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.
A “library-on-library” screening approach to identify small-molecule ligands of methyl-lysine reader proteins
SBARDELLA, Gianluca
2016-01-01
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.File in questo prodotto:
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