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Small molecule inhibitors of NF-kB and JAK/STAT signal transduction pathways as promising anti-inflammatory therapeutics.

机译:NF-kB和JAK / STAT信号转导通路的小分子抑制剂有望成为抗炎治疗剂。

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摘要

In the current review, we discuss the role of NF-kB and JAK/STAT signaling pathways and their small molecule regulators in the therapy of inflammatory diseases. Considering potential harmful effects directly assigned to the COX-2 inhibition, novel therapeutically-relevant biological targets such as NF-kB and JAK/STAT signaling pathways have received a growing attention. Here we summarize recent progress in the identification and development of novel, clinically approved or evaluated small molecule regulators of these signaling cascades as promising anti-inflammatory therapeutics. In addition, we illustrate key structural modifications and bioisosteric transformations among these inhibitors to provide a helpful basis for further development of novel small molecule anti-inflammatory agents.
机译:在当前的审查中,我们讨论了NF-kB和JAK / STAT信号通路及其小分子调节剂在炎性疾病治疗中的作用。考虑到直接分配给COX-2抑制作用的潜在有害作用,新型与治疗相关的生物学靶标,例如NF-kB和JAK / STAT信号通路受到了越来越多的关注。在这里,我们总结了这些信号级联反应的新颖,临床认可或评估的小分子调节剂的鉴定和开发的最新进展,这些调节剂是有希望的抗炎治疗剂。此外,我们举例说明了这些抑制剂之间的关键结构修饰和生物立体转换,为进一步开发新型小分子抗炎药提供了有用的基础。

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