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




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Reference: Vallis, KA, Lam, PYH, Able, SL et al., (2016). Synthesis and evaluation of an 18F-labeled derivative of F3 for targeting surface expressed nucleolin in cancer and tumor endothelial cells. Journal of Labelled Compounds and Radiopharmaceuticals.Citable link to this page:

 

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

Abstract: Surface overexpression of nucleolin provides an anchor for specific attachment of biomolecules to cancer and angiogenic endothelial cells. The peptide F3 is a high affinity ligand of the nucleolin receptor (NR) thathas been investigated as a carrier to deliver biologically active molecules to tumors for both therapeutic and imaging applications. A site-specifically PEGylated F3 derivative was radiolabeled with [18F] AlF3. Binding affinity and cellular distribution ofthe compound was assessed in tumor (H2N) and tumor endothelial (2H-11) cells. Specific uptake via the NR was demonstrated by siRNA knockdown of nucleolin in both cell lines. Partition and plasma stability of the compound were assessed at 37°C. Enzyme-mediated site-specific modification of F3 to give NODA-PEG-F3 (NP-F3) was achieved. Radiolabeling with [18F] Al-F gave 18F-NP-F3. 18F-NP-F3 demonstrated high affinity for cancer and tumor endothelial cells. SiRNA knockdown of nucleolin resulted in a binding affinity reduction of 50-60 %, confirming cell surface binding via the NR. NP-F3 was stable in serum for 2 h. 18F-NP-F3 is reported as the first 18F-labeled F3 derivative. It was obtained in a site-specific, high-yield and efficient manner, and binds to surface NR in the low nanomolar range suggesting it has potentialas a tumor and angiogenesis tracer.

Publication status:PublishedPeer Review status:Peer reviewedVersion:Publisher's version Funder: Medical Research Council   Funder: Cancer Research UK   Funder: CR-UK/EPSRC Oxford Cancer Imaging Centre   Notes:Copyright © 2016 The Authors. Journal of Labelled Compounds and Radiopharmaceuticals published by John Wiley and Sons, Ltd. This is an open access article under the terms of the Creative Commons Attribution License.

Bibliographic Details

Publisher: Wiley

Publisher Website: http://www.wiley.com/

Journal: Journal of Labelled Compounds and Radiopharmaceuticalssee more from them

Publication Website: http://onlinelibrary.wiley.com/journal/10.1002/(ISSN)1099-1344

Issue Date: 2016-09-04Identifiers

Issn: 1099-1344

Uuid: ef1cf600-0b32-470e-8a79-91e63e4c0c06

Urn: uri:ef1cf600-0b32-470e-8a79-91e63e4c0c06

Pubs-id: pubs:638191 Item Description

Type: journal-article;

Version: Publisher's versionKeywords: nucleolin receptor F3 [18F]Al-F endothelial cells transglutaminase

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Autor: Vallis, KA - Oxford, MSD, Oncology, CRUK-MRC Ox Inst for Radiation Oncology - - - Lam, PYH - - - Able, SL - Oxford, MSD, Oncology

Fuente: https://ora.ox.ac.uk/objects/uuid:ef1cf600-0b32-470e-8a79-91e63e4c0c06



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