Emerging protein targets for anticancer metallodrugs: inhibition of thioredoxin reductase and cathepsin B by antitumor ruthenium(II)-arene compounds.

@article{Casini2008EmergingPT,
  title={Emerging protein targets for anticancer metallodrugs: inhibition of thioredoxin reductase and cathepsin B by antitumor ruthenium(II)-arene compounds.},
  author={A. L. Casini and Chiara Gabbiani and Francesca Sorrentino and Maria Pia Rigobello and Alberto Bindoli and Tilmann J. Geldbach and Alessandro Marrone and Nazzareno Re and Christian G Hartinger and Paul J Dyson and Luigi Messori},
  journal={Journal of medicinal chemistry},
  year={2008},
  volume={51 21},
  pages={
          6773-81
        }
}
A series of ruthenium(II)-arene (RAPTA) compounds were evaluated for their ability to inhibit thioredoxin reductase (either cytosolic or mitochondrial) and cathepsin B, two possible targets for anticancer metallodrugs. In general, inhibition of the thioredoxin reductases was lower than that of cathepsin B, although selected compounds were excellent inhibitors of both classes of enzymes in comparison to other metal-based drugs. Some initial structure-activity relationships could be established… CONTINUE READING

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