Attenuation of collagen-induced arthritis by orally available imidazoline-based NF-κB inhibitors

The pathogenesis of rheumatoid arthritis is mainly driven by NF-κB-mediated production of cytokines, such as TNF-α. We report herein that the orally available imidazoline-based NF-κB inhibitor, TCH-013, was found to significantly reduce TNF-α signaling and attenuate collagen antibody induced arthrit...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 22; no. 14; pp. 4816 - 4819
Main Authors Lansdell, Theresa A., O’Reilly, Sandra, Woolliscroft, Tracey, Azevedo, Lauren M., Kahlon, Daljinder K., Hovde, Stacy, McCormick, J. Justin, Henry, R. William, Cornicelli, Joseph A., Tepe, Jetze J.
Format Journal Article
LanguageEnglish
Published England Elsevier Ltd 15.07.2012
Subjects
Administration, Oral
Animals
Arthritis, Experimental - drug therapy
Arthritis, Experimental - immunology
chemistry
collagen
Cytokines
Imidazolines
Imidazolines - administration & dosage
Imidazolines - chemical synthesis
Imidazolines - therapeutic use
Inflammation
Mice
Mice, Inbred BALB C
NF-kappa B - antagonists & inhibitors
NF-κB
pathogenesis
Rheumatoid arthritis
transcription factor NF-kappa B
tumor necrosis factor-alpha
Tumor Necrosis Factor-alpha - biosynthesis
Tumor Necrosis Factor-alpha - immunology
NF-κB
Imidazolines
Inflammation
Cytokines
Rheumatoid arthritis
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Summary:The pathogenesis of rheumatoid arthritis is mainly driven by NF-κB-mediated production of cytokines, such as TNF-α. We report herein that the orally available imidazoline-based NF-κB inhibitor, TCH-013, was found to significantly reduce TNF-α signaling and attenuate collagen antibody induced arthritis in BALB/c mice.
Bibliography:http://dx.doi.org/10.1016/j.bmcl.2012.05.056
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.05.056