期刊
BIOCONJUGATE CHEMISTRY
卷 27, 期 5, 页码 1253-1258出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.bioconjchem.6b00093
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资金
- Koningin Wilhelmina Fonds (KWF) translational research award [PGF 2009-4344]
- Netherlands Organization for Scientific Research STW-VIDI grant [STW BGT11272]
- European Research Council under the European Union [2012-306890]
- Post-Doctoral Molecular Imaging Scholar Program Grant - Society of Nuclear Medicine and Molecular imaging (SNMMI)
- Education and Research Foundation for Nuclear Medicine and Molecular Imaging
Qantitative 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 alpha(v)beta(3)-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 alpha(v)beta(3)-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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