Toxicological profile and safety pharmacology of a single dose of fibroblast activation protein-α-based doxorubicin prodrug: in-vitro and in-vivo evaluation.

@article{Huang2018ToxicologicalPA,
  title={Toxicological profile and safety pharmacology of a single dose of fibroblast activation protein-α-based doxorubicin prodrug: in-vitro and in-vivo evaluation.},
  author={Sichao Huang and Yuchen Zhang and Jinsong Zhong and Ying Chun Pan and Shaohui Cai and Jun Xu},
  journal={Anti-cancer drugs},
  year={2018},
  volume={29 3},
  pages={
          253-261
        }
}
Fibroblast activation protein-α (FAPα) is a promising tumor-associated target expressed by reactive stromal fibroblasts in tumor tissue. FAPα has a postprolyl peptidase activity and can specifically cleave N-terminal benzyloxycarbonyl (Z)-blocked peptides, such as the substrate Z-Gly-Pro-AMC. Doxorubicin (DOX) is an effective antitumor drug, but its application is greatly limited by toxic adverse effects owing to poor tumor selectivity. Based on these facts, we previously designed a FAP… CONTINUE READING

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