A new N-acetylgalactosamine containing peptide as a targeting vehicle for mammalian hepatocytes via asialoglycoprotein receptor endocytosis.

Ying Ta Wu, Weir Torn Jiaang, Kuo Ging Lin, Chun Ming Huang, Chin Hsien Chang, Ying Ling Sun, Kuo Hsien Fan, Wei Chuan Hsu, Hsin Ell Wang, Shwu Bin Lin, Shui Tein Chen

研究成果: 雜誌貢獻期刊論文同行評審

17 引文 斯高帕斯(Scopus)

摘要

Galactoside-containing cluster ligands have high affinity for asialoglycoprotein receptors (ASGP-r), which are found in abundance in mammalian parenchymal liver cells. These ligands may be conjugated with a therapeutic drug to improve the efficiency of delivery to diseased liver cells. This report describes a new synthetic route towards clustering glycopeptides containing N-acetyl-D-galactosamine (GalNAc). The building block Fmoc-alpha-(ah-Ac3GalNAc)-L-glutamate allowed access to the target compound YEEE(alpha-ah-GalNAc)(3), a structural mimic of YEE(ah-GalNAc)(3), via solid phase peptide synthesis (SPPS). Fatty acid, poly-lysine, fluorescein and biotin conjugates further demonstrate the facility of the described method. Using fluorescein labeling and 131I labeling, in vitro and in vivo assays confirmed that YEEE(alpha-ah-GalNAc)(3) possesses both specificity and affinity to the liver, similar to the agent YEE(ah-GalNAc)(3), which targets liver lesions. The synthesis described in this report represents a considerable improvement in synthesizing a ligand for ASGP-r by simplifying both the preparation of the starting material and the procedure for conjugating the galactosidase cluster to drugs.

原文???core.languages.en_GB???
頁(從 - 到)119-127
頁數9
期刊Current drug delivery
1
發行號2
DOIs
出版狀態已出版 - 4月 2004

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