Holt Lowenna J, Lyons Ruth J, Ryan Ashleigh S, Beale Susan M, Ward Andrew, Cooney Gregory J, Daly Roger J
Cancer Research Program, Garvan Institute of Medical Research, 384 Victoria Street, Darlinghurst, Sydney, New South Wales 2010, Australia.
Mol Endocrinol. 2009 Sep;23(9):1406-14. doi: 10.1210/me.2008-0386. Epub 2009 Jun 18.
Growth factor receptor bound (Grb)10 and Grb14 are closely related adaptor proteins that bind directly to the insulin receptor (IR) and regulate insulin-induced IR tyrosine phosphorylation and signaling to IRS-1 and Akt. Grb10- and Grb14-deficient mice both exhibit improved whole-body glucose homeostasis as a consequence of enhanced insulin signaling and, in the case of the former, altered body composition. However, the combined physiological role of these adaptors has remained undefined. In this study we utilize compound gene knockout mice to demonstrate that although deficiency in one adaptor can enhance insulin-induced IRS-1 phosphorylation and Akt activation, insulin signaling is not increased further upon dual ablation of Grb10 and Grb14. Context-dependent limiting mechanisms appear to include IR hypophosphorylation and decreased IRS-1 expression. In addition, the compound knockouts exhibit an increase in lean mass comparable to Grb10-deficient mice, indicating that this reflects a regulatory function specific to Grb10. However, despite the absence of additive effects on insulin signaling and body composition, the double-knockout mice are protected from the impaired glucose tolerance that results from high-fat feeding, whereas protection is not observed with animals deficient for individual adaptors. These results indicate that, in addition to their described effects on IRS-1/Akt, Grb10 and Grb14 may regulate whole-body glucose homeostasis by additional mechanisms and highlight these adaptors as potential therapeutic targets for amelioration of the insulin resistance associated with type 2 diabetes.
生长因子受体结合蛋白(Grb)10和Grb14是密切相关的衔接蛋白,它们直接与胰岛素受体(IR)结合,并调节胰岛素诱导的IR酪氨酸磷酸化以及向胰岛素受体底物-1(IRS-1)和蛋白激酶B(Akt)的信号传导。Grb10和Grb14基因缺陷型小鼠均表现出全身葡萄糖稳态改善,这是胰岛素信号增强的结果,对于前者而言,其身体组成也发生了改变。然而,这些衔接蛋白的联合生理作用仍不明确。在本研究中,我们利用复合基因敲除小鼠证明,尽管单一衔接蛋白缺陷可增强胰岛素诱导的IRS-1磷酸化和Akt激活,但Grb10和Grb14双敲除后胰岛素信号并未进一步增强。依赖于背景的限制机制似乎包括IR磷酸化不足和IRS-1表达降低。此外,复合基因敲除小鼠的瘦体重增加,与Grb10基因缺陷型小鼠相当,这表明这反映了Grb10特有的调节功能。然而,尽管对胰岛素信号和身体组成没有累加效应,但双敲除小鼠可免受高脂喂养导致的葡萄糖耐量受损的影响,而单一衔接蛋白缺陷的动物则未观察到这种保护作用。这些结果表明,除了对IRS-1/Akt的已知作用外,Grb10和Grb14可能通过其他机制调节全身葡萄糖稳态,并突出了这些衔接蛋白作为改善2型糖尿病相关胰岛素抵抗的潜在治疗靶点。