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Journal: Endocrinology
Article Title: Nongenomic ERα-AMPK Signaling Regulates Sex-Dependent Bcrp Transport Activity at the Blood-Brain Barrier
doi: 10.1210/endocr/bqae081
Figure Lengend Snippet: Signaling downstream of ERα involves AMPK. (A) Inhibition Akt and PI3K does not block E2-elicited decrease in specific Bcrp transport activity. (B) Treatment with an inhibitor of AMPK completely attenuates E2-elicited decrease in specific Bcrp transport activity. (C) Western blots of MBC cytosolic fractions showing increase in phosphorylated AMPKβ1 following exposure of MBCs to 1 nM E2 for 30 minutes. (D) Abbreviated working model. Each bar or point represents the mean value for 10 to 18 capillaries from a single isolation with tissue pooled from 5 mice. SEM bars depict variability and units are arbitrary fluorescence. Statistical comparisons: ***P < .001. Abbreviations: Bcrp, breast cancer resistance protein; DMD, dorsomorphin dihydrochloride; E2, 17β-estradiol; ERα, estrogen receptor α; ERαKO; GSK, GSK690693; LY, LY294002.
Article Snippet: The Bcrp-specific inhibitor KO143, P-glycoprotein-specific inhibitor PSC833, Multidrug resistance-associated protein 2 (Mrp2)-specific inhibitor MK571, ERα agonist propyl pyrazole triol (PPT), ERβ agonist diarylpropionitrile (DPN), GPER agonist G1,
Techniques: Inhibition, Blocking Assay, Activity Assay, Western Blot, Isolation, Fluorescence