3 years ago

“Polymultivalent” Polymer–Peptide Cluster Conjugates for an Enhanced Targeting of Cells Expressing αvβ3 Integrins

“Polymultivalent” Polymer–Peptide Cluster Conjugates for an Enhanced Targeting of Cells Expressing αvβ3 Integrins
Didier Boturyn, Sandrine Denis-Quanquin, Thibault Jacquet, Jean-Luc Coll, Marie-Thérèse Charreyre, Arnaud Favier, Maxime Henry, Damien Duret, Fabien Thoreau, Adrien Grassin
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 IC50 values). In addition, confocal microscopy and flow cytometry demonstrated that fluorescent “polymultivalent” conjugates (emitting in the far-red/near-infrared region) were able to specifically and selectively label cells expressing αvβ3-integrin, the natural receptor of cRGD.

Publisher URL: http://dx.doi.org/10.1021/acs.bioconjchem.7b00362

DOI: 10.1021/acs.bioconjchem.7b00362

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