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

Theresa A Lansdell; Sandra O'Reilly; Tracey Woolliscroft; Lauren M Azevedo; Daljinder K Kahlon; Stacy Hovde; J Justin McCormick; R William Henry; Joseph A Cornicelli; Jetze J Tepe

doi:10.1016/j.bmcl.2012.05.056

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

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4816-9. doi: 10.1016/j.bmcl.2012.05.056. Epub 2012 May 18.

Authors

Theresa A Lansdell¹, Sandra O'Reilly, Tracey Woolliscroft, Lauren M Azevedo, Daljinder K Kahlon, Stacy Hovde, J Justin McCormick, R William Henry, Joseph A Cornicelli, Jetze J Tepe

Affiliation

¹ Department of Chemistry, Michigan State University, East Lansing, MI, USA.

PMID: 22682057
DOI: 10.1016/j.bmcl.2012.05.056

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Administration, Oral
Animals
Arthritis, Experimental / drug therapy*
Arthritis, Experimental / immunology
Imidazolines / administration & dosage
Imidazolines / chemical synthesis
Imidazolines / therapeutic use*
Mice
Mice, Inbred BALB C
NF-kappa B / antagonists & inhibitors*
Tumor Necrosis Factor-alpha / biosynthesis
Tumor Necrosis Factor-alpha / immunology

Substances

Imidazolines
NF-kappa B
Tumor Necrosis Factor-alpha