Epoxyquinol B, a Naturally Occurring Pentaketide Dimer, Inhibits NF-κB Signaling by Crosslinking TAK1

摘要: Several epoxyquinoids interfere with NF-κB signaling by targeting IKKβ or NF-κB. We report that epoxyquinol B (EPQB), classified as an epoxyquiniod, inhibits through inhibition of the TAK1 complex, a factor upstream and cDNA microarray analysis revealed EPQB decreased TNF-α-induced expression target genes. covalently bound to recombinant TAK1-TAB1 fusion protein in vitro, inhibited its kinase activity. Furthermore, vitro/in situ treatment resulted ladder-like hypershift bands. reported recently crosslinks proteins via cysteine residues opening two epoxides, our current results suggest crosslinking itself other proteins.