[HTML][HTML] Mechanism of action of A-769662, a valuable tool for activation of AMP-activated protein kinase
O Göransson, A McBride, SA Hawley, FA Ross… - Journal of Biological …, 2007 - ASBMB
We have studied the mechanism of A-769662, a new activator of AMP-activated protein
kinase (AMPK). Unlike other pharmacological activators, it directly activates native rat AMPK
by mimicking both effects of AMP, ie allosteric activation and inhibition of dephosphorylation.
We found that it has no effect on the isolated α subunit kinase domain, with or without the
associated autoinhibitory domain, or on interaction of glycogen with the β subunit glycogen-
binding domain. Although it mimics actions of AMP, it has no effect on binding of AMP to the …
kinase (AMPK). Unlike other pharmacological activators, it directly activates native rat AMPK
by mimicking both effects of AMP, ie allosteric activation and inhibition of dephosphorylation.
We found that it has no effect on the isolated α subunit kinase domain, with or without the
associated autoinhibitory domain, or on interaction of glycogen with the β subunit glycogen-
binding domain. Although it mimics actions of AMP, it has no effect on binding of AMP to the …