AMP-activated protein kinase (AMPK) (AMPK)

AMP-activated protein kinase (AMPK) is a heterotrimeric enzyme complex that serves as the central energy sensor and "cellular master regulator" of metabolism and homeostasis. It is activated in response to a high AMP:ATP ratio, signaling a low-energy state, and acts to restore energy balance by promoting catabolic pathways (such as fatty acid oxidation and glucose uptake) while inhibiting anabolic processes (such as protein and lipid synthesis). Beyond its metabolic roles, AMPK is a critical regulator of autophagy, mitochondrial biogenesis, and cell growth, primarily through the inhibition of the mTORC1 pathway and the activation of ULK1. Due to its broad influence on cellular health, AMPK is a major therapeutic target for metabolic disorders like type 2 diabetes and obesity, as well as cardiovascular diseases, neurodegeneration, and cancer. Recent drug development efforts, such as those by Saillant Therapeutics, also explore its potential in treating viral infections and promoting tissue rejuvenation.

Other names

Cellular master regulator5'-AMP-activated protein kinaseAdenosine monophosphate-activated protein kinaseEnergy sensorMetabolic master regulator

AMPK activation via allosteric binding of AMP/ADP to the gamma subunit and phosphorylation of the alpha subunit (Thr172) by upstream kinases like LKB1 or CaMKK2, leading to the phosphorylation of downstream targets such as Acetyl-CoA Carboxylase (ACC) and the inhibition of the mTORC1 complex.