Ultra-highly selective recognition of nucleosides over nucleotides by rational modification of tetralactam macrocycle and its application in enzyme assay  

作　　者：Huan Yao Jian Qin Yan-Fang Wang Song-Meng Wang Liu-Huan Yi Shi-Yao Li Fangfang Du Liu-Pan Yang Li-Li Wang 

机构地区：[1]School of Pharmaceutical Science,Postdoctoral Research Station of Basic Medicine,Hengyang Medical School,University of South China,Hengyang 421001,China [2]Department of Chemistry,Southern University of Science and Technology,Shenzhen 518055,China

出　　处：《Chinese Chemical Letters》2024年第6期274-278,共5页中国化学快报（英文版）

基　　金：financially supported by National Natural Science Foundation of China(Nos.22174059 and 22201128);Hunan Provincial Natural Science Foundation of China(Nos.2022JJ40363,2022JJ40365 and 2022RC1230);the Excellent youth funding of Hunan Provincial Education Department(No.22B0460);China Postdoctoral Science Foundation(No.2022M721542)。

摘　　要：Artificial macrocycle with high binding selectivity in water is often challenging but urgently needed in various research and application areas.Herein,we report a new water-soluble biomimetic tetralactam macrocycle and realize the ultra-high selectivity to nucleosides over corresponding monophosphate nucleotides by rational modification.The introduction of charged groups at the periphery of endofunctionalized cavity makes the selectivity(guanosine to guanosine 5-monophosphate)increase remarkably from 100 to 1119.Based on the ultra-high selectivity of biomimetic tetralactam macrocycle,the sensitive CD73 enzyme activity assay was then achieved through product-selective fluorescence indicator displacement assay.Furthermore,the capability of the proposed method for inhibitor screening was successfully displayed.

关 键 词：Rational modification Biomimetic macrocycle Ultra-high selectivity Enzyme assay 

分 类 号：O652[理学—分析化学]