Chen Yi-Chun, Lutkewitte Andrew J, Basavarajappa Halesha D, Fueger Patrick T
Department of Pediatrics and Herman B. Wells Center for Pediatric Research, Indiana University School of Medicine, Indianapolis, IN 46202, USA.
Department of Cellular & Integrative Physiology, Indiana University School of Medicine, Indianapolis, IN 46202, USA.
Metabolites. 2023 May 4;13(5):627. doi: 10.3390/metabo13050627.
A loss of functional beta cell mass is a final etiological event in the development of frank type 2 diabetes (T2D). To preserve or expand beta cells and therefore treat/prevent T2D, growth factors have been considered therapeutically but have largely failed to achieve robust clinical success. The molecular mechanisms preventing the activation of mitogenic signaling pathways from maintaining functional beta cell mass during the development of T2D remain unknown. We speculated that endogenous negative effectors of mitogenic signaling cascades impede beta cell survival/expansion. Thus, we tested the hypothesis that a stress-inducible epidermal growth factor receptor (EGFR) inhibitor, mitogen-inducible gene 6 (Mig6), regulates beta cell fate in a T2D milieu. To this end, we determined that: (1) glucolipotoxicity (GLT) induces Mig6, thereby blunting EGFR signaling cascades, and (2) Mig6 mediates molecular events regulating beta cell survival/death. We discovered that GLT impairs EGFR activation, and Mig6 is elevated in human islets from T2D donors as well as GLT-treated rodent islets and 832/13 INS-1 beta cells. Mig6 is essential for GLT-induced EGFR desensitization, as Mig6 suppression rescued the GLT-impaired EGFR and ERK1/2 activation. Further, Mig6 mediated EGFR but not insulin-like growth factor-1 receptor nor hepatocyte growth factor receptor activity in beta cells. Finally, we identified that elevated Mig6 augmented beta cell apoptosis, as Mig6 suppression reduced apoptosis during GLT. In conclusion, we established that T2D and GLT induce Mig6 in beta cells; the elevated Mig6 desensitizes EGFR signaling and induces beta cell death, suggesting Mig6 could be a novel therapeutic target for T2D.
功能性β细胞数量的减少是显性2型糖尿病(T2D)发生发展中的最终病因学事件。为了保存或增加β细胞数量从而治疗/预防T2D,生长因子已被视为一种治疗手段,但在很大程度上未能取得显著的临床成功。在T2D发生发展过程中,阻止有丝分裂信号通路激活以维持功能性β细胞数量的分子机制仍不清楚。我们推测有丝分裂信号级联反应的内源性负效应器会阻碍β细胞的存活/增殖。因此,我们检验了这样一个假设:一种应激诱导的表皮生长因子受体(EGFR)抑制剂,即有丝分裂原诱导基因6(Mig6),在T2D环境中调节β细胞命运。为此,我们确定:(1)糖脂毒性(GLT)诱导Mig6,从而减弱EGFR信号级联反应;(2)Mig6介导调节β细胞存活/死亡的分子事件。我们发现GLT损害EGFR激活,在T2D供体的人胰岛以及经GLT处理的啮齿动物胰岛和832/13 INS-1β细胞中,Mig6水平升高。Mig6对于GLT诱导的EGFR脱敏至关重要,因为抑制Mig6可挽救GLT损害的EGFR和ERK1/2激活。此外,Mig6介导β细胞中的EGFR活性,但不介导胰岛素样生长因子-1受体或肝细胞生长因子受体的活性。最后,我们确定Mig6水平升高会增加β细胞凋亡,因为抑制Mig6可减少GLT期间的细胞凋亡。总之,我们证实T2D和GLT在β细胞中诱导Mig6;升高的Mig6使EGFR信号脱敏并诱导β细胞死亡,这表明Mig6可能是T2D的一个新的治疗靶点。