School of Chemistry and Chemical Engineering, Shandong University, Shanda Nanlu 27, 250100 Jinan, Shandong Province, PR China.
Bioorg Med Chem Lett. 2011 Oct 1;21(19):5905-9. doi: 10.1016/j.bmcl.2011.07.122. Epub 2011 Aug 10.
Quantum dots (QDs) that are conjugated to small molecule derivatives of drugs and endogenous ligands may be useful tools to study the distribution and dynamic of membrane bound receptors, ion channels and transporters in live cells. In order to use these tools, it is necessary to functionalize QDs with bioactive ligands. In this paper, we successfully synthesized a ligand of α(1)-adrenoceptor that could be conjugated to QDs. In addition, the conjugation of the ligands to QDs and their biological activity were evaluated through binding assay with 30 nM QD conjugates in living human embryonic kidney 293 cells.
量子点（QD）与药物小分子衍生物和内源性配体偶联，可能成为研究活细胞中膜结合受体、离子通道和转运体分布和动态的有用工具。为了使用这些工具，有必要将生物活性配体功能化到 QD 上。在本文中，我们成功合成了可与 QD 偶联的α(1)-肾上腺素受体配体。此外，通过在活的人胚肾 293 细胞中用 30 nM QD 缀合物进行结合测定，评估了配体与 QD 的缀合及其生物活性。
