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

doi:10.1038/nm0402-366

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

Clinic of Dermatology, Allergology and Venerology

112 Citations (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.

Original language	English
Journal	Nature Medicine
Volume	8
Issue number	4
Pages (from-to)	366-372
Number of pages	7
ISSN	1078-8956
DOIs	https://doi.org/10.1038/nm0402-366
Publication status	Published - 01.04.2002

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Schön, M. P., Krahn, T., Schön, M., Rodriguez, M. L., Antonicek, H., Schultz, J. E., Ludwig, R. J., Zollner, T. M., Bischoff, E., Bremm, K. D., Schramm, M., Henninger, K., Kaufmann, R., Gollnick, H. P. M., Parker, C. M., & Boehncke, W. H. (2002). Efomycine M, a new specific inhibitor of selectin, impairs leukocyte adhesion and alleviates cutaneous inflammation. Nature Medicine, 8(4), 366-372. https://doi.org/10.1038/nm0402-366

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

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.",

author = "Sch{\"o}n, {Michael P.} and Thomas Krahn and Margarete Sch{\"o}n and Rodriguez, {Maria L.} and Horst Antonicek and Schultz, {Jeanette E.} and Ludwig, {Ralf J.} and Zollner, {Thomas M.} and Erwin Bischoff and Bremm, {Klaus D.} and Matthias Schramm and Kerstin Henninger and Roland Kaufmann and Gollnick, {Harald P.M.} and Parker, {Christina M.} and Boehncke, {W. Henning}",

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Schön, MP, Krahn, T, Schön, M, Rodriguez, ML, Antonicek, H, Schultz, JE, Ludwig, RJ, Zollner, TM, Bischoff, E, Bremm, KD, Schramm, M, Henninger, K, Kaufmann, R, Gollnick, HPM, Parker, CM & Boehncke, WH 2002, 'Efomycine M, a new specific inhibitor of selectin, impairs leukocyte adhesion and alleviates cutaneous inflammation', Nature Medicine, vol. 8, no. 4, pp. 366-372. https://doi.org/10.1038/nm0402-366

TY - JOUR

T1 - Efomycine M, a new specific inhibitor of selectin, impairs leukocyte adhesion and alleviates cutaneous inflammation

AU - Schön, Michael P.

AU - Krahn, Thomas

AU - Schön, Margarete

AU - Rodriguez, Maria L.

AU - Antonicek, Horst

AU - Schultz, Jeanette E.

AU - Ludwig, Ralf J.

AU - Zollner, Thomas M.

AU - Bischoff, Erwin

AU - Bremm, Klaus D.

AU - Schramm, Matthias

AU - Henninger, Kerstin

AU - Kaufmann, Roland

AU - Gollnick, Harald P.M.

AU - Parker, Christina M.

AU - Boehncke, W. Henning

PY - 2002/4/1

Y1 - 2002/4/1

N2 - 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.

AB - 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.

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C2 - 11927942

AN - SCOPUS:0036117531

SN - 1078-8956

VL - 8

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EP - 372

JO - Nature Medicine

JF - Nature Medicine

IS - 4

ER -

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

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