Structural studies of Mycobacterium tuberculosis DprE1 interacting with its inhibitors.

@article{Piton2017StructuralSO,
  title={Structural studies of Mycobacterium tuberculosis DprE1 interacting with its inhibitors.},
  author={J{\'e}r{\'e}mie Piton and Caroline Shi-Yan Foo and Stewart T Cole},
  journal={Drug discovery today},
  year={2017},
  volume={22 3},
  pages={526-533}
}
The flavoenzyme DprE1 catalyses a crucial step in arabinan production for cell wall biosynthesis in Mycobacterium tuberculosis and is a highly vulnerable drug target. It was first discovered using benzothiazinones (BTZ): exquisitely potent bactericidal agents that are being developed as drugs to treat tuberculosis. Subsequently, many compounds with diverse scaffolds were found to act as either covalent or noncovalent DprE1 inhibitors. Covalent inhibitors, like the BTZ, are all nitroaromatic… CONTINUE READING