Department of Pharmacology, Zhongshan School of Medicine, Sun Yat-sen University, Guangzhou, PR China.
Mol Pharmacol. 2012 Mar;81(3):292-8. doi: 10.1124/mol.111.076166. Epub 2011 Dec 15.
Glioma is the most common malignant cancer affecting the central nerve system, with dismal prognosis. Differentiation-inducing therapy is a novel strategy that has been preliminarily proved effective against malignant glioma. We have reported previously that activation of cAMP/protein kinase A (PKA) pathway is capable of inducing glioma cell differentiation, characterized by astrocyte-like shape and dramatic induction of astrocyte biomarker glial fibrillary acidic protein (GFAP). However, little progress has been made on molecular mechanisms related. Here we demonstrate that microRNA 335 (miR-335) is responsible for the glioma cell differentiation stimulated by activation of cAMP/PKA pathway. In the cAMP elevator cholera toxin-induced differentiation model of rat C6 glioma cells, miR-335 was significantly up-regulated, which was mimicked by other typical cAMP/PKA pathway activators (e.g., forskolin, dibutyryl-cAMP) and abolished by PKA-specific inhibitor (9R,10S,12S)-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i] [1,6]benzodiazocine-10-carboxylic acid, hexyl ester (KT5720). In an assay measuring gain and loss of miR-335 function, exogenetic miR-335 resulted in induction of GFAP, whereas miR-335 specific inhibitor antagomir-335 violently blocked cholera toxin-induced GFAP up-regulation. It is noteworthy that in human U87-MG glioma cells and human primary culture glioma cells, miR-335 also mediated cholera toxin-induced differentiation. Taken together, our findings suggest that miR-335 is potently required for differentiation of malignant glioma cells induced by cAMP/PKA pathway activation, and a single microRNA may act as an important fate determinant to control the differentiation status of malignant gliomas, which has provided a new insight into differentiation-inducing therapy against malignant gliomas.
神经胶质瘤是最常见的影响中枢神经系统的恶性肿瘤,预后不良。诱导分化治疗是一种针对恶性神经胶质瘤的新策略,已初步证明其有效。我们之前曾报道过,激活 cAMP/蛋白激酶 A(PKA)通路能够诱导神经胶质瘤细胞分化,表现为星形胶质细胞样形态和神经胶质纤维酸性蛋白(GFAP)的显著诱导。然而,与相关分子机制相关的研究进展甚微。在这里,我们证明微 RNA 335(miR-335)是 cAMP/PKA 通路激活刺激神经胶质瘤细胞分化的原因。在大鼠 C6 神经胶质瘤细胞的 cAMP 升高剂霍乱毒素诱导分化模型中,miR-335 显著上调,这可被其他典型的 cAMP/PKA 通路激活剂(如霍乱毒素、二丁酰环磷腺苷)模拟,并可被 PKA 特异性抑制剂(9R,10S,12S)-2,3,9,10,11,12-六氢-10-羟基-9-甲基-1-氧代-9,12-环氧-1H-二吲哚[1,2,3-fg:3',2',1'-kl]吡咯[3,4-i][1,6]苯并二氮杂环庚烷-10-羧酸,己酯(KT5720)消除。在测量 miR-335 功能增益和丧失的实验中,外源性 miR-335 导致 GFAP 的诱导,而 miR-335 特异性抑制剂 antagomir-335 则强烈阻断霍乱毒素诱导的 GFAP 上调。值得注意的是,在人 U87-MG 神经胶质瘤细胞和人原代培养神经胶质瘤细胞中,miR-335 也介导了霍乱毒素诱导的分化。总之,我们的研究结果表明,miR-335 是 cAMP/PKA 通路激活诱导恶性神经胶质瘤细胞分化所必需的,单个 microRNA 可能作为一个重要的命运决定因素来控制恶性神经胶质瘤的分化状态,这为恶性神经胶质瘤的诱导分化治疗提供了新的思路。