John August J, Ghose Emily T, Gao Huanyao, Luck Meagan, Jeong Dabin, Kalari Krishna R, Wang Liewei
Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Rochester, MN, United States.
Department of Biological Sciences, University of Notre Dame, South Bend, IN, United States.
Front Oncol. 2024 May 31;14:1343091. doi: 10.3389/fonc.2024.1343091. eCollection 2024.
Cancer is typically treated with combinatorial therapy, and such combinations may be synergistic. However, discovery of these combinations has proven difficult as brute force combinatorial screening approaches are both logistically complex and resource-intensive. Therefore, computational approaches to augment synergistic drug discovery are of interest, but current approaches are limited by their dependencies on combinatorial drug screening training data or molecular profiling data. These dataset dependencies can limit the number and diversity of drugs for which these approaches can make inferences. Herein, we describe a novel computational framework, ReCorDE (Recurrent Correlation of Drugs with Enrichment), that uses publicly-available cell line-derived monotherapy cytotoxicity datasets to identify drug classes targeting shared vulnerabilities across multiple cancer lineages; and we show how these inferences can be used to augment synergistic drug combination discovery. Additionally, we demonstrate in preclinical models that a drug class combination predicted by ReCorDE to target shared vulnerabilities (PARP inhibitors and Aurora kinase inhibitors) exhibits class-class synergy across lineages. ReCorDE functions independently of combinatorial drug screening and molecular profiling data, using only extensive monotherapy cytotoxicity datasets as its input. This allows ReCorDE to make robust inferences for a large, diverse array of drugs. In conclusion, we have described a novel framework for the identification of drug classes targeting shared vulnerabilities using monotherapy cytotoxicity datasets, and we showed how these inferences can be used to aid discovery of novel synergistic drug combinations.
癌症通常采用联合疗法进行治疗,而且这种联合可能具有协同作用。然而,事实证明,发现这些联合疗法很困难,因为蛮力组合筛选方法在逻辑上既复杂又耗费资源。因此,增强协同药物发现的计算方法备受关注,但目前的方法受到对组合药物筛选训练数据或分子谱数据的依赖的限制。这些数据集依赖性会限制这些方法能够进行推断的药物的数量和多样性。在此,我们描述了一种新颖的计算框架ReCorDE(药物与富集的循环相关性),它使用公开可用的细胞系衍生单药细胞毒性数据集来识别针对多个癌症谱系中共同脆弱性的药物类别;并且我们展示了如何利用这些推断来增强协同药物组合的发现。此外,我们在临床前模型中证明,ReCorDE预测的针对共同脆弱性的药物类别组合(聚(ADP - 核糖)聚合酶抑制剂和极光激酶抑制剂)在各谱系中表现出类别 - 类别协同作用。ReCorDE独立于组合药物筛选和分子谱数据发挥作用,仅使用广泛的单药细胞毒性数据集作为其输入。这使得ReCorDE能够对大量多样的药物做出可靠的推断。总之,我们描述了一种使用单药细胞毒性数据集识别针对共同脆弱性的药物类别的新颖框架,并且展示了如何利用这些推断来辅助发现新型协同药物组合。