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Regulation of stress-induced cytokine production by pyridinylimidazoles; inhibition of CSBP kinase |
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| Authors: | TF Gallagher GL Seibel S Kassis JT Laydon MJ Blumenthal JC Lee D Lee JC Boehm SM Fier-Thompson JW Abt ME Soreson JM Smietana RF Hall RS Garigipati PE Bender KF Erhard AJ Krog GA Hofmann PL Sheldrake PC McDonnell S Kumar PR Young JL Adams |
| Affiliation: | Department of Medicinal Chemistry, SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406-0939, USA. |
| 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, PKC alpha and ERK kinase activity is observed. |
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