pH-(low)-insertion-peptide (pHLIP) translocation of membrane impermeable phalloidin toxin inhibits cancer cell proliferation.

@article{An2010pHlowinsertionpeptideT,
  title={pH-(low)-insertion-peptide (pHLIP) translocation of membrane impermeable phalloidin toxin inhibits cancer cell proliferation.},
  author={Ming An and D. P. D. Wijesinghe and Oleg A. Andreev and Yana K. Reshetnyak and Donald M. Engelman},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={2010},
  volume={107 47},
  pages={
          20246-50
        }
}
We find that pH-(low)-insertion-peptide (pHLIP)-facilitated translocation of phalloidin, a cell-impermeable polar toxin, inhibits the proliferation of cancer cells in a pH-dependent fashion. The monomeric pHLIP inserts its C terminus across a membrane under slightly acidic conditions (pH 6-6.5), forming a transmembrane helix. The delivery construct carries phalloidin linked to its inserting C terminus via a disulfide bond that is cleaved inside cells, releasing the toxin. To facilitate delivery… CONTINUE READING
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