Saccharide Receptor-Mediated Drug Delivery

  • M. M. Ponpipom
  • R. L. Bugianesi
  • J. C. Robbins
  • T. W. Doebber
  • T. Y. Shen


Since the pioneering work of Ashwell and Morell on the in-vivo plasma clearance of desialylated serum glycoproteins, 1 the concept has become widely accepted that exposed sugar residues on glycoproteins serve as determinants for in-vivo (i.e., clearance) and in-vitro (i.e., uptake) recognition. Carbohydrate-mediated endocytosis in mammals has since become the subject of intensive studies.2,3 Mammalian hepatic receptors are known to be specific for terminal D-galactose of desialylated serum glycoproteins;4 whereas in avian liver, the receptors recognize terminal 2-acetamido-2-deoxy-D-glucose residues.5 Hepatocytes also contain a receptor that binds glycoproteins specifically through L-fucose in α (1→3) linkage to 2-ace-tamido-2-deoxy-D-glucose.6 Macrophages and Kupffer cells have been shown to bind glycoproteins and synthetic neoglycoconjugates that have D-mannose and 2-acetamido-2-deoxy-D-glucose in the exposed non-reducing position.7,8 The uptake of some lysosomal enzymes by fibroblasts involves recognition of D-mannose 6-phosphate.9


Alveolar Macrophage Native Enzyme Lipoic Acid Macrophage Uptake Label Ligand 
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Copyright information

© Plenum Press, New York 1984

Authors and Affiliations

  • M. M. Ponpipom
    • 1
  • R. L. Bugianesi
    • 1
  • J. C. Robbins
    • 1
  • T. W. Doebber
    • 1
  • T. Y. Shen
    • 1
  1. 1.Merck Sharp & Dohme Research LaboratoriesRahwayUSA

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