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

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

扫码查看
原文链接
  • NETL
  • NSTL
  • 万方数据
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.

Rational modificationBiomimetic macrocycleUltra-high selectivityEnzyme assay

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

展开 >

School of Pharmaceutical Science,Postdoctoral Research Station of Basic Medicine,Hengyang Medical School,University of South China,Hengyang 421001,China

Department of Chemistry,Southern University of Science and Technology,Shenzhen 518055,China

National Natural science Foundation of ChinaNational Natural science Foundation of ChinaHunan Provincial Natural Science Foundation of ChinaHunan Provincial Natural Science Foundation of ChinaHunan Provincial Natural Science Foundation of ChinaExcellent youth funding of Hunan Provincial Education DepartmentChina Postdoctoral Science Foundation

22174059222011282022JJ403632022JJ403652022RC123022B04602022M721542

2024

10.1016/j.cclet.2023.109154

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
年,卷(期)：2024.35(6)
  • 1