Pub. Date : 2020
PMID : 32082480
7 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Farrerol Directly Targets GSK-3beta to Activate Nrf2-ARE Pathway and Protect EA.hy926 Cells against Oxidative Stress-Induced Injuries. | farrerol | glycogen synthase kinase 3 alpha | Homo sapiens |
| 2 | Our results demonstrated that farrerol could specifically target Nrf2 negative regulator GSK-3beta and inhibit its kinase activity. | farrerol | glycogen synthase kinase 3 alpha | Homo sapiens |
| 3 | Mechanistic studies proved that farrerol could induce an inhibitory phosphorylation of GSK-3beta at Ser9 without affecting the expression level of total GSK-3beta protein and promote the nuclear translocation of Nrf2 as well as the mRNA and protein expression of its downstream target genes heme oxygenase-1 (HO-1) and NAD(P)H: quinone oxidoreductase 1 (NQO1) in EA.hy926 cells. | farrerol | glycogen synthase kinase 3 alpha | Homo sapiens |
| 4 | Further studies performed with GSK-3beta siRNA and specific inhibitor lithium chloride (LiCl) confirmed that GSK-3beta inhibition was involved in farrerol-mediated endothelial protection and Nrf2 signaling activation. | farrerol | glycogen synthase kinase 3 alpha | Homo sapiens |
| 5 | Further studies performed with GSK-3beta siRNA and specific inhibitor lithium chloride (LiCl) confirmed that GSK-3beta inhibition was involved in farrerol-mediated endothelial protection and Nrf2 signaling activation. | farrerol | glycogen synthase kinase 3 alpha | Homo sapiens |
| 6 | Moreover, molecular docking and molecular dynamics studies revealed that farrerol could bind to the ATP pocket of GSK-3beta, which is consistent with the ATP-competitive kinetic behavior. | farrerol | glycogen synthase kinase 3 alpha | Homo sapiens |
| 7 | Collectively, our results firstly demonstrate that farrerol could attenuate endothelial oxidative stress by specifically targeting GSK-3beta and further activating the Nrf2-ARE signaling pathway. | farrerol | glycogen synthase kinase 3 alpha | Homo sapiens |