Studies on high-dimensional functions of glycoconjugates toward development of new medicines and biomaterials

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1. Studies on novel, endogenous ligand for selectins, and molecular design for selectin blockers: We have found that GSC-150, a selectin blocker, would be useful for treatment of allergies such as atopic dermatitis, and have developed an efficient procedure for mass production of GSC-150. 6-Sulfo sialyl LeィイD1XィエD1 has been found to be an endogenous ligand for L-selectin on high endothelial venules (HEV) of human lymph nodes (J. Biol. Chem., 273, 11225-11233. 1998), and very recently, a novel 6-sulfo de-N-acetyl sialyl LeィイD1XィエD1 has been discovered to be a superior ligand for L-selectin (Angew. Chem. Int. Ed., 38, 1131-1133, 1999).2. Studies on α-series (Chol-1) gangliosides, and structure-activity relationship for MAG binding: We have succeeded in an efficient, total synthesis of GT1aα (Glycoconjugate J., in press), and have demonstrated that the internal sialic acid α(1-6)-linked to GalNAc might be replaced by other anionic substituents such as sulfate (Carbohydr. Res., 316, 1-5, 1999; J. Biol. Chem., in press).Based on these new findings, design and synthesis of novel medicines and biomaterials are now proceeding.