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pubmed-article:21459583pubmed:abstractTextNew multi-valent, carbohydrate ligands that contain terminal N-acetylgalactosamine (GalNAc) or lactose (Lac) were prepared using a nitrilotriacetic acid (NTA) derivative of L-lysine as scaffold. Tri-valent structures were prepared by attaching an ?-amino glycoside of GalNAc or Lac to each of the three carboxyl groups of N(?)-protected N(?)-dicarboxymethyl-L-lysine. In addition, a hexa-valent lactoside was synthesized by attaching N(?)-deprotected trivalent lactoside to each of the carboxyl group of N(?)-(trifluoroacetamido)hexanoyl L-aspartic acid. Tri-valent GalNAc glycosides and the hexa-valent lactoside had high affinity (dissociation constants approaching nM) for rat hepatocytes. The hexa-valent lactoside, after de-N(?)-protection, was modified with a chelator, diethylenetriaminepentaacetic acid (DTPA), through which a fluorescent or radioactive tag, such as europium or indium, can be firmly attached. Intravenous infusion of (111)Indium-tagged hexa-valent lactoside to rats and mice resulted in nearly exclusive accumulation of radioactivity in the liver.lld:pubmed
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pubmed-article:21459583pubmed:authorpubmed-author:LeeReiko TRTlld:pubmed
pubmed-article:21459583pubmed:authorpubmed-author:LeeYuan CYClld:pubmed
pubmed-article:21459583pubmed:authorpubmed-author:WangMei-HuiMHlld:pubmed
pubmed-article:21459583pubmed:authorpubmed-author:LinWuu-JyhWJlld:pubmed
pubmed-article:21459583pubmed:copyrightInfoCopyright © 2011 Elsevier Ltd. All rights reserved.lld:pubmed
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pubmed-article:21459583pubmed:year2011lld:pubmed
pubmed-article:21459583pubmed:articleTitleNew and more efficient multivalent glyco-ligands for asialoglycoprotein receptor of mammalian hepatocytes.lld:pubmed
pubmed-article:21459583pubmed:affiliationDepartment of Biology, Johns Hopkins University, Baltimore, MD 21218, USA.lld:pubmed
pubmed-article:21459583pubmed:publicationTypeJournal Articlelld:pubmed
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