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Bioconjug Chem. 2016 May 18;27(5):1253-8. doi: 10.1021/acs.bioconjchem.6b00093. Epub 2016 Apr 28.

Tailoring Fluorescent Dyes To Optimize a Hybrid RGD-Tracer.

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Interventional Molecular Imaging Laboratory, Department of Radiology, Leiden University Medical Center , Albinusdreef 2, PO BOX 9600, 2300 RC, Leiden, The Netherlands.
Departments of Urology and Head and Neck Surgery & Oncology, The Netherlands Cancer Institute - Antoni van Leeuwenhoek Hospital , Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands.
Pharmaceutical Radiochemistry, Faculties of Chemistry and Medicine, Technische Universität München , 85748 Garching, Germany.


Quantitative assessment of affinity and kinetics is a critical component in the development of (receptor-targeted) radiotracers. For fluorescent tracers, such an assessment is currently not yet applied, while (small) changes in chemical composition of the fluorescent component might have substantial influence on the overall properties of a fluorescent tracer. Hybrid imaging labels that contain both a radiolabel and a fluorescent dye can be used to evaluate both the affinity (fluorescent label) and the in vivo distribution (radiolabel) of a targeted tracer. We present a hybrid label oriented and matrix-based scoring approach that enabled quantitative assessment of the influence of (overall) charge and lipophilicity of the fluorescent label on the (in vivo) characteristics of αvβ3-integrin targeted tracers. Systematic chemical alterations in the fluorescent dye were shown to result in a clear difference in the in vivo distribution of the different hybrid tracers. The applied evaluation technique resulted in an optimized targeted tracer for αvβ3-integrin, which combined the highest T/M ratio with the lowest uptake in other organs. Obviously this selection concept would also be applicable during the development of other (receptor-targeted) imaging tracers.

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