Vander Haar Emilie, Lee Seong-Il, Bandhakavi Sricharan, Griffin Timothy J, Kim Do-Hyung
Department of Biochemistry, Molecular Biology and Biophysics, University of Minnesota, 6-155 Jackson Hall, 321 Church Street SE, Minneapolis, MN 55455, USA.
Nat Cell Biol. 2007 Mar;9(3):316-23. doi: 10.1038/ncb1547. Epub 2007 Feb 4.
Insulin stimulates protein synthesis and cell growth by activation of the protein kinases Akt (also known as protein kinase B, PKB) and mammalian target of rapamycin (mTOR). It was reported that Akt activates mTOR by phosphorylation and inhibition of tuberous sclerosis complex 2 (TSC2). However, in recent studies the physiological requirement of Akt phosphorylation of TSC2 for mTOR activation has been questioned. Here, we identify PRAS40 (proline-rich Akt/PKB substrate 40 kDa) as a novel mTOR binding partner that mediates Akt signals to mTOR. PRAS40 binds the mTOR kinase domain and its interaction with mTOR is induced under conditions that inhibit mTOR signalling, such as nutrient or serum deprivation or mitochondrial metabolic inhibition. Binding of PRAS40 inhibits mTOR activity and suppresses constitutive activation of mTOR in cells lacking TSC2. PRAS40 silencing inactivates insulin-receptor substrate-1 (IRS-1) and Akt, and uncouples the response of mTOR to Akt signals. Furthermore, PRAS40 phosphorylation by Akt and association with 14-3-3, a cytosolic anchor protein, are crucial for insulin to stimulate mTOR. These findings identify PRAS40 as an important regulator of insulin sensitivity of the Akt-mTOR pathway and a potential target for the treatment of cancers, insulin resistance and hamartoma syndromes.
胰岛素通过激活蛋白激酶Akt(也称为蛋白激酶B,PKB)和雷帕霉素哺乳动物靶蛋白(mTOR)来刺激蛋白质合成和细胞生长。据报道,Akt通过磷酸化和抑制结节性硬化复合物2(TSC2)来激活mTOR。然而,在最近的研究中,Akt对TSC2的磷酸化对于mTOR激活的生理需求受到了质疑。在这里,我们鉴定出富含脯氨酸的Akt/PKB底物40kDa(PRAS40)作为一种新型的mTOR结合伴侣,它介导Akt信号至mTOR。PRAS40结合mTOR激酶结构域,并且在抑制mTOR信号传导的条件下,如营养或血清剥夺或线粒体代谢抑制,其与mTOR的相互作用被诱导。PRAS40的结合抑制mTOR活性,并抑制缺乏TSC2的细胞中mTOR的组成型激活。PRAS40沉默使胰岛素受体底物1(IRS-1)和Akt失活,并使mTOR对Akt信号的反应解偶联。此外,Akt对PRAS40的磷酸化以及与胞质锚定蛋白14-3-3的结合,对于胰岛素刺激mTOR至关重要。这些发现确定PRAS40是Akt-mTOR途径胰岛素敏感性的重要调节因子,也是治疗癌症、胰岛素抵抗和错构瘤综合征的潜在靶点。