CEA, IRAMIS, SIS2M, Laboratoire Structure et Dynamique par Résonance Magnétique, UMR CEA/CNRS 3299, Gif sur Yvette, France.
Bioorg Med Chem. 2011 Jul 1;19(13):4135-43. doi: 10.1016/j.bmc.2011.05.002. Epub 2011 May 6.
For detection of biological events in vitro, sensors using hyperpolarized (129)Xe NMR can become a powerful tool, provided the approach can bridge the gap in sensitivity. Here we propose constructs based on the non-selective grafting of cryptophane precursors on holo-transferrin. This biological system was chosen because there are many receptors on the cell surface, and endocytosis further increases this density. The study of these biosensors with K562 cell suspensions via fluorescence microscopy and (129)Xe NMR indicates a strong interaction, as well as interesting features such as the capacity of xenon to enter the cryptophane even when the biosensor is endocytosed, while keeping a high level of polarization. Despite a lack of specificity for transferrin receptors, undoubtedly due to the hydrophobic character of the cryptophane moiety that attracts the biosensor into the cell membrane, these biosensors allow the first in-cell probing of biological events using hyperpolarized xenon.
为了检测体外的生物事件，使用超极化（129）Xe NMR 的传感器可以成为一种强大的工具，只要该方法能够弥补灵敏度上的差距。在这里，我们提出了基于隐杯芳烃前体非选择性接枝在全转铁蛋白上的构建体。选择这个生物系统是因为细胞表面有许多受体，而内吞作用进一步增加了这种密度。通过荧光显微镜和（129）Xe NMR 研究这些生物传感器与 K562 细胞悬浮液表明存在强烈的相互作用，以及一些有趣的特征，例如即使在生物传感器被内吞时，氙气仍有进入隐杯芳烃的能力，同时保持高水平的极化。尽管对转铁蛋白受体缺乏特异性，这无疑是由于隐杯芳烃部分的疏水性吸引生物传感器进入细胞膜，但这些生物传感器允许首次使用超极化氙气对细胞内的生物事件进行探测。
