Synthesis and evaluation of an ¹⁸ F-labeled derivative of F3 for targeting surface-expressed nucleolin in cancer and tumor endothelial cells.

ABSTRACT: The surface overexpression of nucleolin provides an anchor for the specific attachment of biomolecules to cancer and angiogenic endothelial cells. The peptide F3 is a high-affinity ligand of the nucleolin receptor (NR) that has been investigated as a carrier to deliver biologically active molecules to tumors for both therapeutic and imaging applications. A site-specific PEGylated F3 derivative was radiolabeled with [¹⁸ F]Al-F. The binding affinity and cellular distribution of the compound was assessed in tumor (H2N) and tumor endothelial (2H-11) cells. Specific uptake via the NR was demonstrated by the siRNA knockdown of nucleolin in both cell lines. The partition and the plasma stability of the compound were assessed at 37°C. The enzyme-mediated site-specific modification of F3

SUBMITTER: Lam PY 

PROVIDER: S-EPMC5082555 | biostudies-literature | 2016 Oct

REPOSITORIES: biostudies-literature