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Article Dans Une Revue Chemistry - A European Journal Année : 2020

Synthesis and Biological Characterization of Monomeric and Tetrameric RGD‐Cryptophycin Conjugates

Adina Borbély
  • Fonction : Auteur
Eduard Figueras
  • Fonction : Auteur
Malika Kadri
  • Fonction : Auteur
Jean-Luc Coll
Norbert Sewald
  • Fonction : Auteur
  • PersonId : 1077858

Résumé

The effective delivery of cytotoxic agents to the tumor cells is a key challenge in anticancer therapy. Multivalent integrinspecific ligands are considered a promising tool to increase the binding affinity, selectivity, and internalization efficiency of small molecule-drug conjugates. Here we report the synthesis and biological evaluation of a multimeric conjugate containing the high-affinity integrin αvβ3binding ligand RAFT-c(RGDfK)4, a lysosomally cleavable Val-Cit linker and cryptophycin-55 glycinate, a potent inhibitor of tubulin polymerization. In vitro cytotoxicity assays verified that the multimeric RGD-cryptophycin conjugate displays improved potency compared to the monomeric analogue in integrin αvβ3overexpressing tumor cell lines, while significantly reduced activity was observed in the antigen-negative cell line
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Dates et versions

hal-02565761 , version 1 (24-09-2020)

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Adina Borbély, Fabien Thoreau, Eduard Figueras, Malika Kadri, Jean-Luc Coll, et al.. Synthesis and Biological Characterization of Monomeric and Tetrameric RGD‐Cryptophycin Conjugates. Chemistry - A European Journal, 2020, 26 (12), pp.2602-2605. ⟨10.1002/chem.201905437⟩. ⟨hal-02565761⟩
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