EGF Receptor-Targeting Peptide Conjugate Incorporating a Near-IR Fluorescent Dye and a Novel 1,4,7-Triazacyclononane-Based ^sup 64^Cu(II) Chelator Assembled via Click Chemistry

EGF Receptor-Targeting Peptide Conjugate Incorporating a Near-IR Fluorescent Dye and a Novel 1,4,7-Triazacyclononane-Based ^sup 64^Cu(II) Chelator Assembled via Click Chemistry

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 deprot...

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Veröffentlicht in:Bioconjugate chemistry 2014-05, Vol.25 (5), p.1011
Hauptverfasser: Viehweger, Katrin, Barbaro, Lisa, García, Karina Pombo, Joshi, Tanmaya, Geipel, Gerhard, Steinbach, Jörg, Stephan, Holger, Spiccia, Leone, Graham, Bim
Format: Artikel
Sprache:eng
Schlagworte:
Cancer
Crystallography
Fluorescence
Phosphorylation
Radioactivity
Tomography
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Zusammenfassung: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
ISSN:1043-1802
1520-4812