Identifying bioisosteres for cationic epigenetic motifs

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This project aims to identify a family of molecules that can generally bind to conserved binding pockets inepigenetic proteins. These molecules (called bioisosteres) would be generally useful starting points forepigenetic drug development efforts, as well as valuable tools for basic research into epigenetic modulators.ChemRoutes has a family of scaffold molecules - called ChemCores - that are potentially well suited to bind toepigenetic methyl reader pockets. The Hof lab at UVic are world leaders in the development of biochemicalassays for binding to such proteins. The proposal is first to establish a panel of fluorescence polarization assaysfor five distinct methyl reader proteins, and then to run three series of proprietary compounds prepared byChemRoutes through the panel of assays. The project will identify novel bioisosteres that ChemRoutes will beable to leverage in further research efforts and partnerships towards epigenetic modulation.