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Glycoprotein-inspired materials promote the proteolytic release of cell surface L-selectin.

Abstract：

:The proteolytic release, or shedding, of a cell surface protein can serve a regulatory role; the process liberates a soluble form of the protein into circulation while downregulating its cell surface concentration. The characteristics that render a protein susceptible to proteolytic cleavage are not known. We hypothesized that the clustering of a protein at the cell surface might target it for proteolysis. To test this hypothesis, we synthesized molecules that display multiple copies of sulfated galactose residues, termed neoglycopolymers, that are designed to mimic natural ligands for the cell adhesion protein L-selectin. We found that treatment of human neutrophils with the neoglycopolymers resulted in a dose-dependent loss of L-selectin from the cell surface, while monovalent compounds and unsulfated neoglycopolymers had no effect. Because L-selectin is an important mediator in the inflammatory response, such compounds could lead to novel antiinflammatory drugs. Moreover, molecules that control receptor shedding can be used to alter cellular responsiveness to specific ligands or to promote responses at distal sites; consequently, these results have broad implications for regulating the location and presentation of important biomolecules.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Gordon EJ,Strong LE,Kiessling LL

doi

10.1016/s0968-0896(98)00122-9

subject

Has Abstract

pub_date

1998-08-01 00:00:00

pages

1293-9

issue

8

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(98)00122-9

journal_volume

6

pub_type

杂志文章

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