Flex Elisabetta, Petrangeli Valentina, Stella Lorenzo, Chiaretti Sabina, Hornakova Tekla, Knoops Laurent, Ariola Cristina, Fodale Valentina, Clappier Emmanuelle, Paoloni Francesca, Martinelli Simone, Fragale Alessandra, Sanchez Massimo, Tavolaro Simona, Messina Monica, Cazzaniga Giovanni, Camera Andrea, Pizzolo Giovanni, Tornesello Assunta, Vignetti Marco, Battistini Angela, Cavé Hélène, Gelb Bruce D, Renauld Jean-Christophe, Biondi Andrea, Constantinescu Stefan N, Foà Robin, Tartaglia Marco
Dipartimento di Biologia Cellulare e Neuroscienze, Istituto Superiore di Sanità, Rome, 00161, Italy.
J Exp Med. 2008 Apr 14;205(4):751-8. doi: 10.1084/jem.20072182. Epub 2008 Mar 24.
Aberrant signal transduction contributes substantially to leukemogenesis. The Janus kinase 1 (JAK1) gene encodes a cytoplasmic tyrosine kinase that noncovalently associates with a variety of cytokine receptors and plays a nonredundant role in lymphoid cell precursor proliferation, survival, and differentiation. We report that somatic mutations in JAK1 occur in individuals with acute lymphoblastic leukemia (ALL). JAK1 mutations were more prevalent among adult subjects with the T cell precursor ALL, where they accounted for 18% of cases, and were associated with advanced age at diagnosis, poor response to therapy, and overall prognosis. All mutations were missense, and some were predicted to destabilize interdomain interactions controlling the activity of the kinase. Three mutations that were studied promoted JAK1 gain of function and conferred interleukin (IL)-3-independent growth in Ba/F3 cells and/or IL-9-independent resistance to dexamethasone-induced apoptosis in T cell lymphoma BW5147 cells. Such effects were associated with variably enhanced activation of multiple downstream signaling pathways. Leukemic cells with mutated JAK1 alleles shared a gene expression signature characterized by transcriptional up-regulation of genes positively controlled by JAK signaling. Our findings implicate dysregulated JAK1 function in ALL, particularly of T cell origin, and point to this kinase as a target for the development of novel antileukemic drugs.
异常的信号转导在白血病发生过程中起重要作用。Janus激酶1(JAK1)基因编码一种细胞质酪氨酸激酶,它与多种细胞因子受体非共价结合,并在淋巴样细胞前体的增殖、存活和分化中发挥不可替代的作用。我们报告称,JAK1的体细胞突变发生在急性淋巴细胞白血病(ALL)患者中。JAK1突变在成人T细胞前体ALL患者中更为普遍,占病例的18%,且与诊断时年龄较大、对治疗反应不佳及总体预后相关。所有突变均为错义突变,其中一些预计会破坏控制激酶活性的结构域间相互作用的稳定性。研究的三个突变促进了JAK1的功能获得,并赋予Ba/F3细胞白细胞介素(IL)-3非依赖性生长和/或T细胞淋巴瘤BW5147细胞对IL-9非依赖性地抵抗地塞米松诱导的凋亡。这些效应与多个下游信号通路的不同程度增强的激活有关。携带JAK1等位基因突变的白血病细胞具有一种基因表达特征,其特点是受JAK信号正向调控的基因转录上调。我们的研究结果表明JAK1功能失调在ALL中起作用,尤其是T细胞起源的ALL,并指出该激酶是开发新型抗白血病药物的靶点。