[HTML][HTML] Defining the mechanism of activation of AMP-activated protein kinase by the small molecule A-769662, a member of the thienopyridone family

MJ Sanders, ZS Ali, BD Hegarty, R Heath… - Journal of biological …, 2007 - ASBMB
AMP-activated protein kinase (AMPK) plays a key role in maintaining energy homeostasis.
Activation of AMPK in peripheral tissues has been shown to alleviate the symptoms of
metabolic diseases, such as type 2 diabetes, and consequently AMPK is a target for
treatment of these diseases. Recently, a small molecule activator (A-769662) of AMPK was
identified that had beneficial effects on metabolism in ob/ob mice. Here we show that A-
769662 activates AMPK both allosterically and by inhibiting dephosphorylation of AMPK on …