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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, <t>GSK690693;</t> LY, LY294002.
Akt Inhibitor Gsk690693, supplied by Tocris, used in various techniques. Bioz Stars score: 93/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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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, <t>GSK690693;</t> LY, LY294002.
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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, <t>GSK690693;</t> LY, LY294002.
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Tocris gsk 690693 4144 standard
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, <t>GSK690693;</t> LY, LY294002.
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Lipomed fabrikmattenweg 4 ch 4144
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, <t>GSK690693;</t> LY, LY294002.
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NCIMB Ltd isom 4144
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, <t>GSK690693;</t> LY, LY294002.
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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.

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, Akt inhibitor GSK690693, PI3K inhibitor LY294002, and AMPK inhibitor dorsomorphin dihydrochloride were all purchased from Tocris Bioscience.

Techniques: Inhibition, Blocking Assay, Activity Assay, Western Blot, Isolation, Fluorescence