Target intelligence / Profile preview

AMP-activated protein kinase alpha catalytic subunit isoform alpha-1 (AMPKA1)

Target
AMPKA1
Molecular classification
Enzyme, Serine/threonine protein kinases
01

Overview

AMPKA1 is the catalytic subunit of the heterotrimeric AMP-activated protein kinase (AMPK) complex, a central regulator of cellular energy homeostasis. It is activated by increased AMP/ATP ratio or calcium-mediated signaling and phosphorylates numerous substrates to regulate metabolism. Dysregulation or mutation in AMPKA1/PRKAA1 has been implicated in several diseases.

Other names
PRKAA1
02

Mechanism of action

Activation via phosphorylation at threonine 172 (Thr172). Direct activation by small molecules.

03

Biological functions

Energy homeostasis regulationRegulation of metabolismRegulation of autophagyRegulation of cell growth/proliferationRegulation of cell polarityTranscriptional regulationChromatin structure modificationProtection against metabolic stress
04

Disease associations

Diabetes/metabolic syndromeCardiovascular diseasesNeurodegenerative disordersVarious cancers
05

Safety considerations

Overlapping functions of AMPKα isoforms make it difficult to discriminate disease involvement.Potential for off-target effects due to broad substrate specificity.
06

Interacting drugs

A769662

1 more in the full profile.

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