In Vivo Albumin‐Binding of a C‐Functionalized Cyclam Platform for 64Cu‐PET/CT Imaging in Breast Cancer Model,ChemMedChem

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In Vivo Albumin‐Binding of a C‐Functionalized Cyclam Platform for 64Cu‐PET/CT Imaging in Breast Cancer Model
ChemMedChem ( IF 3.6 ) Pub Date : 2020-11-15 , DOI: 10.1002/cmdc.202000800
Thomas Le Bihan ₁ , Cathryn H S Driver ₂ , Thomas Ebenhan ₂ , Nathalie Le Bris ₁ , Jan Rijn Zeevaart ₂ , Raphaël Tripier ₁

Affiliation

An improved glucose‐chelator‐albumin bioconjugate (GluCAB) derivative, GluCAB‐2^Mal, has been synthesized and studied for in vivo ⁶⁴Cu‐PET/CT imaging in breast cancer mice models together with its first‐generation analogue GluCAB‐1^Mal. The radioligand works on the principle of tumor targeting through the enhanced permeability and retention (EPR) effect with a supportive role played by glucose metabolism. [⁶⁴Cu]Cu‐GluCAB‐2^Mal (99 % RCP) exhibited high serum stability with immediate binding to serum proteins. In vivo experiments for comparison between tumor targeting of [⁶⁴Cu]Cu‐GluCAB‐2^Mal and previous‐generation [⁶⁴Cu]Cu‐GluCAB‐1^Mal encompassed microPET/CT imaging and biodistribution analysis in an allograft E0771 breast cancer mouse model. Tumor uptake of [⁶⁴Cu]Cu‐GluCAB‐2^Mal was clearly evident with twice as much accumulation as compared to its predecessor and a tumor/muscle ratio of up to 5 after 24 h. Further comparison indicated a decrease in liver accumulation for [⁶⁴Cu]Cu‐Glu‐CAB‐2^Mal.

中文翻译：

用于乳腺癌模型中 64Cu-PET/CT 成像的 C 功能化 Cyclam 平台的体内白蛋白结合

已经合成并研究了改进的葡萄糖螯合剂白蛋白生物缀合物 (GluCAB) 衍生物 GluCAB-2 ^Mal及其第一代类似物 GluCAB-1 ^Mal用于乳腺癌小鼠模型的体内 ⁶⁴ Cu-PET/CT 成像。放射性配体通过增强通透性和保留 (EPR) 效应实现肿瘤靶向，并通过葡萄糖代谢发挥支持作用。[ ⁶⁴ Cu]Cu-GluCAB-2 ^Mal (99 % RCP) 表现出高血清稳定性，可立即与血清蛋白结合。[ ⁶⁴ Cu]Cu-GluCAB-2 ^Mal与上一代肿瘤靶向比较的体内实验⁶⁴ Cu]Cu-GluCAB-1 ^Mal包括同种异体移植 E0771 乳腺癌小鼠模型中的 microPET/CT 成像和生物分布分析。[ ⁶⁴ Cu]Cu-GluCAB-2 ^{Mal 的}肿瘤吸收明显明显，其积累量是其前身的两倍，24 小时后肿瘤/肌肉比高达 5。进一步的比较表明 [ ⁶⁴ Cu]Cu-Glu-CAB-2 ^{Mal 的}肝脏积累减少。

更新日期：2020-11-15

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