A PRMT1 inhibitor
C7280948 is a novel PRMT1 inhibitor with IC50 value of 12.75 μM [1].
Protein arginine methyltransferase 1 (PRMT1) is a histone methyltransferase specific for histone H4. PRMT1 catalyzes the transfer of the methyl group from SAM to the guanidine nitrogen atoms of arginine residues to produce monomethyl arginines (MMA) and asymmetric dimethyl arginines (ADMA) [2].
C7280948 is a novel PRMT1 inhibitor. C7280948 interacts with aromatic residues at the hPRMT1 substrate binding pocket (Tyr 147 and Tyr 160) [1]. C7280948 inhibited hPRMT1 with IC50 value of 26.7 μM [3].
参考文献:
[1].? Heinke R, Spannhoff A, Meier R, et al. Virtual screening and biological characterization of novel histone arginine methyltransferase PRMT1 inhibitors. ChemMedChem, 2009, 4(1): 69-77.
[2].? Itoh Y, Suzuki T, Miyata N. Small-molecular modulators of cancer-associated epigenetic mechanisms. Mol Biosyst, 2013, 9(5): 873-896.
[3].? Bissinger EM, Heinke R, Spannhoff A, et al. Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1. Bioorg Med Chem, 2011, 19(12): 3717-3731.
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