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Ratiometric Fluorescence Monitoring of Antibody-Guided Drug Delivery to Cancer Cells
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2021-06-11 , DOI: 10.1021/acs.bioconjchem.1c00205 Dvir Poplinger 1 , Maksym Bokan 1 , Arkadi Hesin 2 , Ebaston Thankarajan 1 , Helena Tuchinsky 2 , Gary Gellerman 1 , Leonid Patsenker 1
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2021-06-11 , DOI: 10.1021/acs.bioconjchem.1c00205 Dvir Poplinger 1 , Maksym Bokan 1 , Arkadi Hesin 2 , Ebaston Thankarajan 1 , Helena Tuchinsky 2 , Gary Gellerman 1 , Leonid Patsenker 1
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Ratiometric measurements utilizing two independent fluorescence signals from a dual-dye molecular system help to improve the detection sensitivity and quantification of many analytical, bioanalytical, and pharmaceutical assays, including drug delivery monitoring. Nevertheless, these dual-dye conjugates have never been utilized for ratiometric monitoring of antibody (Ab)-guided targeted drug delivery (TDD). Here, we report for the first time on the new, dual-dye TDD system, Cy5s-Ab-Flu-Aza, comprising the switchable fluorescein-based dye (Flu) linked to the anticancer drug azatoxin (Aza), reference pentamethine cyanine dye (Cy5s), and Her2-specific humanized monoclonal Trastuzumab (Herceptin) antibody. The ability of ratiometric fluorescence monitoring of drug release was demonstrated with this model system in vitro in the example of the human breast cancer SKBR3 cell line overexpressing Her2 receptors. The proposed approach for designing ratiometric, antibody-guided TDD systems, where a “drug–switchable dye” conjugate and a reference dye are independently linked to an antibody, can be expanded to other drugs, dyes, and antibodies. Replacement of the green-emitting dye Flu, which was found not detectable in vivo, with a longer-wavelength (red or near-IR) switchable fluorophore should enable quantification of drug release in the body.
中文翻译：
抗体引导药物递送至癌细胞的比率荧光监测
利用来自双染料分子系统的两个独立荧光信号的比率测量有助于提高许多分析、生物分析和药物分析的检测灵敏度和定量，包括药物输送监测。然而，这些双染料偶联物从未用于对抗体 (Ab) 引导的靶向药物递送 (TDD) 进行比例监测。在这里，我们首次报告了新的双染料 TDD 系统 Cy5s-Ab-Flu-Aza，该系统包含与抗癌药物氮杂毒素 (Aza) 连接的可切换荧光素染料 (Flu)，参考五甲川花青染料(Cy5s) 和 Her2 特异性人源化单克隆曲妥珠单抗 (Herceptin) 抗体。该模型系统在体外证明了药物释放的比率荧光监测能力在过表达 Her2 受体的人乳腺癌 SKBR3 细胞系的例子中。用于设计比例、抗体引导 TDD 系统的建议方法，其中“药物可切换染料”偶联物和参考染料独立连接到抗体，可以扩展到其他药物、染料和抗体。用更长波长（红色或近红外）可切换荧光团替代在体内无法检测到的发绿光染料 Flu应该能够量化体内药物释放。
更新日期：2021-08-19
中文翻译：
抗体引导药物递送至癌细胞的比率荧光监测
利用来自双染料分子系统的两个独立荧光信号的比率测量有助于提高许多分析、生物分析和药物分析的检测灵敏度和定量，包括药物输送监测。然而，这些双染料偶联物从未用于对抗体 (Ab) 引导的靶向药物递送 (TDD) 进行比例监测。在这里，我们首次报告了新的双染料 TDD 系统 Cy5s-Ab-Flu-Aza，该系统包含与抗癌药物氮杂毒素 (Aza) 连接的可切换荧光素染料 (Flu)，参考五甲川花青染料(Cy5s) 和 Her2 特异性人源化单克隆曲妥珠单抗 (Herceptin) 抗体。该模型系统在体外证明了药物释放的比率荧光监测能力在过表达 Her2 受体的人乳腺癌 SKBR3 细胞系的例子中。用于设计比例、抗体引导 TDD 系统的建议方法，其中“药物可切换染料”偶联物和参考染料独立连接到抗体，可以扩展到其他药物、染料和抗体。用更长波长（红色或近红外）可切换荧光团替代在体内无法检测到的发绿光染料 Flu应该能够量化体内药物释放。
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