Bioorganic and Medicinal Chemistry p. 49 - 64 (1997)
Update date:2022-09-26
Topics:
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.
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, PKα and ERK kinase activity is observed.
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Doi:10.1021/acs.jmedchem.0c02266
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