Suppr超能文献

用二肽抑制剂阐明寨卡病毒NS2B-NS3蛋白酶的抑制机制:来自分子对接和分子动力学模拟的见解

Elucidating the inhibitory mechanism of Zika virus NS2B-NS3 protease with dipeptide inhibitors: Insights from molecular docking and molecular dynamics simulations.

作者信息

Ullah Shahid, Ullah Farhan, Rahman Wajeeha, Ullah Anees, Haider Sultan, Yueguang Cao

机构信息

S-Khan Lab, Mardan, Khyber Pakhtunkhwa, Pakistan.

Huazhong University of Science and Technology Union Shenzhen Hospital, Nanshan, Shenzhen, China.

出版信息

PLoS One. 2024 Aug 8;19(8):e0307902. doi: 10.1371/journal.pone.0307902. eCollection 2024.

Abstract

Microcephaly, Guillain-Barré syndrome, and potential sexual transmission stand as prominent complications associated with Zika virus (ZIKV) infection. The absence of FDA-approved drugs or vaccines presents a substantial obstacle in combatting the virus. Furthermore, the inclusion of pregnancy in the pharmacological screening process complicates and extends the endeavor to ensure molecular safety and minimal toxicity. Given its pivotal role in viral assembly and maturation, the NS2B-NS3 viral protease emerges as a promising therapeutic target against ZIKV. In this context, a dipeptide inhibitor was specifically chosen as a control against 200 compounds for docking analysis. Subsequent molecular dynamics simulations extending over 200 ns were conducted to ascertain the stability of the docked complex and confirm the binding of the inhibitor at the protein's active site. The simulation outcomes exhibited conformity to acceptable thresholds, encompassing parameters such as root mean square deviation (RMSD), root mean square fluctuation (RMSF), ligand-protein interaction analysis, ligand characterization, and surface area analysis. Notably, analysis of ligand angles bolstered the identification of prospective ligands capable of inhibiting viral protein activity and impeding virus dissemination. In this study, the integration of molecular docking and dynamics simulations has pinpointed the dipeptide inhibitor as a potential candidate ligand against ZIKV protease, thereby offering promise for therapeutic intervention against the virus.

摘要

小头畸形、吉兰-巴雷综合征以及潜在的性传播是与寨卡病毒(ZIKV)感染相关的主要并发症。缺乏FDA批准的药物或疫苗在对抗该病毒方面构成了重大障碍。此外,将妊娠纳入药理筛选过程使确保分子安全性和最小毒性的努力变得复杂且耗时。鉴于NS2B-NS3病毒蛋白酶在病毒组装和成熟中起关键作用,它成为对抗ZIKV的一个有前景的治疗靶点。在此背景下,特意选择一种二肽抑制剂作为对照,与200种化合物进行对接分析。随后进行了长达200纳秒的分子动力学模拟,以确定对接复合物的稳定性,并确认抑制剂在蛋白质活性位点的结合。模拟结果符合可接受的阈值,包括均方根偏差(RMSD)、均方根波动(RMSF)、配体-蛋白质相互作用分析、配体表征和表面积分析等参数。值得注意的是,配体角度分析有助于识别能够抑制病毒蛋白活性并阻止病毒传播的潜在配体。在本研究中,分子对接和动力学模拟的结合已确定二肽抑制剂是对抗ZIKV蛋白酶的潜在候选配体,从而为针对该病毒的治疗干预带来了希望。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/54c1/11309477/e3a3ce69a834/pone.0307902.g001.jpg

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验