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Biological Activity:
TAK-242 (resatorvid), a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, inhibits the production of lipopolysaccharide-induced inflammatory mediators by binding to the intracellular domain of TLR4. Cys747 in TLR4 has been identified previously as the binding site of TAK-242. However, the mechanism by which TAK-242 inhibits TLR4 signaling after binding to TLR4 remains unknown. The present study demonstrated, using coimmunoprecipitation, that TAK-242 interferes with protein-protein interactions between TLR4 and its adaptor molecules.TAK-242 is in treatment of sepsis and septic shock.
References:
1.Naoko Matsunaga et al. TAK-242 (Resatorvid), a Small-Molecule Inhibitor of Toll-Like Receptor (TLR) 4 Signaling, Binds Selectively to TLR4 and Interferes with Interactions between TLR4 and Its Adaptor Molecules. Molecular Pharmacology January 2011 vol. 79 no. 1 34-41
2.Xie H, Zhou H, Wang H, Chen D, Xia L, Wang T, Yan J.Anti-β(2)GPI/β(2)GPI induced TF and TNF-α expression in monocytes involving both TLR4/MyD88 and TLR4/TRIF signaling pathways.Mol Immunol. 2012 Sep 7;53(3):246-254.
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C14205 TAK-242(Resatorvid) (243984-11-4)