PEGylation of therapeutic oligonucletides： From linear to highly branched PEG architectures  

作　　者：Xueguang Lu Ke Zhang 

机构地区：[1]Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, USA

出　　处：《Nano Research》2018年第10期5519-5534,共16页纳米研究（英文版）

基　　金：Financial support by the National Institute of General Medical Sciences Award Number 1R01GM121612-01, the National Science Foundation （CAREER Award Number 1453255）, and the American Chemical Society Petroleum Research Fund （No. PRF 54905-DNI5）, is acknowledged.

摘　　要：PEGylation, the attachment of poly（ethylene glycol） （PEG）, has been adopted to improve the pharmacokinetic properties of oligonucleotide therapeutics for nearly 30 years. Prior efforts mainly focused on the investigation of linear or slightly branched PEG having different molecular weights, terminal functional groups, and possible oligonucleotide sites for functionalization. Recent studies on highly branched PEG （including brush, star, and micellar structures） indicate superior properties in several areas including cellular uptake, gene regulation efficac~ reduction of side effects, and biodistribution. This review focuses on comparing the effects of PEG architecture on the physiochemical and biological properties of the PEGylated oligonucleotide.PEGylation, the attachment of poly（ethylene glycol） （PEG）, has been adopted to improve the pharmacokinetic properties of oligonucleotide therapeutics for nearly 30 years. Prior efforts mainly focused on the investigation of linear or slightly branched PEG having different molecular weights, terminal functional groups, and possible oligonucleotide sites for functionalization. Recent studies on highly branched PEG （including brush, star, and micellar structures） indicate superior properties in several areas including cellular uptake, gene regulation efficac~ reduction of side effects, and biodistribution. This review focuses on comparing the effects of PEG architecture on the physiochemical and biological properties of the PEGylated oligonucleotide.

关 键 词：PEGYLATION OLIGONUCLEOTIDE brush polymer ANTISENSE small interfering RNA APTAMER PHOSPHOROTHIOATE 

分 类 号：TQ457.29[化学工程—农药化工] S854.5[农业科学—临床兽医学]