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对恶性疟原虫DegP蛋白进行计算机模拟研究以寻找抗疟药物。

In-silico studies on DegP protein of Plasmodium falciparum in search of anti-malarials.

作者信息

Sharma Drista, Soni Rani, Patel Sachin, Joshi Deepti, Bhatt Tarun Kumar

机构信息

Department of Biotechnology, Central University of Rajasthan, NH-8, Bandarsindri, Rajasthan, India, 305801.

出版信息

J Mol Model. 2016 Sep;22(9):201. doi: 10.1007/s00894-016-3064-3. Epub 2016 Aug 4.

Abstract

Despite encouraging progress over the past decade, malaria caused by the Plasmodium parasite continues to pose an enormous disease burden and is one of the major global health problems. The extreme challenge in malaria management is the resistance of parasites to traditional monochemotherapies like chloroquine and sulfadoxine-pyrimethamine. No vaccine is yet in sight, and the foregoing effective drugs are also losing ground against the disease due to the resistivity of parasites. New antimalarials with novel mechanisms of action are needed to circumvent existing or emerging drug resistance. DegP protein, secretory in nature has been shown to be involved in regulation of thermo-oxidative stress generated during asexual life cycle of Plasmodium, probably required for survival of parasite in host. Considering the significance of protein, in this study, we have generated a three-dimensional structure of PfDegP followed by validation of the modeled structure using several tools like RAMPAGE, ERRAT, and others. We also performed an in-silico screening of small molecule database against PfDegP using Glide. Furthermore, molecular dynamics simulation of protein and protein-ligand complex was carried out using GROMACS. This study substantiated potential drug-like molecules and provides the scope for development of novel antimalarial drugs.

摘要

尽管在过去十年中取得了令人鼓舞的进展,但疟原虫引起的疟疾仍然构成巨大的疾病负担,是全球主要的健康问题之一。疟疾管理面临的极端挑战是寄生虫对氯喹和磺胺多辛-乙胺嘧啶等传统单一化疗药物产生耐药性。目前尚无疫苗,而且由于寄生虫的耐药性,上述有效药物在对抗该疾病方面也逐渐失效。需要具有新作用机制的新型抗疟药来规避现有的或新出现的耐药性。本质上具有分泌性的DegP蛋白已被证明参与疟原虫无性生命周期中产生的热氧化应激的调节,这可能是寄生虫在宿主体内存活所必需的。鉴于该蛋白的重要性,在本研究中,我们生成了PfDegP的三维结构,随后使用RAMPAGE、ERRAT等多种工具对建模结构进行了验证。我们还使用Glide对小分子数据库针对PfDegP进行了虚拟筛选。此外,使用GROMACS对蛋白质和蛋白质-配体复合物进行了分子动力学模拟。本研究证实了潜在的类药物分子,并为新型抗疟药物的开发提供了空间。

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