Title:
SOLID- AND SOLUTION -PHASE SYNTHESIS OF HEPARIN AND OTHER GLYCOSAMINOGLYCANS
Document Type and Number:
WIPO Patent Application WO2002058633
Kind Code:
A3
Abstract:
Described is a modular, general synthetic strategy for the preparation in solution and on a solid support of heparin, heparin-like glycosaminoglycans, glycosaminoglycans and non-natural analogs of each of them. Additionally, the modular strategy provides the basis for the preparation of combinatorial libraries and parallel libraries of defined glycosaminoglycan oligosaccharides. The defined glycosaminoglycan structures may be used in high-throughput screening experiments to identify carbohydrate sequences that regulate a host of recognition and signal-transduction processes. The determination of specifi sequences involved in receptor binding holds great promise for the develpment of molecular tools which will allow modulation of processes underlying viral entry, angiog enesis, kidney diseases and diseases of the control nervous system. Notably, the present invention enables the automated synthesis of glycosaminoglycans in much the same fashion that peptides and oligonucleotides are currently assembled.
Inventors:
SEEBERGER PETER H
ORGUEIRA HERNAN
SCHELL PETER
ORGUEIRA HERNAN
SCHELL PETER
Application Number:
PCT/US2002/001772
Publication Date:
October 17, 2002
Filing Date:
January 22, 2002
Export Citation:
Assignee:
MASSACHUSETTS INST TECHNOLOGY (US)
International Classes:
C07H3/04; C07H3/06; C08B37/00; (IPC1-7): A01N43/04; A61K31/715
Other References:
KOSHIDA ET AL.: "Synthesis and biological activity of oligomer-model compounds containing units of a key platelet-binding disaccharide of heparin", TERAHEDRON LETTERS, no. 40, 1999, pages 5725 - 5728, XP000417550
KOVENSKY ET AL.: "Binding of heparan sulfate to fibroblast growth factor-2. Total synthesis of a putative pentasaccharide binding site", TETRAHEDRON: ASYMMETRY, vol. 7, no. 11, 1996, pages 3119 - 3128, XP004068971
SUDA ET AL.: "Synthesis and biological activity of a model disaccharide containing to key unit in heparin for binding to platelets", TETRAHEDRON LETTERS, vol. 37, no. 7, 1996, pages 1053 - 1056, XP004030226
See also references of EP 1353556A4
KOVENSKY ET AL.: "Binding of heparan sulfate to fibroblast growth factor-2. Total synthesis of a putative pentasaccharide binding site", TETRAHEDRON: ASYMMETRY, vol. 7, no. 11, 1996, pages 3119 - 3128, XP004068971
SUDA ET AL.: "Synthesis and biological activity of a model disaccharide containing to key unit in heparin for binding to platelets", TETRAHEDRON LETTERS, vol. 37, no. 7, 1996, pages 1053 - 1056, XP004030226
See also references of EP 1353556A4
Download PDF: