5 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

You might also like
Discover & Discuss Important Research

Keeping up-to-date with research can feel impossible, with papers being published faster than you'll ever be able to read them. That's where Researcher comes in: we're simplifying discovery and making important discussions happen. With over 19,000 sources, including peer-reviewed journals, preprints, blogs, universities, podcasts and Live events across 10 research areas, you'll never miss what's important to you. It's like social media, but better. Oh, and we should mention - it's free.

  • Download from Google Play
  • Download from App Store
  • Download from AppInChina

Researcher displays publicly available abstracts and doesn’t host any full article content. If the content is open access, we will direct clicks from the abstracts to the publisher website and display the PDF copy on our platform. Clicks to view the full text will be directed to the publisher website, where only users with subscriptions or access through their institution are able to view the full article.