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首页> 外文期刊>Drug discovery today >Targeted library design for the generation of actives against biological targets Peptidomimetic inhibitors of myeloid differentiation factor 88
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Targeted library design for the generation of actives against biological targets Peptidomimetic inhibitors of myeloid differentiation factor 88

机译:针对生物靶标生成活性物质的靶向文库设计髓样分化因子88的拟肽抑制剂

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摘要

The nuclear transcription factor-KappaB (NF-KappaB~a) is known to be involved in a host of disease states, such as inflammation, immunity and apoptosis. In response to damaging stimuli, NF-KappaB activation is observed in most cells involved in the immune response, such as neutrophils, macro-phages and lymphocytes. Thus, the immediate and transitory activation of NF-kB is important to the normal physiological response to pathogenic damage. NF-kB recognizes consensus sequences for the enhancers of genes coding for pro-inflammatory cytokines (e.g.TNF, IL-1, IL-2, IL-6 and IL-11), chemokines (e.g. IL-8, RANTES and MIP-1R), adhesive molecules (ICAM-1, VCAM-1, E-selectin), and enzymes producing inflammatory mediators (iNOS and COX2).
机译:已知核转录因子-KappaB(NF-KappaB_a)涉及许多疾病状态,例如炎症,免疫力和细胞凋亡。作为对破坏性刺激的反应,在大多数参与免疫反应的细胞(如嗜中性粒细胞,巨噬细胞和淋巴细胞)中都观察到了NF-κB的活化。因此,NF-kB的立即和短暂激活对于对病原体损害的正常生理反应很重要。 NF-kB识别编码促炎性细胞因子(例如TNF,IL-1,IL-2,IL-6和IL-11),趋化因子(例如IL-8,RANTES和MIP-1R)的基因增强子的共有序列),黏附分子(ICAM-1,VCAM-1,E-选择素)和产生炎性介质的酶(iNOS和COX2)。

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