Duret, D;
Grassin, A;
Henry, M;
Jacquet, T;
Thoreau, F;
Denis-Quanquin, S;
Coll, J-L;
... Charreyre, M-T; + view all
(2017)
"Polymultivalent" Polymer-Peptide Cluster Conjugates for an Enhanced Targeting of Cells Expressing alpha(v)beta(3) Integrins.
Bioconjugate Chemistry
, 28
(9)
pp. 2241-2245.
10.1021/acs.bioconjchem.7b00362.
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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 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.
| Type: | Article |
|---|---|
| Title: | "Polymultivalent" Polymer-Peptide Cluster Conjugates for an Enhanced Targeting of Cells Expressing alpha(v)beta(3) Integrins |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1021/acs.bioconjchem.7b00362 |
| Publisher version: | https://doi.org/10.1021/acs.bioconjchem.7b00362 |
| Language: | English |
| Additional information: | This version is the author accepted manuscript. For information on re-use, please refer to the publisher’s terms and conditions. |
| Keywords: | Science & Technology, Life Sciences & Biomedicine, Physical Sciences, Biochemical Research Methods, Biochemistry & Molecular Biology, Chemistry, Multidisciplinary, Chemistry, Organic, Chemistry, FRAGMENTATION CHAIN TRANSFER, RGD PEPTIDES, RAFT PROCESS, MULTIVALENT, BINDING, ANGIOGENESIS, AFFINITY, THERAPY, LIGANDS |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > UCL BEAMS UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences > Dept of Chemistry |
| URI: | https://discovery.ucl.ac.uk/id/eprint/10092112 |
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