Peptide-substituted oligonucleotide synthesis and non-toxic,passive cell delivery  

作　　者：Shiying Shang Luca Monfregola Marvin H Caruthers 

机构地区：[1]Department of Chemistry and Biochemistry,University of Colorado,Boulder,Colorado,USA

出　　处：《Signal Transduction and Targeted Therapy》2016年第1期52-60,共9页信号转导与靶向治疗（英文）

摘　　要：Chemically modified oligodeoxynucleotides(ODNs)are known to modulate gene expression by interacting with RNA.An efficient approach for synthesizing amino acid-or peptide-substituted triazolylphosphonate analogs(TP ODNs)has been developed to provide improved stability and cell uptake.The chemistry is quite general,as peptides can be introduced throughout the TP ODN at any preselected internucleotide linkage.These synthetic TP ODNs enter cells through endocytosis in the absence of transfection reagents and localize into perinuclear organelles.The entrapped ODNs are released into the cytoplasm by treatment with endosomal-releasing agents and several are then active as microRNA inhibitors.

关 键 词：SUBSTITUTED SYNTHESIS ANALOGS 

分 类 号：O62[理学—有机化学]