Design and synthesis of an RGD peptidomimetic-paclitaxel conjugate targeting αvβ3 integrin for tumour-directed drug delivery

Monica Piras, Alexandra Andriu, Andrea Testa, Paul Wienecke, Ian N Fleming, Matteo Zanda

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A 1,2,3-triazole-based RGD peptidomimetic having nanomolar affinity for αvβ3 integrin was conjugated to the potent antimitotic paclitaxel via an oxime heterobifunctional linker. The resulting construct maintained nanomolar binding concentration to αvβ3 integrin and showed 11-fold selectivity in terms of cytotoxicity towards highly αvβ3 expressing U87MG cancer cells relative to non αvβ3 expressing MCF7 cells, indicating promising cancer cell targeting capacity.
Original languageEnglish
Pages (from-to)2769-2776
Number of pages8
Issue number20
Early online date1 Sep 2017
Publication statusPublished - 2017



  • RGD
  • peptidomimetic
  • integrin
  • paclitaxel
  • click
  • cytotoxicity
  • cancer

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