Inhibiting NF-κB activation by small molecules as a therapeutic strategy.
Inhibiting NF-κB activation by small molecules as a therapeutic strategy.
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通过小分子抑制 NF-κB 激活作为治疗策略。
DOI：
10.1016/j.bbagrm.2010.05.004
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发表时间：
2010-10
影响因子：
4.7
通讯作者：
Aggarwal, Bharat B.
中科院分区：
文献类型：
--
作者：
Gupta, Subash C.;Sundaram, Chitra;Reuter, Simone;Aggarwal, Bharat B.
由于核因子-κB(NF-κB，核因子-κB)是一种普遍表达的促炎性转录因子，可调控细胞转化、存活、增殖、侵袭、血管生成、转移和炎症等多个基因的表达，因此，核因子-CFB信号通路已成为药物干预的潜在靶点。多种药物可通过典型和非典型途径激活核因子-κB。经典途径涉及多个步骤，包括核转录因子-κB抑制物(IκBα，IκBα)的磷酸化、泛化和降解，导致核转位，随后是p65的磷酸化、乙酰化和甲基化、κ结合和基因转录。因此，可以抑制蛋白激酶、蛋白磷酸酶、蛋白酶体、泛素化、乙酰化、甲基化和dna结合步骤的药物已被确定为NF-κB抑制剂。在这里，我们回顾了抑制核因子-κB激活的小分子，从而可能具有治疗潜力。
Because nuclear factor-κB (NF-κB) is a ubiquitously expressed proinflammatory transcription factor that regulates the expression of over 500 genes involved in cellular transformation, survival, proliferation, invasion, angiogenesis, metastasis, and inflammation, the NF-κB signaling pathway has become a potential target for pharmacological intervention. A wide variety of agents can activate NF-κB through canonical and noncanonical pathways. Canonical pathway involves various steps including the phosphorylation, ubiquitnation, and degradation of the inhibitor of NF-κB (IκBα), which leads to the nuclear translocation of the p50- p65 subunits of NF-κB followed by p65 phosphorylation, acetylation and methylation, DNA binding, and gene transcription. Thus, agents that can inhibit protein kinases, protein phosphatases, proteasomes, ubiquitnation, acetylation, methylation, and DNA binding steps have been identified as NF-κB inhibitors. Here, we review the small molecules that suppress NF-κB activation and thus may have therapeutic potential.
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