Rational design of broad spectrum antibacterial activity based on a clinically relevant enoyl-acyl carrier protein (ACP) reductase inhibitor.

@article{Schiebel2014RationalDO,
  title={Rational design of broad spectrum antibacterial activity based on a clinically relevant enoyl-acyl carrier protein (ACP) reductase inhibitor.},
  author={Johannes Schiebel and Andrew S. Chang and Sonam Shah and Yang Lu and Li Liu and Pan Pan and Maria W. Hirschbeck and Mona Tareilus and Sandra Eltschkner and Weixuan Yu and Jason E. Cummings and Susan E. Knudson and Gopal Reddy Bommineni and S. G. Walker and Richard A. Slayden and Christoph A. Sotriffer and Peter J. Tonge and Caroline Kisker},
  journal={The Journal of biological chemistry},
  year={2014},
  volume={289 23},
  pages={15987-6005}
}
Determining the molecular basis for target selectivity is of particular importance in drug discovery. The ideal antibiotic should be active against a broad spectrum of pathogenic organisms with a minimal effect on human targets. CG400549, a Staphylococcus-specific 2-pyridone compound that inhibits the enoyl-acyl carrier protein reductase (FabI), has recently been shown to possess human efficacy for the treatment of methicillin-resistant Staphylococcus aureus infections, which constitute a… CONTINUE READING