AMP-activated protein kinase

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Contents 1 Function 2 Relevance 3 Structural highlights 4 3D structures of AMP-activated protein kinase

Function

AMP-activated protein kinase (AMPK) is a nuclear receptor which regulates cellular uptake of glucose, β-oxidation of fatty acids and biogenesis of glucose transporter thus playing a role in cellular energy homeostasis by phosphorylating key proteins. In response to low levels of ATP, AMPK activates energy-producing pathways and inhibits energy-consuming pathways.

Relevance

AMPK is an important drug target for obesity, type 2 diabetes and cancer. AMPK activity is enhanced during exercise resulting in muscle increased glucose uptake and blood supply.

Structural highlights

AMPK is a heterotrimer:
AMPK α subunit is the catalytic subunit and contains Thr174 (TPO) or Ser108 (SEP) which undergoes phosphorylation.
AMPK β subunit is a scaffold on which the heterotrimer assembles.
AMPK γ subunit detects shifts in AMP:ATP ratio via its 4 cystathionine β synthase (CBS) domains. The active site binds AMP.

3D structures of AMP-activated protein kinase

Updated on 01-November-2015