发明名称 TARGETING OF GLYCOPROTEIN THERAPEUTICS
摘要 Methods of making ligand-decorated polymer conjugates of therapeutic glycoproteins are described. Improved targeting of glycoproteins to specific tissues is achieved by masking the natural carbohydrate and other surface determinants with high molecular weight polymers, such as, e.g., PEG, polysialic acid, etc., which in turn are decorated with target-specific ligands. In some embodiments, acid-labile linkages in such conjugates or rapidly degradable masking groups allow for the intracellular release of the polymer from the glycoprotein, for example, under conditions found in lysosomes.
申请公布号 US2017042979(A1) 申请公布日期 2017.02.16
申请号 US201615297083 申请日期 2016.10.18
申请人 Genzyme Corporation 发明人 STEFANO James
分类号 A61K38/47;A61K47/48;C12N9/40;C12N9/96 主分类号 A61K38/47
代理机构 代理人
主权项 1. A conjugate comprising: (1) a therapeutic glycoprotein (G), (2) a masking moiety (M) covalently linked to an oligosaccharide side chain of the glycoprotein through a first linker (L1), and (3) a targeting moiety (T) covalently linked to the masking moiety through a second linker (L2), wherein the glycoprotein is released from the conjugate under lysosomal conditions.
地址 Cambridge MA US