Systems Biology Ireland, and UCD Charles Institute of Dermatology, School of Medicine, University College Dublin, Belfield, Ireland.
UCL Institute of Ophthalmology, and NIHR Moorfields Biomedical Research Centre, University College London, London, UK.
Small GTPases. 2021 May;12(3):209-225. doi: 10.1080/21541248.2020.1724596. Epub 2020 Feb 14.
Cancer is the second leading cause of death globally, and colorectal cancer (CRC) is among the five most common cancers. The small GTPase KRAS is an oncogene that is mutated in ~30% of all CRCs. Pharmacological treatments of CRC are currently unsatisfactory, but much hope rests on network-centric approaches to drug development and cancer treatment. These approaches, however, require a better understanding of how networks downstream of Ras oncoproteins are connected in a particular tissue context - here colon and CRC. Previously we have shown that competition for binding to a 'hub' protein, such as Ras, can induce a rewiring of signal transduction networks. In this study, we analysed 56 established and predicted effectors that contain a structural domain with the potential ability to bind to Ras oncoproteins and their link to pathways coordinating intestinal homoeostasis and barrier function. Using protein concentrations in colon tissue and Ras-effector binding affinities, a computational network model was generated that predicted how effectors differentially and competitively bind to Ras in colon context. The model also predicted both qualitative and quantitative changes in Ras-effector complex formations with increased levels of active Ras - to simulate its upregulation in cancer - simply as an emergent property of competition for the same binding interface on the surface of Ras. We also considered how the number of Ras-effector complexes at the membrane can be increased by additional domains present in some effectors that are recruited to the membrane in response to specific conditions (inputs/stimuli/growth factors) in colon context and CRC.
癌症是全球第二大致死原因,而结直肠癌(CRC)是最常见的五种癌症之一。小 GTP 酶 KRAS 是一种致癌基因,约 30%的 CRC 都发生了 KRAS 突变。目前 CRC 的药物治疗效果并不理想,但人们普遍寄希望于以网络为中心的药物开发和癌症治疗方法。然而,这些方法需要更好地了解 Ras 癌蛋白下游的网络在特定组织背景(此处为结肠和 CRC)中是如何连接的。此前我们已经表明,与 Ras 等“枢纽”蛋白的结合竞争可以诱导信号转导网络的重新布线。在这项研究中,我们分析了 56 种已建立和预测的效应物,这些效应物包含一个潜在的结构域,能够与 Ras 癌蛋白及其与协调肠道内稳态和屏障功能的途径结合。利用结肠组织中的蛋白质浓度和 Ras 效应物的结合亲和力,生成了一个计算网络模型,预测了效应物在结肠环境中如何竞争地、差异化地与 Ras 结合。该模型还预测了活性 Ras 水平升高(模拟癌症中的 Ras 上调)时 Ras 效应物复合物形成的定性和定量变化,这仅仅是由于竞争 Ras 表面相同结合界面的结果。我们还考虑了在结肠环境和 CRC 中,一些效应物由于特定条件(输入/刺激/生长因子)而被募集到膜上,从而增加了膜上 Ras 效应物复合物的数量。