Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University , Jinan, Shandong 250012, China.
Key Laboratory of Theoretical Organic Chemistry and Functional Molecule (MOE), College of Chemistry and Chemical Engineering, Hunan University of Science and Technology , Xiangtan, Hunan 411201, China.
Anal Chem. 2017 Nov 7;89(21):11173-11177. doi: 10.1021/acs.analchem.7b01148. Epub 2017 Oct 16.
The environment-sensitive probe 2 with turn-on switch for Mcl-1 protein was developed herein. After careful evaluation, this small molecule fluorescent probe revealed a selective binding affinity with Mcl-1 protein with a K value of 2.6 μM and can be well applied to imaging Mcl-1 protein or detecting the cellular distribution of Mcl-1 protein inhibitors. Compared with other imaging approaches, such as the immunofluorescence and fluorescent protein-based techniques, this fluorescent method is rapid, convenient, and affordable, especially since a washing procedure is no longer needed. This environment-sensitive "off-on" design strategy may present a case in point for developing small-molecule fluorescent probe of Bcl-2 family proteins.
本文开发了一种具有 Mcl-1 蛋白开关的环境敏感探针 2。经过仔细评估，这种小分子荧光探针与 Mcl-1 蛋白具有选择性结合亲和力，Kd 值为 2.6 μM，可以很好地应用于 Mcl-1 蛋白的成像或检测 Mcl-1 蛋白抑制剂的细胞分布。与其他成像方法（如免疫荧光和荧光蛋白技术）相比，这种荧光方法快速、方便、经济实惠，尤其是不再需要洗涤步骤。这种环境敏感的“关-开”设计策略可能为开发 Bcl-2 家族蛋白的小分子荧光探针提供了一个范例。
