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

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

  • Bioorg Med Chem. 1997 Jan;5(1):49-64. doi: 10.1016/s0968-0896(96)00212-x.
T F Gallagher 1,  G L Seibel,  S Kassis,  J T Laydon,  M J Blumenthal,  J C Lee,  D Lee,  J C Boehm,  S M Fier-Thompson,  J W Abt,  M E Soreson,  J M Smietana,  R F Hall,  R S Garigipati,  P E Bender,  K F Erhard,  A J Krog,  G A Hofmann,  P L Sheldrake,  P C McDonnell,  S Kumar,  P R Young,  J L Adams
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406-0939, USA.
PMID: 9043657 DOI: 10.1016/s0968-0896(96)00212-x
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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