A fluoro analogue of the menadione derivative 6-[2'-(3'-methyl)-1',4'-naphthoquinolyl]hexanoic acid is a suicide substrate of glutathione reductase. Crystal structure of the alkylated human enzyme.

@article{Bauer2006AFA,
  title={A fluoro analogue of the menadione derivative 6-[2'-(3'-methyl)-1',4'-naphthoquinolyl]hexanoic acid is a suicide substrate of glutathione reductase. Crystal structure of the alkylated human enzyme.},
  author={Holger Bauer and Karin Fritz-Wolf and Andreas Winzer and Sebastian K{\"u}hner and Susan Little and Vanessa Yardley and Herv{\'e} Vezin and Bruce Allan Palfey and R. Heiner Schirmer and Elisabeth Davioud-Charvet},
  journal={Journal of the American Chemical Society},
  year={2006},
  volume={128 33},
  pages={10784-94}
}
Glutathione reductase is an important housekeeping enzyme for redox homeostasis both in human cells and in the causative agent of tropical malaria, Plasmodium falciparum. Glutathione reductase inhibitors were shown to have anticancer and antimalarial activity per se and to contribute to the reversal of drug resistance. The development of menadione chemistry has led to the selection of 6-[2'-(3'-methyl)-1',4'-naphthoquinolyl]hexanoic acid, called M(5), as a potent reversible and uncompetitive… CONTINUE READING
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