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

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 y D1X文件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 novel6-sulfo de-N-acetyl sialyl Le I D1X文件D1 has been discovered to be a superior ligand for L-selectin(Angew.Chem.Int.Ed.，38，1131-1133，1999).2.Studies onα-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 acidα(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.

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.