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Merck

A protein kinase involved in the regulation of inflammatory cytokine biosynthesis.

Nature (1994-12-22)
J C Lee, J T Laydon, P C McDonnell, T F Gallagher, S Kumar, D Green, D McNulty, M J Blumenthal, J R Heys, S W Landvatter, J E Strickler, M M McLaughlin, I R Siemens, S M Fisher, G P Livi, J R White, J L Adams, P R Young
RESUMEN

Production of interleukin-1 and tumour necrosis factor from stimulated human monocytes is inhibited by a new series of pyridinyl-imidazole compounds. Using radiolabelled and radio-photoaffinity-labelled chemical probes, the target of these compounds was identified as a pair of closely related mitogen-activated protein kinase homologues, termed CSBPs. Binding of the pyridinyl-imidazole compounds inhibited CSBP kinase activity and could be directly correlated with their ability to inhibit cytokine production, suggesting that the CSBPs are critical for cytokine production.