Figure 7.
The phenanthrene, Lusianthrin, also directly activates AMPK through the ADaM-binding site. A, structure of Lusianthrin. B, AMPK activity of bacterially expressed recombinant α2β1γ1 in the presence of increasing concentrations of Lusianthridin or Lusianthridin. AMPK activity was determined using the HTRF KinEASE assay kit, and results are presented as fold increase in AMPK activity (±SEM, n = 3) relative to the activity in the absence of activator. C and D, pACC HTRF analysis of stable cell lines expressing β1 WT/S108A (C) or β2 WT/S108A (D) treated with Lusianthrin. Results are presented as the fold increase in pACC HTRF signal and are means ± SEM of at least three independent experiments. ADaM, allosteric drug and metabolite; AMPK, AMP-activated protein kinase; HTRF, Homogenous Time-Resolved Fluorescence; pACC, phospho-ACC.
