Gambogic Acid Activates AMP-activated Protein Kinase in Mammalian Cells

Zhao, B., et al., 424(1), 100-4, Biochem Biophys Res Commun, 2012

Gambogic acid (GB), a known antitumor agent, activates AMP-activated protein kinase (AMPK) by increasing the phosphorylation of AMPKa and its downstream substrate in various cell lines. GB does this by physically interacting with the AMPKa subunit as measured by Octet RED system with a Kd of 7.81uM (similar Kd determined by quenching experiments). Kinetics measurements were performed using biotinylated AMPKa subunit immobilized onto Super Streptavidin biosensors. Association and dissociation rate constants were reported.

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