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设计多靶点分子:结合分子筛选和计算机药物心脏毒性预测方法。

Designing of multi-targeted molecules using combination of molecular screening and in silico drug cardiotoxicity prediction approaches.

机构信息

Computational Biology and Bioinformatics, Graduate School of Science and Engineering, Kadir Has University, Istanbul, Turkey.

Department of Biophysics, School of Medicine, Bahcesehir University, Istanbul, Turkey.

出版信息

J Mol Graph Model. 2014 May;50:16-34. doi: 10.1016/j.jmgm.2014.02.007. Epub 2014 Mar 6.

Abstract

We have previously investigated and reported a set of phenol- and indole-based derivatives at the binding pockets of carbonic anhydrase isoenzymes using in silico and in vitro analyses. In this study, we extended our analysis to explore multi-targeted molecules from this set of compounds. Thus, 26 ligands are screened at the binding sites of 229 proteins from 5 main enzyme family classes using molecular docking algorithms. Derived docking scores are compared with reported results of ligands at carbonic anhydrase I and II isoenzymes. Results showed potency of multi-targeted drugs of a few compounds from investigated ligand set. These promising ligands are then tested in silico for their cardiotoxicity risks. Results of this work can be used to improve the desired effects of these compounds by molecular engineering studies. In addition these results may lead to further investigation of studied molecules by medicinal chemists to explore different therapeutic aims.

摘要

我们之前已经使用计算机模拟和体外分析的方法,研究并报道了一组结合在碳酸酐酶同工酶结合口袋中的酚类和吲哚类衍生物。在本研究中,我们扩展了分析,从这组化合物中探索多靶标分子。因此,使用分子对接算法在 5 个主要酶家族类别的 229 个蛋白质的结合位点上筛选了 26 个配体。所得对接评分与碳酸酐酶 I 和 II 同工酶中配体的报道结果进行了比较。结果表明,从研究的配体集中有几个化合物具有多靶标药物的潜力。然后,通过计算机模拟测试这些有前途的配体的心脏毒性风险。这项工作的结果可用于通过分子工程研究来提高这些化合物的预期效果。此外,这些结果可能导致药物化学家进一步研究这些分子,以探索不同的治疗目标。

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