A cell permeable inhibitor of PRMTs
Protein arginine methyltransferases (PRMTs) post-translationally modify proteins, including histones, and in this way regulate gene expression, signal transduction, and protein-protein interactions. AMI-1 is a cell permeable inhibitor of PRMTs. It inhibits both yeast Type I arginine methyltransferase Hmt1p and human PRMT1 (IC50 = 3.0 and 8.8 μM, respectively). AMI-1 also effectively blocks the activity of PRMTs 3, 4, and 6 but not that of either SET (Sub39H1, Suv39H2, SET7) or non-SET (DOT1) lysine methyltransferases. The mechanism of inhibition of PRMTs by AMI-1 involves blocking peptide-substrate binding. AMI-1 also inhibits HIV-1 reverse transcriptase (IC50 = 5.0 μM).
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