Efomycine M, a new specific inhibitor of selectin, impairs leukocyte adhesion and alleviates cutaneous inflammation

Michael P. Schön, Thomas Krahn, Margarete Schön, Maria L. Rodriguez, Horst Antonicek, Jeanette E. Schultz, Ralf J. Ludwig, Thomas M. Zollner, Erwin Bischoff, Klaus D. Bremm, Matthias Schramm, Kerstin Henninger, Roland Kaufmann, Harald P.M. Gollnick, Christina M. Parker, W. Henning Boehncke

112 Zitate (Scopus)

Abstract

Specific interference with molecular mechanisms guiding tissue localization of leukocytes may be of great utility for selective immunosuppressive therapies. We have discovered and characterized efomycines, a new family of selective small-molecule inhibitors of selectin functions. Members of this family significantly inhibited leukocyte adhesion in vitro. Efomycine M, which was nontoxic and showed the most selective inhibitory effects on selectin-mediated leukocyte-endothelial adhesion in vitro, significantly diminished rolling in mouse ear venules in vivo as seen by intravital microscopy. In addition, efomycine M alleviated cutaneous inflammation in two complementary mouse models of psoriasis, one of the most common chronic inflammatory skin disorders. Molecular modeling demonstrated a spatial conformation of efomycines mimicking naturally occurring selectin ligands. Efomycine M might be efficacious in the treatment of human inflammatory disorders through a similar mechanism.

OriginalspracheEnglisch
ZeitschriftNature Medicine
Jahrgang8
Ausgabenummer4
Seiten (von - bis)366-372
Seitenumfang7
ISSN1078-8956
DOIs
PublikationsstatusVeröffentlicht - 01.04.2002

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