BAY 11-7082 is a broad-spectrum inhibitor with anti-inflammatory activity against multiple targets.
BAY 11-7082 is a broad-spectrum inhibitor with anti-inflammatory activity against multiple targets.
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DOI：
10.1155/2012/416036
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发表时间：
2012
影响因子：
4.6
通讯作者：
Cho JY
中科院分区：
文献类型：
--
作者：
Lee J;Rhee MH;Kim E;Cho JY
BAY 11-7082 (BAY) 是一种 κB 激酶 (IKK) 抑制剂，具有抗癌、神经保护和抗炎作用等药理活性。在这项研究中，进一步表征了 BAY 药理学目标途径，以确定该化合物如何同时抑制各种反应。原代和癌性（RAW264.7细胞）巨噬细胞被脂多糖（Toll样受体4的配体）激活。正如之前报道的，BAY强烈抑制一氧化氮、前列腺素E2和肿瘤坏死因子-α的产生，并减少核因子-κB主要亚基p65的易位及其上游信号转导事件，例如IκBα、IKK和Akt的磷酸化。此外，BAY还通过抑制细胞外信号相关激酶、p38、TANK结合蛋白和Janus激酶-2的磷酸化或激活，抑制激活蛋白-1、干扰素调节因子-3、信号转导子和转录激活子-1的易位和激活。这些数据强烈表明，BAY 是一种具有多个靶点的抑制剂，可以作为开发具有多个炎症反应靶点的强效抗炎药物的先导化合物。
BAY 11-7082 (BAY) is an inhibitor of κB kinase (IKK) that has pharmacological activities that include anticancer, neuroprotective, and anti-inflammatory effects. In this study, BAY-pharmacological target pathways were further characterized to determine how this compound simultaneously suppresses various responses. Primary and cancerous (RAW264.7 cells) macrophages were activated by lipopolysaccharide, a ligand of toll-like receptor 4. As reported previously, BAY strongly suppressed the production of nitric oxide, prostaglandin E2, and tumor necrosis factor-α and reduced the translocation of p65, major subunit of nuclear factor-κB, and its upstream signaling events such as phosphorylation of IκBα, IKK, and Akt. In addition, BAY also suppressed the translocation and activation of activator protein-1, interferon regulatory factor-3, and signal transducer and activator of transcription-1 by inhibiting the phosphorylation or activation of extracellular signal-related kinase, p38, TANK-binding protein, and Janus kinase-2. These data strongly suggest that BAY is an inhibitor with multiple targets and could serve as a lead compound in developing strong anti-inflammatory drugs with multiple targets in inflammatory responses.
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DOI：
10.1196/annals.1397.071
发表时间：
2007-01-01
期刊：
SIGNAL TRANSDUCTION PATHWAYS, PT D
影响因子：
--
作者：
Dos Santos, S.;Delattre, A.-I.;Raes, M.
通讯作者：
Raes, M.
影响因子：
2.7
作者：
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Alvarez, E
影响因子：
6.1
作者：
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通讯作者：
Kang, Seog Youn
影响因子：
1.6
作者：
Kim, Min Ho;Yoo, Dae Sung;Cho, Jae Youl
通讯作者：
Cho, Jae Youl
影响因子：
4.8
作者：
Clark, Kristopher;Plater, Lorna;Cohen, Philip
通讯作者：
Cohen, Philip