In eukaryotic cells AMP-activated protein kinase (AMPK) plays a major role in regulating cellular energy balance. AMPK responds to changes in intracellular adenine nucleotide levels, being activated by an increase in AMP/ADP relative to ATP.Mammalian AMPK exists as 12 different complexes composed of different subunit isoforms. AMPK is activated by phosphorylation of threonine 172 (T172) within the activation segment of the KD of the a subunit. In mammals, calcium/calmodulin dependent protein kinase kinase (CaMKK) b and liver kinase B1 (LKB1) have been identified as the two upstream kinases in the cascade.AMPK plays an important role in maintaining energy homeostasis in eukaryotic cells. In multicellular organisms, the role of AMPK has been adapted to play a role in integrating energy metabolism at an organismal level.There has been a significant development over the last few years in identifying small molecule direct AMPK activators, and we now understand the mechanism by which a major class of these drugs work to activate the kinase.


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