Athreya Arjun P, Kalari Krishna R, Cairns Junmei, Gaglio Alan J, Wills Quin F, Niu Nifang, Weinshilboum Richard, Iyer Ravishankar K, Wang Liewei
Department of Electrical and Computer Engineering, University of Illinois at Urbana-Champaign, Champaign, IL, USA.
Department of Health Sciences Research, Mayo Clinic, Rochester, MN, USA.
Oncotarget. 2017 Apr 18;8(16):27199-27215. doi: 10.18632/oncotarget.16109.
We demonstrate that model-based unsupervised learning can uniquely discriminate single-cell subpopulations by their gene expression distributions, which in turn allow us to identify specific genes for focused functional studies. This method was applied to MDA-MB-231 breast cancer cells treated with the antidiabetic drug metformin, which is being repurposed for treatment of triple-negative breast cancer. Unsupervised learning identified a cluster of metformin-treated cells characterized by a significant suppression of 230 genes (p-value < 2E-16). This analysis corroborates known studies of metformin action: a) pathway analysis indicated known mechanisms related to metformin action, including the citric acid (TCA) cycle, oxidative phosphorylation, and mitochondrial dysfunction (p-value < 1E-9); b) 70% of these 230 genes were functionally implicated in metformin response; c) among remaining lesser functionally-studied genes for metformin-response was CDC42, down-regulated in breast cancer treated with metformin. However, CDC42's mechanisms in metformin response remained unclear. Our functional studies showed that CDC42 was involved in metformin-induced inhibition of cell proliferation and cell migration mediated through an AMPK-independent mechanism. Our results points to 230 genes that might serve as metformin response signatures, which needs to be tested in patients treated with metformin and, further investigation of CDC42 and AMPK-independence's role in metformin's anticancer mechanisms.
我们证明,基于模型的无监督学习能够通过单细胞亚群的基因表达分布对其进行独特区分,这反过来又使我们能够识别出用于重点功能研究的特定基因。该方法应用于用抗糖尿病药物二甲双胍处理的MDA-MB-231乳腺癌细胞,二甲双胍正被重新用于治疗三阴性乳腺癌。无监督学习识别出一组经二甲双胍处理的细胞,其特征是230个基因受到显著抑制(p值<2E-16)。该分析证实了关于二甲双胍作用的已知研究:a)通路分析表明了与二甲双胍作用相关的已知机制,包括柠檬酸(TCA)循环、氧化磷酸化和线粒体功能障碍(p值<1E-9);b)这230个基因中有70%在功能上与二甲双胍反应有关;c)在其余功能研究较少的二甲双胍反应相关基因中,有CDC42,在用二甲双胍治疗的乳腺癌中其表达下调。然而,CDC42在二甲双胍反应中的机制仍不清楚。我们的功能研究表明,CDC42参与了二甲双胍诱导的细胞增殖抑制和通过非AMPK依赖机制介导的细胞迁移抑制。我们的结果指出了230个可能作为二甲双胍反应特征的基因,这需要在接受二甲双胍治疗的患者中进行测试,并进一步研究CDC42和AMPK非依赖性在二甲双胍抗癌机制中的作用。