Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: discovery and in vivo activity of selective pyrazolo[1,5-a]pyrimidine inhibitors using a focused library and structure-based optimization approach. [electronic resource]
- Journal of medicinal chemistry Aug 2012
- 6700-15 p. digital
Publication Type: Journal Article
1520-4804
10.1021/jm300411k doi
Animals Anti-Inflammatory Agents, Non-Steroidal--chemical synthesis Cell Line Crystallography, X-Ray HSP27 Heat-Shock Proteins--metabolism Humans Intracellular Signaling Peptides and Proteins--antagonists & inhibitors Lipopolysaccharides--pharmacology Male Mice Mice, Inbred C57BL Models, Molecular Phosphorylation Protein Conformation Protein Serine-Threonine Kinases--antagonists & inhibitors Pyrazoles--chemical synthesis Pyrimidines--chemical synthesis Shock, Septic--metabolism Small Molecule Libraries Stereoisomerism Structure-Activity Relationship Tumor Necrosis Factor-alpha--biosynthesis