Title : Inhibition of NF-kappa B activation through targeting I kappa B kinase by celastrol, a quinone methide triterpenoid.

Pub. Date : 2006 Nov 15

PMID : 16984800






7 Functional Relationships(s)
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1 Inhibition of NF-kappa B activation through targeting I kappa B kinase by celastrol, a quinone methide triterpenoid. celastrol nuclear factor kappa B subunit 1 Homo sapiens
2 Importantly, celastrol inhibited IKK activity and the constitutively active IKK beta activity in a dose-dependent manner without either affecting the NF-kappa B activation induced by RelA over-expression or directly suppressing the DNA-binding of activated NF-kappa B. celastrol nuclear factor kappa B subunit 1 Homo sapiens
3 However, mutation of cysteine 179 in the activation loop of IKK beta abolished sensitivity towards to celastrol, suggesting that celastrol suppressed the NF-kappa B activation by targeting cysteine 179 in the IKK. celastrol nuclear factor kappa B subunit 1 Homo sapiens
4 To verify that celastrol is a NF-kappa B inhibitor, we investigated its effect on some NF-kappa B target genes expressions. celastrol nuclear factor kappa B subunit 1 Homo sapiens
5 To verify that celastrol is a NF-kappa B inhibitor, we investigated its effect on some NF-kappa B target genes expressions. celastrol nuclear factor kappa B subunit 1 Homo sapiens
6 Taken together, this study extends our understanding on the molecular mechanisms underlying the anti-inflammatory and anti-cancer activities of celastrol and celastrol-containing medicinal plant, which would be a valuable candidate for the intervention of NF-kappa B-dependent pathological conditions. celastrol nuclear factor kappa B subunit 1 Homo sapiens
7 Taken together, this study extends our understanding on the molecular mechanisms underlying the anti-inflammatory and anti-cancer activities of celastrol and celastrol-containing medicinal plant, which would be a valuable candidate for the intervention of NF-kappa B-dependent pathological conditions. celastrol nuclear factor kappa B subunit 1 Homo sapiens