Anaxomics Biotech SL, Barcelona, Catalonia, Spain.
Structural Bioinformatics Group, Research Programme on Biomedical Informatics, Department of Experimental and Health Science, Universitat Pompeu Fabra, Barcelona, Catalonia, Spain.
PLoS One. 2020 Feb 13;15(2):e0228926. doi: 10.1371/journal.pone.0228926. eCollection 2020.
Unveiling the mechanism of action of a drug is key to understand the benefits and adverse reactions of a medication in an organism. However, in complex diseases such as heart diseases there is not a unique mechanism of action but a wide range of different responses depending on the patient. Exploring this collection of mechanisms is one of the clues for a future personalized medicine. The Therapeutic Performance Mapping System (TPMS) is a Systems Biology approach that generates multiple models of the mechanism of action of a drug. Each molecular mechanism generated could be associated to particular individuals, here defined as prototype-patients, hence the generation of models using TPMS technology may be used for detecting adverse effects to specific patients. TPMS operates by (1) modelling the responses in humans with an accurate description of a protein network and (2) applying a Multilayer Perceptron-like and sampling strategy to find all plausible solutions. In the present study, TPMS is applied to explore the diversity of mechanisms of action of the drug combination sacubitril/valsartan. We use TPMS to generate a wide range of models explaining the relationship between sacubitril/valsartan and heart failure (the indication), as well as evaluating their association with macular degeneration (a potential adverse effect). Among the models generated, we identify a set of mechanisms of action associated to a better response in terms of heart failure treatment, which could also be associated to macular degeneration development. Finally, a set of 30 potential biomarkers are proposed to identify mechanisms (or prototype-patients) more prone of suffering macular degeneration when presenting good heart failure response. All prototype-patients models generated are completely theoretical and therefore they do not necessarily involve clinical effects in real patients. Data and accession to software are available at http://sbi.upf.edu/data/tpms/.
揭示药物的作用机制是理解药物在生物体中的益处和不良反应的关键。然而,在复杂疾病如心脏病中,不存在单一的作用机制,而是根据患者的不同存在广泛的不同反应。探索这一系列机制是未来个性化药物的线索之一。治疗性能映射系统 (TPMS) 是一种系统生物学方法,可生成药物作用机制的多个模型。生成的每个分子机制都可以与特定的个体相关联,在这里定义为原型患者,因此使用 TPMS 技术生成模型可用于检测特定患者的不良反应。TPMS 通过以下两种方式运行:(1)使用蛋白质网络的精确描述来模拟人类的反应;(2)应用多层感知器类似的和采样策略来找到所有合理的解决方案。在本研究中,TPMS 用于探索药物组合沙库比曲缬沙坦的作用机制多样性。我们使用 TPMS 生成广泛的模型来解释沙库比曲缬沙坦与心力衰竭(适应症)之间的关系,并评估它们与黄斑变性(一种潜在的不良反应)的关联。在所生成的模型中,我们确定了一组与心力衰竭治疗反应更好相关的作用机制,这些机制也可能与黄斑变性的发展相关。最后,提出了一组 30 个潜在的生物标志物,以识别在表现出良好心力衰竭反应时更容易发生黄斑变性的机制(或原型患者)。生成的所有原型患者模型都是完全理论上的,因此它们不一定涉及真实患者的临床效果。数据和软件访问可在 http://sbi.upf.edu/data/tpms/ 上获得。