Roche pRED (Pharmaceutical Research and Early Development), Roche Innovation Center Basel, F.Hoffmann-La Roche Ltd., CH-4070 Basel, Switzerland.
Department of Medicine, Division of Cardiology, Beth Israel Deaconess Medical Center (BIDMC), Harvard Medical School, Boston, MA 02215, USA.
Int J Mol Sci. 2019 Dec 9;20(24):6201. doi: 10.3390/ijms20246201.
The kinase AKT2 (PKB) is an important mediator of insulin signaling, for which loss-of-function knockout (KO) mutants lead to early onset diabetes mellitus, and dominant active mutations lead to early development of obesity and endothelial cell (EC) dysfunction. To model EC dysfunction, we used edited human pluripotent stem cells (hPSCs) that carried either a homozygous deletion of AKT2 (AKT2 KO) or a dominant active mutation (AKT2 E17K), which, along with the parental wild type (WT), were differentiated into ECs. Profiling of EC lines indicated an increase in proinflammatory and a reduction in anti-inflammatory fatty acids, an increase in inflammatory chemokines in cell supernatants, increased expression of proinflammatory genes, and increased binding to the EC monolayer in a functional leukocyte adhesion assay for both AKT2 KO and AKT2 E17K. Collectively, these findings suggest that vascular endothelial inflammation that results from dysregulated insulin signaling (homeostasis) may contribute to coronary artery disease, and that either downregulation or upregulation of the insulin pathway may lead to inflammation of endothelial cells. This suggests that the standard of care for patients must be expanded from control of metabolic parameters to include control of inflammation, such that endothelial dysfunction and cardiovascular disorders can ultimately be prevented.
蛋白激酶 AKT2(PKB)是胰岛素信号的重要介质,其功能丧失的敲除(KO)突变会导致早发性糖尿病,而显性激活突变会导致肥胖和内皮细胞(EC)功能障碍的早期发展。为了模拟 EC 功能障碍,我们使用了经过编辑的人多能干细胞(hPSC),这些细胞要么携带 AKT2 的纯合缺失(AKT2 KO),要么携带显性激活突变(AKT2 E17K),以及亲本野生型(WT),这些细胞被分化为 EC。对 EC 系的分析表明,促炎脂肪酸增加,抗炎脂肪酸减少,细胞上清液中的炎症趋化因子增加,促炎基因表达增加,在用于功能性白细胞黏附测定的 EC 单层上的结合增加,这两种情况在 AKT2 KO 和 AKT2 E17K 中均存在。总之,这些发现表明,由于胰岛素信号失调(稳态)导致的血管内皮炎症可能导致冠状动脉疾病,而胰岛素通路的下调或上调可能导致内皮细胞炎症。这表明,患者的标准治疗必须从控制代谢参数扩展到控制炎症,从而最终可以预防内皮功能障碍和心血管疾病。