a-769662 and Colonic-Neoplasms

a-769662 has been researched along with Colonic-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for a-769662 and Colonic-Neoplasms

Article	Year
An Underlying Mechanism of Dual Wnt Inhibition and AMPK Activation: Mitochondrial Uncouplers Masquerading as Wnt Inhibitors. Journal of medicinal chemistry, 2019, 12-26, Volume: 62, Issue:24 The importance of upregulated Wnt signaling in colorectal cancers led to efforts to develop inhibitors that target β-catenin in this pathway. We now report that several "Wnt inhibitors" that allegedly target β-catenin actually function as mitochondrial proton uncouplers that independently activate AMPK and concomitantly inhibit Wnt signaling. As expected for a process in which mitochondrial uncoupling diminishes ATP production, a mitochondrial proton uncoupler, FCCP, and a glucose metabolic inhibitor, 2-DG, activated AMPK and inhibited Wnt signaling. Also consistent with these findings, a well-known "Wnt inhibitor", FH535, functioned as a proton uncoupler, and in support of this finding, the Topics: AMP-Activated Protein Kinases; Animals; beta Catenin; Brain; Colonic Neoplasms; Energy Metabolism; Enzyme Activation; Enzyme Activators; Gene Expression Regulation, Neoplastic; Humans; Hydrocarbons, Fluorinated; Mitochondria; Oxygen Consumption; Sulfonamides; Tumor Cells, Cultured; Urea; Wnt Proteins	2019

Article

Year

An Underlying Mechanism of Dual Wnt Inhibition and AMPK Activation: Mitochondrial Uncouplers Masquerading as Wnt Inhibitors.

Journal of medicinal chemistry, 2019, 12-26, Volume: 62, Issue:24

The importance of upregulated Wnt signaling in colorectal cancers led to efforts to develop inhibitors that target β-catenin in this pathway. We now report that several "Wnt inhibitors" that allegedly target β-catenin actually function as mitochondrial proton uncouplers that independently activate AMPK and concomitantly inhibit Wnt signaling. As expected for a process in which mitochondrial uncoupling diminishes ATP production, a mitochondrial proton uncoupler, FCCP, and a glucose metabolic inhibitor, 2-DG, activated AMPK and inhibited Wnt signaling. Also consistent with these findings, a well-known "Wnt inhibitor", FH535, functioned as a proton uncoupler, and in support of this finding, the

Topics: AMP-Activated Protein Kinases; Animals; beta Catenin; Brain; Colonic Neoplasms; Energy Metabolism; Enzyme Activation; Enzyme Activators; Gene Expression Regulation, Neoplastic; Humans; Hydrocarbons, Fluorinated; Mitochondria; Oxygen Consumption; Sulfonamides; Tumor Cells, Cultured; Urea; Wnt Proteins

2019