Dipolar coupling-based electron paramagnetic resonance method for protease enzymatic characterization and inhibitor screening
收藏科学数据银行2023-02-15 更新2026-04-23 收录
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资源简介：
Herein, we report an EPR-based method for protease enzymatic characterization and inhibitor screening. This method utilizes dual paramagnetically-labeled probes consisting of a nitroxide spin probe and a Gd3+ ion flanking a peptide that could be specifically cleaved by protease caspase-3. Distance-dependent dipolar coupling between the two paramagnetic centers can be modulated by the protease cleavage activity, thus providing a straightforward and convenient method for protease activity detection using EPR spectroscopy under ambient conditions. Moreover, time-course monitoring of the protease catalyzed cleavage reaction demonstrated that this EPR-based method could not only allow a direct quantitative enzymatic kinetic assessment, but also could be used for protease inhibitor screening, thus holding great potential in drug discovery studies.
提供机构：
High Magnetic Field Laboratory; Shanghai Tenth People's Hospital; The First Affiliated Hospital of USTC; University of Illinois at Urbana-Champaign; University of Science and Technology of China
创建时间：
2022-10-31
