Division of Hematology, Department of Medicine, Brigham and Women's Hospital, Boston, MA 02115, USA.
Blood. 2010 Feb 18;115(7):1406-15. doi: 10.1182/blood-2009-06-229443. Epub 2009 Dec 14.
Human cancers, including acute myeloid leukemia (AML), commonly display constitutive phosphoinositide 3-kinase (PI3K) AKT signaling. However, the exact role of AKT activation in leukemia and its effects on hematopoietic stem cells (HSCs) are poorly understood. Several members of the PI3K pathway, phosphatase and tensin homolog (Pten), the forkhead box, subgroup O (FOXO) transcription factors, and TSC1, have demonstrated functions in normal and leukemic stem cells but are rarely mutated in leukemia. We developed an activated allele of AKT1 that models increased signaling in normal and leukemic stem cells. In our murine bone marrow transplantation model using a myristoylated AKT1 (myr-AKT), recipients develop myeloproliferative disease, T-cell lymphoma, or AML. Analysis of the HSCs in myr-AKT mice reveals transient expansion and increased cycling, associated with impaired engraftment. myr-AKT-expressing bone marrow cells are unable to form cobblestones in long-term cocultures. Rapamycin, an inhibitor of the mammalian target of rapamycin (mTOR) rescues cobblestone formation in myr-AKT-expressing bone marrow cells and increases the survival of myr-AKT mice. This study demonstrates that enhanced AKT activation is an important mechanism of transformation in AML and that HSCs are highly sensitive to excess AKT/mTOR signaling.
人类癌症,包括急性髓系白血病(AML),通常表现出组成性磷酸肌醇 3-激酶(PI3K)AKT 信号传导。然而,AKT 激活在白血病中的确切作用及其对造血干细胞(HSCs)的影响尚不清楚。PI3K 途径的几个成员,磷酸酶和张力蛋白同源物(Pten),叉头框亚组 O(FOXO)转录因子和 TSC1,在正常和白血病干细胞中具有功能,但在白血病中很少发生突变。我们开发了 AKT1 的激活等位基因,该基因可模拟正常和白血病干细胞中信号的增加。在我们使用豆蔻酰化 AKT1(myr-AKT)的小鼠骨髓移植模型中,受者会发展为骨髓增生性疾病、T 细胞淋巴瘤或 AML。对 myr-AKT 小鼠的 HSCs 分析显示短暂扩增和增加的细胞周期,伴随着植入受损。myr-AKT 表达的骨髓细胞在长期共培养中无法形成鹅卵石。雷帕霉素,一种哺乳动物雷帕霉素靶蛋白(mTOR)抑制剂,可挽救 myr-AKT 表达的骨髓细胞中的鹅卵石形成,并增加 myr-AKT 小鼠的存活率。这项研究表明,增强的 AKT 激活是 AML 转化的重要机制,并且 HSCs 对过量的 AKT/mTOR 信号非常敏感。