Targeting cell surface alpha(v)beta(3) integrin increases therapeutic efficacies of a legumain protease-activated auristatin prodrug.

@article{Liu2012TargetingCS,
  title={Targeting cell surface alpha(v)beta(3) integrin increases therapeutic efficacies of a legumain protease-activated auristatin prodrug.},
  author={Yuan Sophie Liu and Krishna Mohan Bajjuri and Cheng Liu and Subhash C Sinha},
  journal={Molecular pharmaceutics},
  year={2012},
  volume={9 1},
  pages={
          168-75
        }
}
Novel monomethylauristatin E (MMAE) prodrug 8 was designed and prepared that bound cell surface glycoprotein integrin αvβ3, and was activated using legumain protease as a catalyst. Upon activation, prodrug 8 strongly induced the death of MDA-MB-435 cells that express integrin αvβ3 on cell surface. Efficacies of prodrug 8 were also determined in vivo using animal models of 4T1 murine breast cancer, D121 Lewis lung carcinoma, and MDA-MB-435 human breast cancer. The results demonstrated that… CONTINUE READING

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