【作者】 熊浩； 李荣荣； 杨文超； 杨光富；

【Author】 HaoXiong;Rong-Rong Li;Wen-Chao Yang;Guang-Fu Yang;Key Laboratory of Pesticide & Chemical Biology,Ministry of Education,Central China Normal University;Chemical Biology Center,College of Chemistry,Central China Normal University;

【机构】 华中师范大学化学学院农药与化学生物学教育部重点实验室； 华中师范大学化学学院化学生物学中心；

【摘要】 本文基于分子柔性对接(MDVS)策略,设计了一种高选择性检测胰凝乳蛋白酶的荧光探针。该探针与靶标能呈现出高达250倍以上的选择性,其亲和力也优于商品化的寡肽底物。此外,该探针被成功应用于相关抑制剂筛选实验和斑马鱼成像实验,以此证实探针能满足检测外源性和内源性的胰凝乳蛋白酶活性的要求,这也是首例被报道的可以在斑马鱼体内追踪胰凝乳蛋白酶的小分子底物型荧光探针。更多还原

【Abstract】 Based on the Molecular Docking-Based Virtual Screening(MDVS), we herein developed one fluorescent probe targeting chymotrypsin with high selectivity that presented 250-fold of the selectivity and prior to the commercial peptide-based substrate in the affinity to the enzyme. Besides, the probe was successfully applied in the inhibitors screening and zebrafish imaging, indicating that sensor couldmeetrequirements of in vitro or in vivo detection of chymotrypsin activity. And it was also the first reported small-molecule fluorescent probe tracking chymotrypsin in zebrafish.更多还原