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

Autor:	Jeffrey T. Laydon, Glenn A. Hofmann, Jeffrey C. Boehm, Jeffrey W. Abt, Margaret E. Soreson, Susan M. Fier-Thompson, Juanita M. Smietana, Peter R. Young, Timothy Francis Gallagher, John C. Lee, Mary Jane Blumenthal, Arnold J. Krog, Ralph Hall, Dennis Lee, Paul Elliot Bender, Karl F. Erhard, Ravi Shanker Garigipati, Jerry L. Adams, Peter C. McDonnell, George Leslie Seibel, Shouki Kassis, Sanjay Kumar, Peter L. Sheldrake
Rok vydání:	1997
Předmět:	Models Molecular Magnetic Resonance Spectroscopy Protein Kinase C-alpha Clinical Biochemistry Pharmaceutical Science Mitogen-activated protein kinase kinase MAP3K7 Biochemistry p38 Mitogen-Activated Protein Kinases Mass Spectrometry Cell Line Structure-Activity Relationship Stress Physiological Drug Discovery Humans Kinase activity Enzyme Inhibitors Molecular Biology Protein Kinase C Mitogen-Activated Protein Kinase 3 biology MAP kinase kinase kinase Cyclin-dependent kinase 4 Kinase Chemistry Organic Chemistry Imidazoles Cyclic AMP-Dependent Protein Kinases Cell biology Isoenzymes Calcium-Calmodulin-Dependent Protein Kinases biology.protein Molecular Medicine Cytokines Cyclin-dependent kinase 9 Signal transduction Mitogen-Activated Protein Kinases
Zdroj:	Bioorganicmedicinal chemistry. 5(1)
ISSN:	0968-0896
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4e122df6ffe903523b617fc84550c0c https://pubmed.ncbi.nlm.nih.gov/9043657 Zobrazit plný text záznamu Full Text from ScienceDirect