EGF receptor-targeting peptide conjugate incorporating a near-IR fluorescent dye and a novel 1,4,7-triazacyclononane-based 64Cu(II) chelator assembled via click chemistry

Katrin Viehweger, Lisa Barbaro, Karina Pombo-Garcia, Tanmaya Joshi, Gerhard Geipel, Jorg Steinbach, Holger Stephan, Leone Spiccia, Bimbil Graham

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20 Citations (Scopus)

Abstract

A new Boc-protected 1,4,7-triazacyclononane (TACN)-based pro-chelator compound featuring a clickable azidomethylpyridine pendant has been developed as a building block for the construction of multimodal imaging agents. Conjugation to a model alkyne (propargyl alcohol), followed by deprotection, generates a pentadentate ligand, as confirmed by X-ray crystallographic analysis of the corresponding distorted square-pyramidal Cu(II) complex. The ligand exhibits rapid 64Cu(II)-binding kinetics (>95 radiochemical yield in
Original languageEnglish
Pages (from-to)1011 - 1022
Number of pages12
JournalBioconjugate Chemistry
Volume25
Issue number5
DOIs
Publication statusPublished - 2014

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