Regulation of stress-induced cytokine production by pyridinylimidazoles; inhibition of CSBP kinase

…, JC Lee, D Lee, JC Boehm, SM Fier-Thompson…

Index: Gallagher, Timothy F.; Seibel, George L.; Kassis, Shouki; Laydon, Jeffrey T.; Blumenthal, Mary Jane; Lee, John C.; Lee, Dennis; Boehm, Jeffrey C.; Fier-Thompson, Susan M.; Abt, Jeffrey W.; Soreson, Margaret E.; Smietana, Juanita M.; Hall, Ralph F.; Garigipati, Ravi S.; Bender, Paul E.; Erhard, Karl F.; Krog, Arnold J.; Hofmann, Glenn A.; Sheldrake, Peter L.; McDonnell, Peter C.; Kumar, Sanjay; Young, Peter R.; Adams, Jerry L. Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 1 p. 49 - 64

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Citation Number: 242

Abstract

Members of three classes of pyridinylimidazoles bind with varying affinities to CSBP (p38) kinase which is a member of a stress-induced signal transduction pathway. Based upon SAR and protein homology modeling, the pharmacophore and three potential modes of binding to the enzyme are presented. For a subset of pyridinylimidazoles, binding is shown to correlate with inhibition of CSBP kinase activity, whereas no significant inhibition of PKA ...