Chronic Activation of γ2 AMPK Induces Obesity and Reduces β Cell Function

Cell Metab. 2016 May 10;23(5):821-36. doi: 10.1016/j.cmet.2016.04.003. Epub 2016 Apr 28.

Abstract

Despite significant advances in our understanding of the biology determining systemic energy homeostasis, the treatment of obesity remains a medical challenge. Activation of AMP-activated protein kinase (AMPK) has been proposed as an attractive strategy for the treatment of obesity and its complications. AMPK is a conserved, ubiquitously expressed, heterotrimeric serine/threonine kinase whose short-term activation has multiple beneficial metabolic effects. Whether these translate into long-term benefits for obesity and its complications is unknown. Here, we observe that mice with chronic AMPK activation, resulting from mutation of the AMPK γ2 subunit, exhibit ghrelin signaling-dependent hyperphagia, obesity, and impaired pancreatic islet insulin secretion. Humans bearing the homologous mutation manifest a congruent phenotype. Our studies highlight that long-term AMPK activation throughout all tissues can have adverse metabolic consequences, with implications for pharmacological strategies seeking to chronically activate AMPK systemically to treat metabolic disease.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • AMP-Activated Protein Kinases / metabolism*
  • Adiposity / genetics
  • Adult
  • Aging / pathology
  • Agouti-Related Protein / metabolism
  • Animals
  • Arcuate Nucleus of Hypothalamus / metabolism
  • Energy Metabolism / genetics
  • Enzyme Activation
  • Feeding Behavior
  • Female
  • Heterozygote
  • Humans
  • Hyperphagia / complications
  • Hyperphagia / enzymology
  • Hyperphagia / genetics
  • Hyperphagia / pathology
  • Hypothalamus / metabolism
  • Insulin / metabolism
  • Insulin-Secreting Cells / enzymology*
  • Insulin-Secreting Cells / pathology*
  • Male
  • Mice
  • Mitochondria / metabolism
  • Mutation / genetics
  • Neurons / metabolism
  • Obesity / blood
  • Obesity / complications
  • Obesity / enzymology*
  • Obesity / pathology
  • Oxidative Phosphorylation
  • Receptors, Ghrelin / metabolism
  • Ribosomes / metabolism
  • Signal Transduction / genetics
  • Transcriptome / genetics
  • Up-Regulation / genetics

Substances

  • Agouti-Related Protein
  • Insulin
  • Receptors, Ghrelin
  • AMP-Activated Protein Kinases