Design of new acid-activated cell-penetrating peptides for tumor drug delivery

@inproceedings{Yao2017DesignON,
  title={Design of new acid-activated cell-penetrating peptides for tumor drug delivery},
  author={Jia Yao and Yinyun Ma and Wei Zhang and Li Li and Yun Zhang and Li Zhang and Hui Liu and Jing-man Ni and Rui Wang},
  booktitle={PeerJ},
  year={2017}
}
TH(AGYLLGHINLHHLAHL(Aib)HHIL-NH2), a histidine-rich, cell-penetrating peptide with acid-activated pH response, designed and synthesized by our group, can effectively target tumor tissues with an acidic extracellular environment. Since the protonating effect of histidine plays a critical role in the acid-activated, cell-penetrating ability of TH, we designed a series of new histidine substituents by introducing electron donating groups (Ethyl, Isopropyl, Butyl) to the C-2 position of histidine… CONTINUE READING

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