1279699-70-5Relevant academic research and scientific papers
NOVEL LIVER-TARGETING AGENTS AND THEIR SYNTHESIS
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Page/Page column 1; 3, (2011/04/19)
This invention provides novel liver targeting agents and their synthetic methods. A liver targeting agent, with a lysine based nitrilo triacetic acid structure as backbone which acquires multivalency with saccharide groups, to bind with a galactosamine chain or lactose chain is disclosed. In particular, only one amino acid L-lysine is involved to provide trivalency. All carboxyl groups in Nε-benzyloxycarbonyl-Nα-dicarboxymethyl-L-lysine can be conjugated with three glycosides of ahGalNAc or ahLac in one step. This invention also provides a hexa-lactoside. In particular, the TFA-AHA-Asp was used to conjugate 2 moles of NTA(ahLac)3. This invention also provides a method for adding a spacer between NTA and DTPA. The extended hepatocyte-specific glyco-ligand has higher 111In-radiolabelling yield than those non-extended.
New and more efficient multivalent glyco-ligands for asialoglycoprotein receptor of mammalian hepatocytes
Lee, Reiko T.,Wang, Mei-Hui,Lin, Wuu-Jyh,Lee, Yuan C.
experimental part, p. 2494 - 2500 (2011/06/11)
New 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 ω-amino
