[PDF][PDF] Chronic activation of γ2 AMPK induces obesity and reduces β cell function

A Yavari, CJ Stocker, S Ghaffari, ET Wargent… - Cell metabolism, 2016 - cell.com
A Yavari, CJ Stocker, S Ghaffari, ET Wargent, V Steeples, G Czibik, K Pinter, M Bellahcene…
Cell metabolism, 2016cell.com
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 …
Summary
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.
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