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使用机器学习预测用于治疗杜氏肌营养不良症的提前终止密码子抑制化合物。

Prediction of Premature Termination Codon Suppressing Compounds for Treatment of Duchenne Muscular Dystrophy Using Machine Learning.

机构信息

MAP program, University of California San Diego (UCSD), La Jolla, CA 92093, USA.

Curematch Inc., 6440 Lusk Blvd, Suite D206, San Diego, CA 92121, USA.

出版信息

Molecules. 2020 Aug 26;25(17):3886. doi: 10.3390/molecules25173886.

Abstract

A significant percentage of Duchenne muscular dystrophy (DMD) cases are caused by premature termination codon (PTC) mutations in the dystrophin gene, leading to the production of a truncated, non-functional dystrophin polypeptide. PTC-suppressing compounds (PTCSC) have been developed in order to restore protein translation by allowing the incorporation of an amino acid in place of a stop codon. However, limitations exist in terms of efficacy and toxicity. To identify new compounds that have PTC-suppressing ability, we selected and clustered existing PTCSC, allowing for the construction of a common pharmacophore model. Machine learning (ML) and deep learning (DL) models were developed for prediction of new PTCSC based on known compounds. We conducted a search of the NCI compounds database using the pharmacophore-based model and a search of the DrugBank database using pharmacophore-based, ML and DL models. Sixteen drug compounds were selected as a consensus of pharmacophore-based, ML, and DL searches. Our results suggest notable correspondence of the pharmacophore-based, ML, and DL models in prediction of new PTC-suppressing compounds.

摘要

很大比例的杜氏肌营养不良症(DMD)是由于抗肌萎缩蛋白基因中的提前终止密码子(PTC)突变引起的,导致产生截短的、无功能的抗肌萎缩蛋白多肽。为了通过允许用氨基酸替代终止密码子来恢复蛋白质翻译,已经开发了 PTC 抑制化合物(PTCSC)。然而,在疗效和毒性方面存在限制。为了确定具有 PTC 抑制能力的新化合物,我们选择并聚类了现有的 PTCSC,从而构建了一个共同的药效团模型。基于已知化合物,使用机器学习(ML)和深度学习(DL)模型来开发预测新的 PTCSC 的模型。我们使用基于药效团的模型对 NCI 化合物数据库进行搜索,并使用基于药效团的、ML 和 DL 模型对 DrugBank 数据库进行搜索。选择了 16 种药物化合物作为基于药效团的、ML 和 DL 搜索的共识。我们的结果表明,基于药效团的、ML 和 DL 模型在预测新的 PTC 抑制化合物方面具有显著的一致性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8cd9/7503396/ebb0508de963/molecules-25-03886-g001.jpg

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