Glutathione and specific enzyme-responsive PAMAM dendrimer for gene delivery systems
발표자
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초록
내용
In this study, development of gene delivery systems based PAMAM dendrimer containing the enzyme sensitive sequence (gly-phe-leu-gly, GFLG) and cystamine core was evaluated to efficient transfection efficiency. Cystamine core of PAMAM generation 3 (cPAMAM G3) is responsive intracellular glutathione (GSH), it could cleave a disulfide bond. And surface of cPAMAM G3 was conjugated with ‘GFLG’ peptide sequence, Histidine(His) and Arginine(Arg). ‘GFLG’ sequence is enzyme responsive sequence by cathepsin B and could be cancer specific targeting due to cathepsin B overexpressed in cancer. and His is role of endosomal escape by buffering capacity of imidazole ring, and Arg is one of the representing positive charge amino acid, it could be easily cellular uptake. cG3-GLFG-H-R was synthesized using Fmoc chemistry and confirmed by 1H-NMR. cG3-GLFG-H-R was investigated transfection efficiency, cytotoxicity and cellular uptake in HeLa, Hep G2 cells.