title: Synthesis of antisense oligonucleotide-peptide conjugate targeting to GLUT-1 in HepG-2 and MCF-7 Cells.
abstract: A simple procedure for the preparation of oligonucleotide-peptide conjugate was developed. p-Hydroxy-benzoic acid was used as a linker for the connection of the fragments of peptide and oligonucleotide. It was found that such formed linkage was stable under the conditions of conjugate synthesis. The designed conjugate targeting to GLUT-1 showed up to 50% inhibition of cell proliferation in HepG-2 and MCF-7 cells. Comparing to the results from the expressed antisense RNA in cancer cells, it was proposed that the conjugate of signal peptide mimic and antisense oligonucleotide could improve the permeability of antisense oligonucleotide through cell membrane.
authors: School of Pharmaceutical Sciences, Peking University, Beijing 100083, China.
authors: Chang-Po
authors: CP
authors: Chen
authors: Xiao-Xu
authors: XX
authors: Li
authors: Liang-Ren
authors: LR
authors: Zhang
authors: Ji-Mei
authors: JM
authors: Min
authors: Judy Yuet-Wah
authors: JY
authors: Chan
authors: Kwok-Pui
authors: KP
authors: Fung
authors: Sheng-Qi
authors: SQ
authors: Wang
authors: Li-He
authors: LH
authors: Zhang
mesh_terms: D015152:Blotting, Northern; D015153:Blotting, Western; D002455:Cell Division / Q000187:drug effects; D003432:Cross-Linking Reagents / Q000737:chemistry; D004305:Dose-Response Relationship, Drug; D005260:Female; D051272:Glucose Transporter Type 1; D006801:Humans; D009004:Monosaccharide Transport Proteins / Q000235:genetics*; D016376:Oligonucleotides, Antisense / Q000138:chemical synthesis* / Q000494:pharmacology; D010226:Parabens / Q000737:chemistry; D010455:Peptides / Q000138:chemical synthesis* / Q000494:pharmacology; D012333:RNA, Messenger / Q000378:metabolism; D013873:Thionucleotides; D014162:Transfection; D014407:Tumor Cells, Cultured / Q000187:drug effects
chemical_list: D003432:Cross-Linking Reagents; D051272:Glucose Transporter Type 1; D009004:Monosaccharide Transport Proteins; D016376:Oligonucleotides, Antisense; D010226:Parabens; D010455:Peptides; D012333:RNA, Messenger; C495677:SLC2A1 protein, human; D013873:Thionucleotides; C038193:4-hydroxybenzoic acid