title: A concise method for the preparation of peptide and arginine-rich peptide-conjugated antisense oligonucleotide.
abstract: Peptide-oligonucleotide conjugates were synthesized using two strategies: a mimetic signal peptide-conjugated oligonucleotide was assembled stepwise on CPG by using 2,2-dimethyl-3-hydroxypropionic acid as a linker. To solve the precipitation problem in the coupling reaction caused by the electrostatic interaction of arginine-rich peptides and oligonucleotide, oligonucleotides were absorbed on an anion-exchange resin, and then the on-resin fragment was applied for the conjugation with arginine-rich peptide. The peptide-antisense oligonucleotides showed permeability to the cell membrane of HepG-2 cells.
authors.affiliation: School of Pharmaceutical Sciences, Peking University, Beijing 100083, China.
authors.forename: Chang-Po
authors.initials: CP
authors.lastname: Chen
authors.forename: Liang-Ren
authors.initials: LR
authors.lastname: Zhang
authors.forename: Yue-Feng
authors.initials: YF
authors.lastname: Peng
authors.forename: Xiao-Bo
authors.initials: XB
authors.lastname: Wang
authors.forename: Sheng-Qi
authors.initials: SQ
authors.lastname: Wang
authors.forename: Li-He
authors.initials: LH
authors.lastname: Zhang
mesh_terms: D001120:Arginine / Q000138:chemical synthesis* / Q000235:genetics; D002460:Cell Line; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D006801:Humans; D016376:Oligonucleotides, Antisense / Q000138:chemical synthesis* / Q000235:genetics; D010455:Peptides / Q000138:chemical synthesis* / Q000235:genetics
chemical_list: D016376:Oligonucleotides, Antisense; D010455:Peptides; D001120:Arginine