The discovery of inhibitors of methyl- and acetyl-binding domains has provided evidence for the “druggability” of epigenetic effector molecules. Using a library of biotin-tagged analogs we screened a protein domain microarray of methyl-lysine effector molecules to rapidly detect compounds with novel binding profiles - either improved or loosened specificity. Using this approach, we identified compounds that acquired novel interactions with Tudor domain-and MBT domain-containing proteins.

Sympathy for the methyl: a library-on-library screening approach to identify small-molecule ligands of methyl-lysine reader proteins

SBARDELLA, Gianluca
2017-01-01

Abstract

The discovery of inhibitors of methyl- and acetyl-binding domains has provided evidence for the “druggability” of epigenetic effector molecules. Using a library of biotin-tagged analogs we screened a protein domain microarray of methyl-lysine effector molecules to rapidly detect compounds with novel binding profiles - either improved or loosened specificity. Using this approach, we identified compounds that acquired novel interactions with Tudor domain-and MBT domain-containing proteins.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11386/4680983
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