Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Science, Cheeloo College of Medicine, Shandong University, Ji'nan, Shandong, PR China.
Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Science, Cheeloo College of Medicine, Shandong University, Ji'nan, Shandong, PR China.
Bioorg Med Chem. 2021 Jan 1;29:115850. doi: 10.1016/j.bmc.2020.115850. Epub 2020 Nov 7.
Development of efficient fluorescent probes for detecting the overexpressed Mcl-1 protein in living cells is imperative for the diagnosis and treatment of cancers. In this paper, a new UMI-77 based fluorescent probe (DNSH), was synthesized and characterized. DNSH bound to the hydrophobic pockets of Mcl-1 protein tightly and the binding affinity was 20-fold higher than that of previous developed Mcl-1 probe. DNSH exhibited specific fluorescence response to Mcl-1 protein rather than other proteins. In the presence of Mcl-1 protein, fluorescence emission of DNSH can be switched on. Furthermore, fluorescence colocalization experiment demonstrated that DNSH can be successfully used for imaging mitochondrial Mcl-1 protein in human prostate cancer cells without a washing process. These results showed that DNSH may find useful applications in biological research such as tracking Mcl-1 protein in living biological specimens.
开发用于检测活细胞中超表达的 Mcl-1 蛋白的高效荧光探针对于癌症的诊断和治疗至关重要。本文合成并表征了一种基于 UMI-77 的新型荧光探针（DNSH）。DNSH 与 Mcl-1 蛋白的疏水口袋紧密结合，结合亲和力比以前开发的 Mcl-1 探针高 20 倍。DNSH 对 Mcl-1 蛋白表现出特异性荧光响应，而不是其他蛋白质。在存在 Mcl-1 蛋白的情况下，DNSH 的荧光发射可以被打开。此外，荧光共定位实验表明，DNSH 可在无需洗涤过程的情况下成功用于人前列腺癌细胞中线粒体 Mcl-1 蛋白的成像。这些结果表明，DNSH 可能在生物研究中找到有用的应用，例如在活生物标本中追踪 Mcl-1 蛋白。
