Sinefungin | Methyltransferase inhibitor

Sinefungin (58944-73-3) is a nucleoside S-adenosyl-1-methionine analog. Potent, competitive methyltransferase (protein, DNA, and RNA methyltransferases) inhibitor.^1,2 IC₅₀ < 1.0 and 2.5 μM for PRMT1 and SET7/9, respectively.³ Sinefungin binds with greater affinity to the adenine-specific DNA methyltransferase M.TaqI than S-adenosyl-L-homocysteine.⁴ Inhibits biofilm formation by Streptococcus pneumoniae.⁵

References/Citations

1) Barbes et al. (1990), Effects of sinefungin and S-adenosylhomocysteine on DNA and protein methyltransferases from Streptomyces and other bacteria;  FEMS Microbiol. Lett., 57 239
2) Yebra et al. (1991), The effect of sinefungin and synthetic analogues on RNA and DNA methyltransferases from Streptomyces;  J. Antibiot. (Tokyo), 44 1141
3) Cheng et al. (2004), Small molecule regulators of protein arginine methyltransferases;  J. Biol. Chem., 279 23892
4) Schluckebier et al. (1997), Differential binding of S-andeosylmethionine S-adenosylhomocysteine and Sinefungin to adenine-specific DNA methyltransferase M. TaqI;  J. Mol. Biol., 265 56
5) Yadav et al. (2014), Sinefungin, a natural nucleoside analogue of S-adenosylmethionine, inhibits Streptococcus pneumonia biofilm growth;  Biomed. Res. Int., 2014 156987