BMS309403 stimulates glucose uptake in myotubes through activation of AMP-activated protein kinase.
oleh: Wanhua Lin, Xiaoli Huang, Lina Zhang, Dongmei Chen, Dongye Wang, Qilong Peng, Lei Xu, Jingya Li, Xiujie Liu, Kuai Li, Ke Ding, Ke Ding, Shouguang Jin, Jia Li, Donghai Wu
| Format: | Article |
|---|---|
| Diterbitkan: | Public Library of Science (PLoS) 2012-01-01 |
Deskripsi
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.