Department of Diabetes and Metabolic Diseases, Graduate School of Medicine, University of Tokyo, Tokyo 113-0033, Japan.
Nature. 2010 Apr 29;464(7293):1313-9. doi: 10.1038/nature08991. Epub 2010 Mar 31.
Adiponectin is an anti-diabetic adipokine. Its receptors possess a seven-transmembrane topology with the amino terminus located intracellularly, which is the opposite of G-protein-coupled receptors. Here we provide evidence that adiponectin induces extracellular Ca(2+) influx by adiponectin receptor 1 (AdipoR1), which was necessary for subsequent activation of Ca(2+)/calmodulin-dependent protein kinase kinase beta (CaMKKbeta), AMPK and SIRT1, increased expression and decreased acetylation of peroxisome proliferator-activated receptor gamma coactivator-1alpha (PGC-1alpha), and increased mitochondria in myocytes. Moreover, muscle-specific disruption of AdipoR1 suppressed the adiponectin-mediated increase in intracellular Ca(2+) concentration, and decreased the activation of CaMKK, AMPK and SIRT1 by adiponectin. Suppression of AdipoR1 also resulted in decreased PGC-1alpha expression and deacetylation, decreased mitochondrial content and enzymes, decreased oxidative type I myofibres, and decreased oxidative stress-detoxifying enzymes in skeletal muscle, which were associated with insulin resistance and decreased exercise endurance. Decreased levels of adiponectin and AdipoR1 in obesity may have causal roles in mitochondrial dysfunction and insulin resistance seen in diabetes.
脂联素是一种抗糖尿病的脂肪因子。其受体具有七跨膜拓扑结构,其氨基末端位于细胞内,与 G 蛋白偶联受体相反。在这里,我们提供的证据表明,脂联素通过脂联素受体 1(AdipoR1)诱导细胞外 Ca2+内流,这对于随后 Ca2+/钙调蛋白依赖性蛋白激酶激酶 β(CaMKKβ)、AMPK 和 SIRT1 的激活、过氧化物酶体增殖物激活受体 γ 共激活因子 1α(PGC-1α)的表达增加和乙酰化减少以及肌细胞中线粒体的增加是必要的。此外,肌肉特异性敲除 AdipoR1 抑制了脂联素介导的细胞内 Ca2+浓度增加,并减少了脂联素对 CaMKK、AMPK 和 SIRT1 的激活。AdipoR1 的抑制也导致 PGC-1α表达和去乙酰化减少、线粒体含量和酶减少、氧化型 I 型肌纤维减少以及骨骼肌中氧化应激解毒酶减少,这与胰岛素抵抗和运动耐力降低有关。肥胖症中脂联素和 AdipoR1 水平降低可能与糖尿病中观察到的线粒体功能障碍和胰岛素抵抗有关。