The novel arsenical darinaparsin is transported by cystine importing systems.

  title={The novel arsenical darinaparsin is transported by cystine importing systems.},
  author={Nicolas Garnier and Genevi{\`e}ve G J Redstone and Michael S Dahabieh and Jessica N. Nichol and Sonia Victoria del Rinc{\'o}n and Yuxuan Gu and David Scott Bohle and Yan Sun and Douglas S Conklin and Koren Kathleen Mann and Wilson H. Miller},
  journal={Molecular pharmacology},
  volume={85 4},
Darinaparsin (Dar; ZIO-101; S-dimethylarsino-glutathione) is a promising novel organic arsenical currently undergoing clinical studies in various malignancies. Dar consists of dimethylarsenic conjugated to glutathione (GSH). Dar induces more intracellular arsenic accumulation and more cell death than the FDA-approved arsenic trioxide (ATO) in vitro, but exhibits less systemic toxicity. Here, we propose a mechanism for Dar import that might explain these characteristics. Structural analysis of… CONTINUE READING


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