吡啶基咪唑在蛋白质水平上抑制白细胞介素-1和肿瘤坏死因子的产生。
Pyridinyl imidazoles inhibit IL-1 and TNF production at the protein level.
作者信息
Young P, McDonnell P, Dunnington D, Hand A, Laydon J, Lee J
机构信息
Department of Molecular Genetics, SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406-0939.
出版信息
Agents Actions. 1993;39 Spec No:C67-9. doi: 10.1007/BF01972723.
The mechanism by which SK&F 86002 and other pyridinyl imidazoles inhibit the production of IL-1 and TNF from LPS-stimulated human monocytes was examined. Inhibition of IL-1 and TNF production was found to depend on the time of addition of SK&F 86002, with diminishing effect when added more than 2 h after LPS stimulation. Analysis of Western blots confirmed that both intracellular IL-1 beta and extracellular TNF were significantly reduced in response to SK&F 86002, but these reductions were not paralleled by changes in IL-1 and TNF mRNA. 35S methionine pulse and pulse-chase studies on IL-1 biosynthesis suggest that significant inhibition by SK&F 86002 and related compounds occurs at the translational level.
研究了SK&F 86002和其他吡啶基咪唑抑制脂多糖刺激的人单核细胞产生白细胞介素-1（IL-1）和肿瘤坏死因子（TNF）的机制。发现IL-1和TNF产生的抑制取决于SK&F 86002的添加时间，在脂多糖刺激后超过2小时添加时效果减弱。蛋白质免疫印迹分析证实，响应SK&F 86002时，细胞内IL-1β和细胞外TNF均显著降低，但这些降低与IL-1和TNF mRNA的变化并不平行。对IL-1生物合成的35S甲硫氨酸脉冲和脉冲追踪研究表明，SK&F 86002及相关化合物在翻译水平上有显著抑制作用。
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