Department of Bioinformatics, Fraunhofer Institute for Algorithms and Scientific Computing (SCAI), 53757, Sankt, Augustin, Germany.
Fraunhofer Center for Machine Learning, Sankt, Germany.
Sci Rep. 2023 May 3;13(1):7159. doi: 10.1038/s41598-023-34287-5.
In addition to vaccines, the World Health Organization sees novel medications as an urgent matter to fight the ongoing COVID-19 pandemic. One possible strategy is to identify target proteins, for which a perturbation by an existing compound is likely to benefit COVID-19 patients. In order to contribute to this effort, we present GuiltyTargets-COVID-19 ( https://guiltytargets-covid.eu/ ), a machine learning supported web tool to identify novel candidate drug targets. Using six bulk and three single cell RNA-Seq datasets, together with a lung tissue specific protein-protein interaction network, we demonstrate that GuiltyTargets-COVID-19 is capable of (i) prioritizing meaningful target candidates and assessing their druggability, (ii) unraveling their linkage to known disease mechanisms, (iii) mapping ligands from the ChEMBL database to the identified targets, and (iv) pointing out potential side effects in the case that the mapped ligands correspond to approved drugs. Our example analyses identified 4 potential drug targets from the datasets: AKT3 from both the bulk and single cell RNA-Seq data as well as AKT2, MLKL, and MAPK11 in the single cell experiments. Altogether, we believe that our web tool will facilitate future target identification and drug development for COVID-19, notably in a cell type and tissue specific manner.
除了疫苗,世界卫生组织还将新型药物视为应对当前 COVID-19 大流行的紧急事项。一种可能的策略是确定靶蛋白,通过现有化合物对其进行干扰可能有益于 COVID-19 患者。为了为此项工作做出贡献,我们提出了 GuiltyTargets-COVID-19(https://guiltytargets-covid.eu/),这是一个基于机器学习的网络工具,用于识别新的候选药物靶点。使用六个批量和三个单细胞 RNA-Seq 数据集,以及一个肺组织特异性蛋白质-蛋白质相互作用网络,我们证明了 GuiltyTargets-COVID-19 能够(i)优先考虑有意义的候选靶标,并评估其可成药性,(ii)揭示其与已知疾病机制的联系,(iii)将 ChEMBL 数据库中的配体映射到鉴定出的靶标,以及(iv)在映射的配体对应于已批准药物的情况下指出潜在的副作用。我们的示例分析从数据集确定了 4 个潜在的药物靶点:批量和单细胞 RNA-Seq 数据中的 AKT3 以及单细胞实验中的 AKT2、MLKL 和 MAPK11。总之,我们相信我们的网络工具将有助于未来 COVID-19 的靶标识别和药物开发,特别是在细胞类型和组织特异性方面。