Chloroacetamidine based inhibitors and activity based probes for the protein arginine methytransferases
AssigneeUniversity of South Carolina
InventorsPaul R. Thompson, Tanesha C. Osborne, Obiamaka Obianyo, Corey P. Causey
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Abstract
In accordance with certain embodiments of the present disclosure, a protein arginine methyltransferase inhibitor is provided. The inhibitor comprises an amino acid peptide joined to a chloroacetamidine warhead.
Claims4
A method of identifying a protein arginine methyltransferase inhibitor comprising incubating protein arginine methyltransferase with one or more activity-based protein profiling reagents, at least one reagent comprising peptide joined to a chloroacetamidine warhead, wherein the peptide comprises the first 21 amino acids of histone H4, the reagent further comprising a fluorescent molecule.
A method of inhibiting protein arginine methyltransferase comprising exposing protein arginine methyltransferase to an inhibitor comprising an amino acid peptide joined to a chloroacetamidine warhead, wherein the peptide comprises the first 21 amino acids of histone H4.
Dependencies are inferred from the claim text.