Title:
CELL SPECIFIC GLYCOPEPTIDE LIGAND
Document Type and Number:
Japanese Patent JPS57181095
Kind Code:
A
Abstract:
Cell-specific ligands comprising conjugates of saccharides and amino acids or peptides are synthesized from amino acids such as ornithine, lysine, peptides such as dilysine, diornithine or oligolysine and selected saccharides having reactive functional groups protected by appropriate blocking groups. Such glycopeptides are useful as tissue specific substances, which when coupled with bioactive materials through metabolizable or hydrolyzable linkages, deliver such bioactive materials to the selected site. In this manner, antiinflammatory drugs such as dexamethasone are linked through a metabolizable or hydrolyzable linkage and on administration to an animal suffering from inflammatory disease carries the drug to the site of inflammation for intracellular release. Other examples include the macrophage ligand N2-N2, N6-Bis-[3-( alpha -D-mannopyranosylthio)propionyl]-6-lysyl-N6-[3-( alpha -D-mannopyranosylthio)propionyl]-L-lysine, 5, which when coupled to beta -glucocerebrosidase, can deliver the enzyme selectively to kupffer cells. This is useful in the enzyme replacement therapy of Gaucher's disease.
Inventors:
MITOREE EMU PONPIPOMU
ROBAATO ERU BUGIANESHI
JIEEMUSU SHII ROBINSU
TSUNNYUN SHIEN
ROBAATO ERU BUGIANESHI
JIEEMUSU SHII ROBINSU
TSUNNYUN SHIEN
Application Number:
JP6487082A
Publication Date:
November 08, 1982
Filing Date:
April 20, 1982
Export Citation:
Assignee:
MERCK & CO INC
International Classes:
A61K9/18; A61K47/42; C07H15/00; C07H15/04; C07H15/14; C07J9/00; C07K9/00; C07J31/00; C07J41/00; C07K1/113; (IPC1-7): A61K47/00; C07H13/12; C07H15/04; C07H15/14; C07J9/00; C07J41/00
Other References:
FEBS LETT=1980