SB 203580是一种吡啶咪唑类p38 MAPK抑制剂(IC50=0.3-0.5 µM)。SB 203580抑制IL-2诱导的T细胞增殖(IC50=3-5 µM),激活人肝细胞中ERK和JNK的表达,并激活下游ERK-P、JNK-P和c-Jun-P表达。SB 203580参与多种炎症反应和细胞应激反应。另外,SB 203580通过抑制RIPK2表达从而降低DENV感染的HepG2细胞凋亡,并诱导人肝癌细胞自噬作用。在BALB/c小鼠中,SB 203580降低子宫内膜病变的重量和大小,并降低腹膜细胞中IL-1β、TNF-α、MMP-2和MMP-9 mRNA水平。
参考文献
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[2]Crawley JB, et al. T Cell Proliferation in Response to Interleukins 2 and 7 Requires p38MAP Kinase Activation. J. Biol. Chem. 272: 15023–15027(1997).
[3] Zhang H, et al. Induction of autophagy in hepatocellular carcinoma cells by SB203580 requires activation of AMPK and DAPK but not p38 MAPK. Apoptosis 17(4):325-334 (2012).
[4] Sreekanth GP, et al. SB203580 Modulates p38 MAPK Signaling and Dengue Virus-Induced Liver Injury by Reducing MAPKAPK2, HSP27, and ATF2 Phosphorylation. PLoS ONE 11(2): e0149486 (2016).
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[6] Zhou WD, et al. SB203580, a p38 mitogen-activated protein kinase inhibitor, suppresses the development of endometriosis by down-regulating proinflammatory cytokines and proteolytic factors in a mouse model. Hum. Reprod. 25 (12): 3110-3116(2010).
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