Target intelligence / Profile preview

AMP-dependent protein kinase catalytic subunit alpha 1 (AMPK α₁)

Target
AMPK α₁
Molecular classification
Enzyme, Protein Kinase, Serine/threonine kinase
01

Overview

AMP-dependent protein kinase catalytic subunit alpha 1 (AMPK α₁) is the catalytic component of the heterotrimeric enzyme complex known as AMP-activated protein kinase (AMPK). This enzyme plays a central role in cellular energy homeostasis by sensing and responding to changes in intracellular energy status. AMPK senses cellular energy status through competitive binding of adenine nucleotides—AMP, ADP, and ATP—to specific sites on its γ regulatory subunit. When cellular ATP levels drop and AMP/ADP levels rise, this promotes allosteric activation and enhances phosphorylation at Thr172 by upstream kinases, stabilizing an active conformation that enables substrate binding and catalysis. The primary function of AMPK is to restore energy balance by upregulating catabolic pathways that generate ATP (e.g., glucose uptake, fatty acid oxidation) and downregulating anabolic processes that consume ATP. Dysregulation has been implicated in diseases such as type 2 diabetes, metabolic syndrome, cardiovascular disease, neurodegeneration, and cancer. Due to its central role in metabolism regulation, AMPK is considered a promising drug target for metabolic disorders.

Other names
PRKAA1AMPK alpha 1protein kinase AMP-activated catalytic subunit alpha 1
02

Mechanism of action

Activation of AMPK via distinct mechanisms from physiological nucleotide-mediated activation

03

Biological functions

Regulation of energy homeostasisRegulation of glucose uptakeRegulation of fatty acid oxidationAutophagy regulationCell growth control
04

Disease associations

Type 2 diabetesMetabolic syndromeCardiovascular diseaseNeurodegenerative diseaseAlzheimer's diseaseCancer
05

Safety considerations

Potential off-target effects due to broad metabolic roles
06

Interacting drugs

A769662

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