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p53的稳定和激活通过AMPK下调套细胞淋巴瘤中的mTOR信号传导。

Stabilization and activation of p53 downregulates mTOR signaling through AMPK in mantle cell lymphoma.

作者信息

Drakos E, Atsaves V, Li J, Leventaki V, Andreeff M, Medeiros L J, Rassidakis G Z

机构信息

Department of Hematopathology, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA.

出版信息

Leukemia. 2009 Apr;23(4):784-90. doi: 10.1038/leu.2008.348. Epub 2009 Feb 19.

Abstract

Mantle cell lymphoma (MCL) is a clinically aggressive B-cell non-Hodgkin lymphoma characterized by the t(11;14)(q13;q32) and overexpression of cyclin D1. A high proportion of MCL tumors harbor wild-type (wt) and potentially functional p53 gene. We show here that stabilization and activation of wt-p53 using a recently developed potent MDM2 inhibitor, nutlin 3A, results in significant p53-dependent G1-S cell cycle arrest and apoptosis in MCL cells through regulation of p53 target genes. As mTOR signaling is activated in MCL and may control cyclin D1 levels, we show that p53 activation may downregulate the AKT/mTOR pathway through a mechanism involving AMP kinase (AMPK). Despite the non-genotoxic mode of nutlin 3A treatment, we show evidence that stabilization of p53 is associated with its phosphorylation at serine 15 residue and activation of AMPK. Stimulation of AMPK kinase activity using AICAR inhibits phosphorylation of critical downstream effectors of mTOR signaling, such as 4E-BP1 and rpS6. Pharmacologic inhibition of AMPK using compound C in nutlin-3A-treated MCL cells harboring wt-p53 did not affect the level of (ser15)p-p53, suggesting that the (ser15)p-p53 --> AMPK is the direction involved in the p53/AMPK/mTOR cross talk. These data establish a p53 --> AMPK --> mTOR mechanism in MCL and uncover a novel biologic effect of potent MDM2 inhibitors in preclinical models of MCL.

摘要

套细胞淋巴瘤(MCL)是一种临床上具有侵袭性的B细胞非霍奇金淋巴瘤,其特征为t(11;14)(q13;q32)以及细胞周期蛋白D1的过表达。高比例的MCL肿瘤携带野生型(wt)且可能具有功能的p53基因。我们在此表明,使用最近开发的强效MDM2抑制剂nutlin 3A使wt-p53稳定并激活,通过调节p53靶基因,导致MCL细胞中出现显著的p53依赖性G1-S期细胞周期停滞和凋亡。由于mTOR信号在MCL中被激活且可能控制细胞周期蛋白D1水平,我们表明p53激活可能通过涉及AMP激酶(AMPK)的机制下调AKT/mTOR途径。尽管nutlin 3A治疗是非基因毒性模式,但我们有证据表明p53的稳定与其丝氨酸15残基的磷酸化以及AMPK的激活有关。使用AICAR刺激AMPK激酶活性可抑制mTOR信号关键下游效应物(如4E-BP1和rpS6)的磷酸化。在携带wt-p53的nutlin-3A处理的MCL细胞中使用化合物C对AMPK进行药理学抑制并不影响(ser15)p-p53的水平,这表明(ser15)p-p53 --> AMPK是参与p53/AMPK/mTOR相互作用的方向。这些数据在MCL中建立了p53 --> AMPK --> mTOR机制,并在MCL的临床前模型中揭示了强效MDM2抑制剂的一种新的生物学效应。

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