Author/Authors :
Timothy F. Gallagher، نويسنده , , George L. Seibel، نويسنده , , Shouki Kassis، نويسنده , , Jeffrey T. Laydon، نويسنده , , Mary Jane Blumenthal، نويسنده , , John C. Lee، نويسنده , , Dennis Lee، نويسنده , , Jeffrey C. Boehm، نويسنده , , Susan M. Fier-Thompson، نويسنده , , Jeffrey W. Abt، نويسنده , , Margaret E. Soreson، نويسنده , , Juanita M. Smietana، نويسنده , , Ralph F. Hall، نويسنده , , Ravi S. Garigipati، نويسنده ,
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, PKCα and ERK kinase activity is observed.
