Highly water-soluble, near-infrared emissive BODIPY polymeric dye bearing RGD peptide residues for cancer imaging

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Near-infrared emissive BODIPY polymeric dye bearing cancer-homing cyclic arginine–glycine–aspartic acid (RGD) peptide residues (polymer B) was prepared by post-polymerization functionalization of BODIPY polymeric dye bearing bromo groups through tetra(ethylene glycol) tethered spacers (polymer A) with thiol-functionalized RGD cancer-homing peptide through thioether bonds under a mild basic condition. Polymer B possesses excellent water solubility, good photostability, biocompatibility and resistance to nonspecific interactions to normal endothelial cells, and can efficiently detect breast tumor cells through specific cooperative binding of cancer-homing RGD peptides to αvβ3 integrins of cancer cells while its parent polymer A without RGD residues fails to target cancer cells.

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© 2012 Elsevier B.V. All rights reserved. Publisher's version of record: https://doi.org/10.1016/j.aca.2012.10.026

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Analytica Chimica Acta