Tailoring Cationic Helical Polypeptides for Efficient Cytosolic Protein Delivery

查看全文 作　　者：WANG [1]Ruijue;SHENG [1]Kai;HOU [1]Yingqin;SUN [1]Jialing;LU [1]Hua

机构地区：[1]Beijing National Laboratory for Molecular Sciences,Center for Soft Matter Science and Engineering,Key Laboratory of Polymer Chemistry and Physics of Ministry of Education,College of Chemistry and Molecular Engineering,Peking University,Beijing 100871,P.R.China

出　　处：《Chemical Research in Chinese Universities》索引2020年第36卷第1期,共5页

基　　金：Supported by the National Key Research and Development Program of China(No.2016YFA0201400);the National Natural Science Foundation of China(Nos.21434008,21722401). 摘　　要：Protein delivery is of central importance for both diagnostic and therapeutic applications.However,protein delivery faces challenges including poor endosomal escape and thus limited efficiency.Here,we report the facile construction and screening of a small library of cationic helical polypeptides for cytosolic protein delivery.The library is based on a random copolymer poly(γ-{2-[2-(2-methoxyethoxy)ethoxy]ethoxy}esteryl-L-glutamate)-randompoly(γ-6-chlorohexyl-L-glutamate)[P(EG3-r-ClC6)Glu],which is then modified with various pyridine derivatives and alkyl thiols.Flow Cytometry,confocal laser scanning microscopy,and viability assay collaboratively identify two leading polymers,showing efficient delivery of enhanced green fluorescent protein(eGFP)and low cytoto-xicity.This finding is further validated by the cytosolic delivery of RNase A and cytochrome C(Cyt C)to HeLa cells in the viability assay.Together,this work demonstrates that high-throughput screening is an effective and viable approach to the selection of cationic helical polypeptides for the cytosolic delivery of functional proteins. 关键词：Cationic helical polypeptide Protein delivery Cytosolic protein

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Tailoring Cationic Helical Polypeptides for Efficient Cytosolic Protein Delivery

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