典型文献
SARS-CoV-2 receptor binding domain radio-probe:a non-invasive approach for angiotensin-converting enzyme 2 mapping in mice
文献摘要：
The spike protein of SARS-CoV-2 interacts with angiotensin-converting enzyme 2(ACE2)of human respiratory epithelial cells,which leads to infection.Furthermore,low-dose radiation has been found to reduce inflammation and aid the curing of COVID-19.The receptor binding domain(RBD),a recombinant spike protein with a His tag at the C-terminus,binds to ACE2 in human body.We thus constructed a radioiodinated RBD as a molecule-targeted probe to non-invasively explore ACE2 expression in vivo,and to investigate radiotherapy pathway for inhibiting ACE2.RBD was labeled with[124I]Nal using an N-bromosuccinimide(NBS)-mediated method,and 124I-RBD was obtained after purification with a specific activity of 28.9 GBq/nmol.Its radiochemical purity was(RCP)over 90％in saline for 5 days.The dissociation constant of 124I-RBD binding to hACE2 was 75.7 nM.The uptake of 124I-RBD by HeLaACE+cells at 2 h was 2.96％±0.35％,which could be substantially blocked by an excessive amount of RBD,and drop to 1.71％±0.23％.In BALB/c mice,the biodistribution of 124I-RBD after intravenous injection showed a moderate metabolism rate,and its 24 h-post injection(p.i.)organ distribution was similar to the expression profile in body.Micro-PET imaging of mice after intrapulmonary injection showed high uptake of lung at 1,4,24 h p.i..In conclusion,the experimental results demonstrate the potential of 124I-RBD as a novel targeted molecular probe for COVID-19.This probe may be used for non-invasive ACE2 mapping in mammals.
文献关键词：
中图分类号：
作者姓名：
Dan Li;Jin Ding;Te-li Liu;Feng Wang;Xiang-xi Meng;Song Liu;Zhi Yang;Hua Zhu
作者机构：
Key Laboratory of Carcinogenesis and Translational Research(Ministry of Education/Beijing),NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals(National Medical Products Administration),Department of Nuclear Medicine,Peking University Cancer Hospital&Institute,Beijing 100142,China
文献出处：
引用格式：
[1]Dan Li;Jin Ding;Te-li Liu;Feng Wang;Xiang-xi Meng;Song Liu;Zhi Yang;Hua Zhu-.SARS-CoV-2 receptor binding domain radio-probe:a non-invasive approach for angiotensin-converting enzyme 2 mapping in mice)[J].中国药理学报（英文版）,2022(07):1749-1757
A类：
radioiodinated,124I,bromosuccinimide,HeLaACE+cells
B类：
SARS,CoV,receptor,binding,domain,probe,approach,angiotensin,converting,enzyme,mapping,mice,spike,protein,interacts,human,respiratory,epithelial,which,leads,infection,Furthermore,low,dose,radiation,has,been,found,reduce,inflammation,aid,curing,RBD,recombinant,His,tag,terminus,binds,body,We,thus,constructed,molecule,targeted,invasively,explore,expression,vivo,investigate,radiotherapy,pathway,inhibiting,was,labeled,Nal,using,NBS,mediated,method,obtained,after,purification,specific,activity,GBq,nmol,Its,radiochemical,purity,RCP,over,saline,days,dissociation,constant,hACE2,nM,uptake,by,could,substantially,blocked,excessive,amount,drop,In,BALB,biodistribution,intravenous,injection,showed,moderate,metabolism,its,post,organ,similar,profile,Micro,PET,imaging,intrapulmonary,high,lung,conclusion,experimental,results,demonstrate,potential,novel,molecular,This,may,used,mammals
AB值：
0.530861
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