Obesity-linked phosphorylation of SIRT1 by casein kinase 2 inhibits its nuclear localization and promotes fatty liver

SE Choi, S Kwon, S Seok, Z Xiao, KW Lee… - … and cellular biology, 2017 - Taylor & Francis
SE Choi, S Kwon, S Seok, Z Xiao, KW Lee, Y Kang, X Li, K Shinoda, S Kajimura, B Kemper…
Molecular and cellular biology, 2017Taylor & Francis
ABSTRACT Sirtuin1 (SIRT1) deacetylase delays and improves many obesity-related
diseases, including nonalcoholic fatty liver disease (NAFLD) and diabetes, and has received
great attention as a drug target. SIRT1 function is aberrantly low in obesity, so understanding
the underlying mechanisms is important for drug development. Here, we show that obesity-
linked phosphorylation of SIRT1 inhibits its function and promotes pathological symptoms of
NAFLD. In proteomic analysis, Ser-164 was identified as a major serine phosphorylation site …
Abstract
Sirtuin1 (SIRT1) deacetylase delays and improves many obesity-related diseases, including nonalcoholic fatty liver disease (NAFLD) and diabetes, and has received great attention as a drug target. SIRT1 function is aberrantly low in obesity, so understanding the underlying mechanisms is important for drug development. Here, we show that obesity-linked phosphorylation of SIRT1 inhibits its function and promotes pathological symptoms of NAFLD. In proteomic analysis, Ser-164 was identified as a major serine phosphorylation site in SIRT1 in obese, but not lean, mice, and this phosphorylation was catalyzed by casein kinase 2 (CK2), the levels of which were dramatically elevated in obesity. Mechanistically, phosphorylation of SIRT1 at Ser-164 substantially inhibited its nuclear localization and modestly affected its deacetylase activity. Adenovirus-mediated liver-specific expression of SIRT1 or a phosphor-defective S164A-SIRT1 mutant promoted fatty acid oxidation and ameliorated liver steatosis and glucose intolerance in diet-induced obese mice, but these beneficial effects were not observed in mice expressing a phosphor-mimic S164D-SIRT1 mutant. Remarkably, phosphorylated S164-SIRT1 and CK2 levels were also highly elevated in liver samples of NAFLD patients and correlated with disease severity. Thus, inhibition of phosphorylation of SIRT1 by CK2 may serve as a new therapeutic approach for treatment of NAFLD and other obesity-related diseases.
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