A selective PRMT1 inhibitor and antiprotozoal agent
Furamidine is a cell-permeable inhibitor of protein arginine methyltransferase 1 (PRMT1) that is selective for PRMT1 over PRMT5, PRMT6, and PRMT4/coactivator-associated arginine methyltransferase 1 (CARM1) (IC50s = 9.4, 166, 283, and >400 μM, respectively). In vitro, furamidine (20 μM) inhibits Aly protein methylation in HEK293T cells and growth of several leukemia cell lines. It inhibits tyrosyl-DNA phosphodiesterase (Tdp1) activity on both single- and double-stranded DNA substrates with concentrations in the low micromolar range, but it is more potent against a duplex DNA substrate. Furamidine inhibits growth of T. brucei, the parasite that causes sleeping sickness, with IC50 values of 1.5 to 37 nM across various strains. It inhibits the T. brucei P2 aminopurine transporter (Ki = 1.2 μM). It also binds to AT-rich DNA sequences in trypanosome kinetoplast DNA.
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