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Automation of a Generic Fluorescence Methyltransferase Activity AssayDownload
September 15, 2011
Authors: P. Brescia, M. Todd, P. Banks, BioTek Instruments; Meera Kumar BellBrook Labs
Epigenetic processes are attracting considerable attention in drug discovery as their fundamental roles in controlling normal cell development and contributing to disease states become more clearly defined. 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 some disease states, including a wide variety of cancer types. An HTSready, universal methyltransferase activity assay was recently developed based on fluorescent immunodetection of AMP, formed from the MT reaction product S-adenosylhomocysteine in a dual enzyme coupling step. Here we demonstrate automation of the assay in a 384-well format suitable for HTS while examining assay performance and pharmacology of a HMT.