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C-7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor (IC50 = 12.8 µM, in vitro).1,2 PRMT1 enzymes transfer a methyl group from S-adenosylmethionine to arginine residues on histones, which leads to transcription.2 PRMT1 is essential for mixed lineage leukemia oncogenic transformation and thus its inhibition is a potential treatment for these aggressive leukemias.3
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1. Current chemical biology approaches to interrogate protein methyltransferases. ACS Chem Biol. 7(3), 443-463 (2012).
2. Virtual screening and biological characterization of novel histone arginine methyltransferase PRMT1 inhibitors. Chem. Med. Chem. 4(1), 69-77 (2009).
3. The pathogenesis of mixed-