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

Huan Yao ¹Jian Qin ¹Yan-Fang Wang ²Song-Meng Wang ²Liu-Huan Yi ¹Shi-Yao Li ¹Fangfang Du ¹Liu-Pan Yang ¹Li-Li Wang¹

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作者信息

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
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Abstract

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 tetralac-tam macrocycle and realize the ultra-high selectivity to nucleosides over corresponding monophos-phate nucleotides by rational modification.The introduction of charged groups at the periphery of endo-functionalized cavity makes the selectivity(guanosine to guanosine 5'-monophosphate)increase remark-ably from 100 to 1119.Based on the ultra-high selectivity of biomimetic tetralactam macrocycle,the sen-sitive 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 suc-cessfully displayed.

Key words

Rational modification/Biomimetic macrocycle/Ultra-high selectivity/Enzyme assay

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基金项目

National Natural science Foundation of China(22174059)

National Natural science Foundation of China(22201128)

Hunan Provincial Natural Science Foundation of China(2022JJ40363)

Hunan Provincial Natural Science Foundation of China(2022JJ40365)

Hunan Provincial Natural Science Foundation of China(2022RC1230)

Excellent youth funding of Hunan Provincial Education Department(22B0460)

China Postdoctoral Science Foundation(2022M721542)

出版年

2024

中国化学快报(英文版)

中国化学会

中国化学快报(英文版)

CSTPCD

影响因子：0.771

ISSN：1001-8417

参考文献量1

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