Isoliquiritigenin suppresses human T Lymphocyte activation via covalently binding cysteine 46 of IκB kinase.

ABSTRACT: The efficacious practice of precision personalized medicine requires a more exact understanding of the molecular mechanisms of drug, hence then it is necessary to identify the binding site of the drugs derived from natural sources. In the study, we investigated the suppressive effect and underlying mechanism of isoliquiritigenin (2',4',4-trihydroxychalcone; ILG), a phyto-flavonoid, on human T lymphocyte activation in vitro and in vivo. The results showed that ILG dose-dependently suppressed human T cell activation via suppressing IκBα phosphorylation and degradation, NF-κB nuclear translocation and IKKβ activity. Molecular docking results predicted that cysteine 46 (Cys-46) is probably the binding site of ILG on IKKβ, and this prediction has been validated by competition assay and kinase a

SUBMITTER: Yan F 

PROVIDER: S-EPMC5470962 | biostudies-literature | 2017 May

REPOSITORIES: biostudies-literature