Abstract: Methylation is known to be a ubiquitous covalent modification involved in regulation of a diverse range of biomolecules. Histone methyltransferases (HMTs) are of particular interest as drug targets as histone methylation is linked to certain disease states, including a wide variety of cancer types. A high-throughput screening (HTS)-ready, universal methyltransferase activity assay was recently developed based on competitive fluorescent polarization immunodetection of AMP, formed from the methyltransferase (MT) reaction product S-adenosylhomocysteine in a dual enzyme coupling step. This work demonstrates automation of the assay in a 384-well format suitable for HTS.Summary: Epigenetic processes are attracting considerable attention in drug discovery as their fundamental roles in controlling normal cell development and contributions to disease states become more clearly defined. This work combines a fluorescence-based assay with liquid handling and dispensing instrumentation and a multi-mode reader which can be used to monitor the biological activity of the histone methyltransferase (HMT) G9a, a model system.
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