AS3MT: Inhibitors Conference

Rosen, BP, Dong, H, Packianathan, C et al. (2016). AS3MT: Inhibitors . 402-403. 10.1201/b20466-188

cited authors

  • Rosen, BP; Dong, H; Packianathan, C; Madegowda, M

authors

abstract

  • Modulators of hAS3MT activity may be useful for prevention or treatment of arsenic-related diseases. Using a new high-throughput assay for hAS3MT, we identified ten novel noncompetitive small molecule inhibitors. In silico docking analysis indicate that the inhibitors bind in a cleft distant from the As(III) or SAM binding sites, implying the presence of a regulatory site. Newer bisubstrate inhibitors are being developed that will bridge the SAM and As(III) binding sites. These inhibitors may be useful tools for research in arsenic metabolism and are the starting-point for development of drugs against hAS3MT.

publication date

  • January 1, 2016

Digital Object Identifier (DOI)

start page

  • 402

end page

  • 403