Abstract
A new class of high molecular weight polysulfated PEO dendrimer-like glycopolymer has been synthesized by a combination of arm-first and core-first methodologies followed by trichloroacetimidate glycosidation as a facile bioconjugation strategy. An L-selectin antagonist was identified that exhibits 103-fold greater activity than other multivalent sLex glycopolymers and 20-50 times greater potency than other linear heparinoids. A significant reduction in inflammatory cell recruitment was observed in vivo.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemistry*
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology
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Glycosylation
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Humans
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L-Selectin / chemistry
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L-Selectin / metabolism
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Lactose / analogs & derivatives*
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Lactose / chemistry
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Lactose / pharmacology*
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Mice
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Oligosaccharides / chemistry
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Oligosaccharides / metabolism
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Polyethylene Glycols / chemistry*
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Polyethylene Glycols / pharmacology*
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Sialyl Lewis X Antigen
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U937 Cells
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Oligosaccharides
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Sialyl Lewis X Antigen
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L-Selectin
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Polyethylene Glycols
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Lactose