1. 'Polymultivalent' Polymer-Peptide Cluster Conjugates for an Enhanced Targeting of Cells Expressing α
- Author
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Damien, Duret, Adrien, Grassin, Maxime, Henry, Thibault, Jacquet, Fabien, Thoreau, Sandrine, Denis-Quanquin, Jean-Luc, Coll, Didier, Boturyn, Arnaud, Favier, and Marie-Thérèse, Charreyre
- Subjects
Drug Delivery Systems ,Microscopy, Confocal ,Polymers ,Cell Line, Tumor ,Cell Adhesion ,Humans ,Integrin alphaVbeta3 ,Ligands ,Peptides ,Peptides, Cyclic - Abstract
A new class of "polymultivalent" ligands combining several ligand clusters and a water-soluble biocompatible polymer is introduced. These original conjugates bear two levels of multivalency. They are prepared by covalent coupling of a controlled number of tetrameric cRGD peptide clusters along a well-defined copolymer synthesized by RAFT polymerization. The presence of multiple copies of peptide clusters on the same polymer backbone resulted in a much-higher relative potency than the free cluster reference. Thanks to the "polymultivalency", up to ∼2 orders of magnitude potency enhancement was reached in a competitive cell adhesion assay (nanomolar-range IC
- Published
- 2017