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. 2009 Mar 15;19(6):1722-5.
doi: 10.1016/j.bmcl.2009.01.088. Epub 2009 Jan 30.

Identification of a selective thieno[2,3-c]pyridine inhibitor of COT kinase and TNF-alpha production

Kevin Cusack  1 , Hamish Allen, Agnieszka Bischoff, Anca Clabbers, Richard Dixon, Shannon Fix-Stenzel, Michael Friedman, Yvette Gaumont, Dawn George, Thomas Gordon, Pintipa Grongsaard, Bernd Janssen, Yong Jia, Maria Moskey, Christopher Quinn, Andres Salmeron, Christine Thomas, Grier Wallace, Neil Wishart, Zhengtian Yu
Affiliations

Identification of a selective thieno[2,3-c]pyridine inhibitor of COT kinase and TNF-alpha production

Kevin Cusack et al. Bioorg Med Chem Lett. .

Abstract

COT (Tpl2 in mice) is a serine/threonine MAP3 kinase that regulates production of TNF-alpha and other pro-inflammatory cytokines such as IL-1beta via the ERK/MAP kinase pathway. As TNF-alpha and IL-1beta are clinically validated targets for therapeutic intervention in rheumatoid arthritis (RA), blocking COT provides a potential avenue for amelioration of disease. Herein we describe identification of a cellular active selective small molecule inhibitor of COT kinase.

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