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Al18F-Labeling Of Heat-Sensitive Biomolecules for Positron Emission Tomography Imaging
Theranostics ( IF 12.4 ) Pub Date : 2017-07-14 , DOI: 10.7150/thno.20094
Frederik Cleeren 1 , Joan Lecina 1 , Muneer Ahamed 1 , Geert Raes 2, 3 , Nick Devoogdt 4 , Vicky Caveliers 4 , Paul McQuade 5 , Daniel J Rubins 5 , Wenping Li 5 , Alfons Verbruggen 1 , Catarina Xavier 4 , Guy Bormans 1
Affiliation  

Positron emission tomography (PET) using radiolabeled biomolecules is a translational molecular imaging technology that is increasingly used in support of drug development. Current methods for radiolabeling biomolecules with fluorine-18 are laborious and require multistep procedures with moderate labeling yields. The Al18F-labeling strategy involves chelation in aqueous medium of aluminum mono[18F]fluoride ({Al18F}2+) by a suitable chelator conjugated to a biomolecule. However, the need for elevated temperatures (100-120 °C) required for the chelation reaction limits its widespread use. Therefore, we designed a new restrained complexing agent (RESCA) for application of the AlF strategy at room temperature.

中文翻译:

用于正电子发射断层扫描成像的热敏生物分子的 Al18F 标记

使用放射性标记生物分子的正电子发射断层扫描 (PET) 是一种转化分子成像技术,越来越多地用于支持药物开发。目前用 18 氟放射性标记生物分子的方法非常费力,并且需要多步程序且标记产量适中。Al 18 F-标记策略涉及在水性介质中通过与生物分子缀合的合适螯合剂螯合一[ 18 F]氟化铝({Al 18 F} 2+ )。然而,螯合反应需要升高温度(100-120°C)限制了其广泛使用。因此,我们设计了一种新型受限络合剂(RESCA),用于室温下AlF策略的应用。
更新日期:2017-11-01
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