a Section for Hematology, Department of Clinical Science , University of Bergen , Norway.
b Department of Immunology and Transfusion Medicine , Haukeland University Hospital , Bergen , Norway.
Expert Opin Ther Targets. 2018 Jul;22(7):639-653. doi: 10.1080/14728222.2018.1487401. Epub 2018 Jun 22.
Constitutive signaling through the phosphatidylinositol-3-kinase-Akt-mammalian target of rapamycin (PI3K-Akt-mTOR) pathway is present in acute myeloid leukemia (AML) cells. The aim of the study was to compare constitutive PI3K-Akt-mTOR activation of primary AML cells for a large group of unselected patients.
We investigated expression and phosphorylation of 18 mediators in the PI3K-Akt-mTOR main track by flow cytometry for AML cells derived from 77 patients, and compared this with global gene expression profiles, proteomic, and transcriptomic profiles, and susceptibility to antileukemic agents.
Patients were divided into two main subsets showing generally high or low constitutive pathway activation. The high activation subset was characterized by decreased frequency of cells showing monocytic differentiation, increased frequency of adverse karyotypes, decreased constitutive cytokine release, and increased expression of certain integrins. Finally, the two groups differed in their expression of genes encoding regulators of protein phosphorylation, whereas phosphoproteomic analyses showed differences especially with regard to transcriptional regulation. Antiproliferative effects of pathway inhibition were generally stronger for the low phosphorylation subset.
The constitutive PI3K-Akt-mTOR activation differed between patients; this difference appears to be a part of complex phenotypic differences including cell communication, intracellular signaling through other pathways, and transcriptional regulation.
磷脂酰肌醇-3-激酶-蛋白激酶 B-哺乳动物雷帕霉素靶蛋白(PI3K-Akt-mTOR)通路的组成性信号在急性髓系白血病(AML)细胞中存在。本研究的目的是比较大量未选择患者的原发性 AML 细胞中组成性 PI3K-Akt-mTOR 的激活。
我们通过流式细胞术检测了 77 例患者的 AML 细胞中 PI3K-Akt-mTOR 主轨道的 18 种介质的表达和磷酸化,并将其与全局基因表达谱、蛋白质组学和转录组学谱以及抗白血病药物的敏感性进行了比较。
患者被分为两个主要亚组,其组成性通路激活程度普遍较高或较低。高激活亚组的特点是单核细胞分化的细胞频率降低,不良核型的频率增加,细胞因子的组成性释放减少,某些整合素的表达增加。最后,两组在编码蛋白磷酸化调节剂的基因表达上存在差异,而磷酸化蛋白质组学分析显示在转录调节方面存在差异。通路抑制的抗增殖作用对于低磷酸化亚组通常更强。
患者之间的组成性 PI3K-Akt-mTOR 激活存在差异;这种差异似乎是包括细胞通讯、其他途径的细胞内信号转导和转录调节在内的复杂表型差异的一部分。