Target intelligence / Profile preview

AMP-activated protein kinase alpha catalytic subunit (AMPK alpha)

Target
AMPK alpha
Molecular classification
Enzyme, Kinase (Serine/threonine protein kinase)
01

Overview

AMP-activated protein kinase (AMPK) alpha catalytic subunit is the core enzyme responsible for the kinase activity of the AMPK heterotrimeric complex, which includes regulatory beta and gamma subunits. The alpha subunit contains the active catalytic domain necessary for phosphorylating downstream targets. AMPK acts as a master cellular energy sensor, being activated under conditions of low cellular energy (high AMP/ATP ratio), and switches cells from energy-consuming to energy-generating processes by direct phosphorylation of metabolic enzymes and transcription factors. Two isoforms of the alpha subunit are encoded by the genes PRKAA1 (alpha-1) and PRKAA2 (alpha-2), each with distinct and overlapping tissue distributions. AMPK is a key mediator of the effects of drugs like metformin (widely used in diabetes) and plays a role in multiple pathophysiological processes including metabolic disease, cancer, and cardiovascular disorders[2][4][6][8].

Other names
5'-AMP-activated protein kinase catalytic subunit alpha-1AMPK alpha-1AMPK alpha-2PRKAA1 (alpha-1 gene)PRKAA2 (alpha-2 gene)Sometimes loosely called \"AMPK\"
02

Mechanism of action

Activation of AMPK increases cellular glucose uptake and fatty acid oxidation, and reduces lipid, protein and carbohydrate synthesis. Drugs (e.g., metformin) stimulate AMPK activation, often through increasing AMP/ATP ratio.

03

Biological functions

Cellular energy sensing and metabolic regulationPhosphorylation of metabolic enzymesRegulation of cell growth and proliferationInhibition of anabolic (energy-consuming) pathwaysActivation of catabolic (energy-generating) pathways
04

Disease associations

CancerCardiovascular diseaseMetabolic syndrome/obesityType 2 diabetes mellitusNeurodegenerative disease
05

Safety considerations

Hypoglycemia with potent activatorsInterference with normal anabolic processes (e.g., excessive inhibition of cell growth)Potential effects on cardiac muscle and other tissues with high energy demands
06

Interacting drugs

Metformin

3 more in the full profile.

07

Biomarkers

Phosphorylation status of AMPK (e.g., phospho-Thr172)Expression of AMPK alpha subunits (PRKAA1, PRKAA2)

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