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大环化合物作为FK506结合蛋白抑制剂的分子对接研究

Molecular docking study of macrocycles as Fk506-binding protein inhibitors.

作者信息

MacDonald Corey A, Boyd Russell J

机构信息

Department of Chemistry, Dalhousie University, 62 74 Coburg Road, Halifax, NS, Canada B3H 4R2.

Department of Chemistry, Dalhousie University, 62 74 Coburg Road, Halifax, NS, Canada B3H 4R2.

出版信息

J Mol Graph Model. 2015 Jun;59:117-22. doi: 10.1016/j.jmgm.2015.04.009. Epub 2015 Apr 29.

Abstract

To prepare for future resistance, new methods are being explored for novel treatment of malaria. The current work uses high performance docking methods to model different substrates binding into the active sites of varying Homo sapien and Plasmodium peptidyl-prolyl cis/trans isomerase enzymes and compares their subsequent docking scores. This approach has shown that the substrates ILS-920 and WYE-592 will bind less-favourably with hFKBP12 and PfFKBP35 compared to a competing substrate rapamycin; however, the binding appears to be more favourable in PvFKBP35. This could suggest a possible target for inhibition of the Plasmodium vivax parasite.

摘要

为应对未来的耐药性问题,人们正在探索用于疟疾新疗法的新方法。当前的研究工作使用高性能对接方法来模拟不同底物与人类和疟原虫肽基脯氨酰顺反异构酶不同活性位点的结合,并比较它们随后的对接分数。该方法表明,与竞争性底物雷帕霉素相比,底物ILS-920和WYE-592与hFKBP12和PfFKBP35的结合不太有利;然而,在PvFKBP35中这种结合似乎更有利。这可能提示了一种抑制间日疟原虫的潜在靶点。

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