BMS309403 stimulates glucose uptake in myotubes through activation of AMP-activated protein kinase.
basic_science · Level V
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- Record sourced from PubMed, PMID 22952994.
- Also identified by DOI 10.1371/journal.pone.0044570 and PMC identifier PMC2797930.
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Abstract
BMS309403 is a biphenyl azole inhibitor against fatty acid binding protein 4 (FABP4) and regarded as a lead compound for effective treatment of obesity related cardio-metabolic diseases. Here we discovered an off-target activity of BMS309403 in that it stimulates glucose uptake in C2C12 myotubes in a temporal and dose dependent manner via activation of AMP-activated protein kinase (AMPK) signaling pathway but independent of FABPs. Further analysis indicated that BMS309403 activates AMPK through increasing the ratio of intracellular AMP:ATP while decreasing mitochondrial membrane potential. These findings provide mechanistic insights on the action of BMS309403.