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

Schon, Michael P.
Krahn, Thomas
Schon, Margarete
Rodriguez, Maria-L
Antonicek, Horst
Schultz, Jeanette E.
Ludwig, Ralf J.
Zollner, Thomas Matthias
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Published in Nature medicine. 2002, vol. 8, no. 4, p. 366-372
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.
Keywords AnimalsAnti-Inflammatory Agents, Non-Steroidal/chemistry/*pharmacologyCell Adhesion/drug effectsCell Movement/drug effectsE-Selectin/*drug effectsFemaleHumansLeukocytes/*drug effectsMacrolides/chemistry/*pharmacologyMiceMice, Inbred C57BLMice, SCIDModels, MolecularOligosaccharides/chemistryPsoriasis/*drug therapy/pathologySkin TransplantationStreptomyces/chemistryTransplantation, Heterologous
PMID: 11927942
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SCHON, Michael P. et al. Efomycine M, a new specific inhibitor of selectin, impairs leukocyte adhesion and alleviates cutaneous inflammation. In: Nature medicine, 2002, vol. 8, n° 4, p. 366-372. doi: 10.1038/nm0402-366

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Deposited on : 2013-09-20

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