Covalent inhibitors of LgtC: A blueprint for the discovery of non-substrate-like inhibitors for bacterial glycosyltransferases.

@article{Xu2017CovalentIO,
  title={Covalent inhibitors of LgtC: A blueprint for the discovery of non-substrate-like inhibitors for bacterial glycosyltransferases.},
  author={Yong Xu and R Daron Smith and Mirella Vivoli and Masaki Ema and Niina Goos and Sebastian S. Gehrke and Nicholas J Harmer and Gerd K Wagner},
  journal={Bioorganic & medicinal chemistry},
  year={2017},
  volume={25 12},
  pages={3182-3194}
}
Non-substrate-like inhibitors of glycosyltransferases are sought after as chemical tools and potential lead compounds for medicinal chemistry, chemical biology and drug discovery. Here, we describe the discovery of a novel small molecular inhibitor chemotype for LgtC, a retaining α-1,4-galactosyltransferase involved in bacterial lipooligosaccharide biosynthesis. The new inhibitors, which are structurally unrelated to both the donor and acceptor of LgtC, have low micromolar inhibitory activity… CONTINUE READING