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基于结构预测致病微生物中Nudix酶潜在抑制剂的功能位点

Structure based prediction of functional sites with potential inhibitors to Nudix enzymes from disease causing microbes.

作者信息

Sharma Ashwani, Tendulkar Ashish Vijay, Wangikar Pramod Prabhakar

出版信息

Bioinformation. 2011 Jan 22;5(8):341-9. doi: 10.6026/97320630005341.

Abstract

The functional sites were predicted for Nudix enzymes from pathogenic microorganisms such as Streprococcus pneumonia (2B06) and Enterococcus faecalis (2AZW). Their structures are already determined, however, no data is reported about their functional sites, substrates and inhibitors. Therefore, we report prediction of functional sites in these Nudix enzymes via Geometric Invariant (GI) technique (Construct different geometries of peptides which remain unchanged). The GI method enumerated 2B06: RA57, EA58, EA61, EA62 and 2AZW: RA62, EA63, EA66, EA67 as putative functional sites in these Nudix enzymes. In addition, the substrate was predicted via Molecular docking (Docking of substrates against whole structure of Nudix enzymes). The substrate ADP-Ribose was docked with the Nudix enzymes, 2B06 (Docking energy -15.68 Kcal/mol) and 2AZW (Docking energy -10.86 Kcal/mol) with the higher affinity and the lower docking energy as compared to other substrates. The residues EA62 in 2B06 and RA62 in 2AZW make hydrogen bonds with the ADP-ribose. Furthermore, we screened 51 inhibitor compounds against structures of 2B06 and 2AZW. The inhibitor compounds AMPCPR and CID14258187 were docked well as compared to other compounds. The compound CID14258187 was also in agreement with Lipinski rule of 5 for drug likeness properties. Therefore, our findings of functional sites, substrates and inhibitors for these Nudix enzymes may help in structure based drug designing against Streprococcus pneumonia and Enterococcus faecalis.

摘要

对来自肺炎链球菌(2B06)和粪肠球菌(2AZW)等致病微生物的Nudix酶的功能位点进行了预测。它们的结构已经确定,然而,关于其功能位点、底物和抑制剂尚无数据报道。因此,我们通过几何不变量(GI)技术(构建保持不变的不同肽几何结构)报告了这些Nudix酶功能位点的预测。GI方法列举出2B06的RA57、EA58、EA61、EA62以及2AZW的RA62、EA63、EA66、EA67为这些Nudix酶中的假定功能位点。此外,通过分子对接(将底物与Nudix酶的整个结构进行对接)预测了底物。与其他底物相比,底物ADP - 核糖与Nudix酶2B06(对接能量 - 15.68千卡/摩尔)和2AZW(对接能量 - 10.86千卡/摩尔)以更高的亲和力和更低的对接能量进行了对接。2B06中的残基EA62和2AZW中的RA62与ADP - 核糖形成氢键。此外,我们针对2B06和2AZW的结构筛选了51种抑制剂化合物。与其他化合物相比,抑制剂化合物AMPCPR和CID14258187对接良好。化合物CID14258187在药物相似性性质方面也符合Lipinski的五规则。因此,我们对这些Nudix酶的功能位点、底物和抑制剂的研究结果可能有助于针对肺炎链球菌和粪肠球菌进行基于结构的药物设计。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6f3/3046039/43f96436026c/97320630005341F1.jpg

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