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首页> 外文期刊>Molecular cancer therapeutics >Suppression of lung cancer tumor growth in a nude mouse model by the Ras inhibitor salirasib (farnesylthiosalicylic acid).
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Suppression of lung cancer tumor growth in a nude mouse model by the Ras inhibitor salirasib (farnesylthiosalicylic acid).

机译:Ras抑制剂salirasib(法尼基硫代水杨酸)在裸鼠模型中抑制肺癌肿瘤的生长。

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摘要

Aberrant Ras pathway functions contribute to the malignant phenotype of lung cancers. Inhibitors of Ras might therefore be considered as potential drugs for lung cancer therapy. Here, we show that the Ras inhibitor farnesylthiosalicylic acid (salirasib) inhibits proliferation of human lung cancer cells harboring a mutated K-ras gene (A549, H23, or HTB54) or overexpressing a growth factor receptor (H1299 or HTB58) and enhances the cytotoxic effect of the chemotherapeutic drug gemcitabine. Salirasib inhibited active K-Ras in A549 cells, reversed their transformed morphology, and inhibited their anchorage-independent growth in vitro. Tumor growth in A549 and HTB58 cell nude mouse models was inhibited by i.p. administration of salirasib. P.o. formulated salirasib also inhibited A549 cell tumor growth. Our results suggest that p.o. salirasib may be considered as a potential treatment for lung cancer therapy.
机译:异常的Ras通路功能有助于肺癌的恶性表型。因此,可以将Ras抑制剂视为肺癌治疗的潜在药物。在这里,我们显示Ras抑制剂法呢基硫代水杨酸(salirasib)抑制具有突变K-ras基因(A549,H23或HTB54)或过表达生长因子受体(H1299或HTB58)的人肺癌细胞的增殖,并增强细胞毒性化疗药物吉西他滨的疗效。 Salirasib抑制了A549细胞中的活性K-Ras,逆转了其转化的形态,并抑制了其不依赖锚定的体外生长。 i.p.抑制了A549和HTB58细胞裸鼠模型中的肿瘤生长。 Salirasib的管理。邮局配制的salirasib还可以抑制A549细胞肿瘤的生长。我们的结果表明p.o. salirasib可能被认为是肺癌治疗的潜在疗法。

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