Li Kai-Bin, Li Na, Zang Yi, Chen Guo-Rong, Li Jia, James Tony D, He Xiao-Peng, Tian He
Key Laboratory for Advanced Materials & Institute of Fine Chemicals , School of Chemistry and Molecular Engineering , East China University of Science and Technology , 130 Meilong Rd. , Shanghai 200237 , PR China . Email:
National Center for Protein Science Shanghai , Shanghai Institutes of Biological Sciences , Chinese Academy of Sciences , Shanghai 200031 , PR China.
Chem Sci. 2016 Oct 1;7(10):6325-6329. doi: 10.1039/c6sc02366e. Epub 2016 Jul 12.
Small-molecular probes capable of monitoring and interfering with the activity of biomacromolecules - such as polysaccharides, nucleotides and proteins - are of paramount importance to the advancement of life science. However, such probes that can detect and simultaneously modulate the construction of biomacromolecules are elusive. Here we report a fluorogenic, foldable glycoprobe that can recognize and assemble a protein receptor in a synchronous fashion. The glycoprobe synthesized by introducing a glycoligand (for protein recognition) to a bola-type bis-fluorophore conjugate shows a "self-shielded" fluorescence in the folded state. Association with a receptor protein rapidly unfolds the probe, releasing a fluorophore capable of crosslinking the proteins - as determined using small-angle X-ray scattering - thereby producing a unique fluorescent supramolecular construct. We have demonstrated the use of the foldable glycoprobe in order to track the endocytic cycle of a transmembrane receptor.
能够监测和干扰生物大分子（如多糖、核苷酸和蛋白质）活性的小分子探针对于生命科学的发展至关重要。然而，能够检测并同时调节生物大分子构建的此类探针却难以捉摸。在此，我们报告了一种可荧光成像、可折叠的糖探针，它能够以同步方式识别并组装蛋白质受体。通过将糖配体（用于蛋白质识别）引入到bola型双荧光团共轭物中合成的糖探针在折叠状态下呈现“自屏蔽”荧光。与受体蛋白结合会使探针迅速展开，释放出一种能够交联蛋白质的荧光团（通过小角X射线散射测定），从而产生一种独特的荧光超分子结构。我们已经展示了这种可折叠糖探针在追踪跨膜受体胞吞循环中的应用。
