Structural determinants for small-molecule activation of skeletal muscle AMPK α2β2γ1 by the glucose importagog SC4
The AMP-activated protein kinase (AMPK) αβγ heterotrimer regulates cellular energy
homeostasis with tissue-specific isoform distribution. Small-molecule activation of skeletal
muscle α2β2 AMPK complexes may prove a valuable treatment strategy for type 2 diabetes
and insulin resistance. Herein, we report the small-molecule SC4 is a potent, direct AMPK
activator that preferentially activates α2 complexes and stimulates skeletal muscle glucose
uptake. In parallel with the term secretagog, we propose" importagog" to define a substance …
homeostasis with tissue-specific isoform distribution. Small-molecule activation of skeletal
muscle α2β2 AMPK complexes may prove a valuable treatment strategy for type 2 diabetes
and insulin resistance. Herein, we report the small-molecule SC4 is a potent, direct AMPK
activator that preferentially activates α2 complexes and stimulates skeletal muscle glucose
uptake. In parallel with the term secretagog, we propose" importagog" to define a substance …
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