Identification of amino acids essential for the antiangiogenic activity of tumstatin and its use in combination antitumor activity

@article{Eikesdal2008IdentificationOA,
  title={Identification of amino acids essential for the antiangiogenic activity of tumstatin and its use in combination antitumor activity},
  author={H. P. Eikesdal and H. Sugimoto and G. Birrane and Y. Maeshima and Vesselina G. Cooke and M. Kieran and R. Kalluri},
  journal={Proceedings of the National Academy of Sciences},
  year={2008},
  volume={105},
  pages={15040 - 15045}
}
Tumstatin is an angiogenesis inhibitor that binds to αvβ3 integrin and suppresses tumor growth. Previous deletion mutagenesis studies identified a 25-aa fragment of tumstatin (tumstatin peptide) with in vitro antiangiogenic activity. Here, we demonstrate that systemic administration of this tumstatin peptide inhibits tumor growth and angiogenesis. Site-directed mutagenesis identified amino acids L, V, and D as essential for the antiangiogenic activity of tumstatin. The tumstatin peptide binds… Expand
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