Rationally designed selective inhibitors of trypanothione reductase. Phenothiazines and related tricyclics as lead structures.

@article{Benson1992RationallyDS,
  title={Rationally designed selective inhibitors of trypanothione reductase. Phenothiazines and related tricyclics as lead structures.},
  author={T. J. G. Benson and J. H. McKie and Jason P. Garforth and Alexandre P Borges and Alan H. Fairlamb and Kenneth T. Douglas},
  journal={The Biochemical journal},
  year={1992},
  volume={286 ( Pt 1)},
  pages={9-11}
}
Trypanothione reductase, an essential component of the anti-oxidant defences of parasitic trypanosomes and Leishmania, differs markedly from the equivalent host enzyme, glutathione reductase, in the binding site for the disulphide substrate. Molecular modelling of this region suggested that certain tricyclic compounds might bind selectively to trypanothione reductase without inhibiting host glutathione reductase. This was confirmed by testing 30 phenothiazine and tricyclic antidepressants, of… CONTINUE READING

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