基于亲和力的小分子探针用于Keap1荧光可视化和特异性检测的设计、合成及初步评估
Design, Synthesis, and Initial Evaluation of Affinity-Based Small-Molecule Probes for Fluorescent Visualization and Specific Detection of Keap1.
作者信息
Lu Mengchen, Zhou Hai-Shan, You Qi-Dong, Jiang Zhengyu
机构信息
State Key Laboratory of Natural Medicines and Jiang Su Key Laboratory of Drug Design and Optimization, China Pharmaceutical University , Nanjing 210009, China.
Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University , Nanjing 210009, China.
出版信息
J Med Chem. 2016 Aug 11;59(15):7305-10. doi: 10.1021/acs.jmedchem.6b00775. Epub 2016 Jul 22.
Keap1 is a pluripotent protein which plays a predominant role in cellular homeostasis and stress responses. Given that the cellular environment is quite dynamic and versatile, further investigation of the function of Keap1 depends on tools for specific and real-time detection of Keap1. Herein, we report the development of functional affinity-based small-molecule probes which can overcome some shortcomings of current methods and be applied in further studying the function of Keap1.
Keap1是一种多功能蛋白，在细胞内稳态和应激反应中起主要作用。鉴于细胞环境相当动态且多样，对Keap1功能的进一步研究依赖于对Keap1进行特异性实时检测的工具。在此，我们报道了基于功能亲和力的小分子探针的开发，该探针可克服现有方法的一些缺点，并应用于进一步研究Keap1的功能。
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