liquid chromatography/mass spectrometry-based generic detection method for biochemical assay and hit discovery of histone methyltransferases.
2013
Abstract Epigenetic modifications of the genome, such as DNA methylation and
posttranslational modificationsof histone proteins, contribute to gene regulation. Growing evidence suggests that
histone methyltransferasesare associated with the development of various human diseases, including cancer, and are promising drug targets. High-quality generic assays will facilitate
drug discoveryefforts in this area. In this article, we present a
liquid chromatography/mass spectrometry(LC/MS)-based S -adenosyl homocysteine (SAH) detection assay for
histone methyltransferases(HMTs) and its applications in HMT
drug discovery, including analyzing the activity of newly produced enzymes, developing and optimizing assays, performing focused compound library screens and orthogonal assays for hit confirmations, selectivity profiling against a panel of HMTs, and studying mode of action of select hits. This LC/MS-based generic assay has become a critical platform for our
methyltransferase
drug discoveryefforts.
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