Suppr超能文献

基于结构的计算方法鉴定结核分枝杆菌核相关蛋白的新型抑制剂

Computational Approaches for the Structure-Based Identification of Novel Inhibitors Targeting Nucleoid-Associated Proteins in Mycobacterium Tuberculosis.

机构信息

Department of Microbiology, Maharshi Dayanand University, Rohtak, 124001, Haryana, India.

Bacterial Pathogenesis Laboratory, Department of Zoology, University of Delhi, Delhi, 110007, India.

出版信息

Mol Biotechnol. 2024 Apr;66(4):814-823. doi: 10.1007/s12033-023-00710-5. Epub 2023 Mar 13.

Abstract

Implementation of computational tools in the identification of novel drug targets for Tuberculosis (TB) has been a promising area of research. TB has been a chronic infectious disease caused by Mycobacterium tuberculosis (Mtb) localized primarily on the lungs and it has been one of the most successful pathogen in the history of mankind. Extensively arising drug resistivity in TB has made it a global challenge and need for new drugs has become utmost important.The involvement of Nucleoid-Associated Proteins (NAPs) in maintaining the structure of the genomic material and regulating various cellular processes like transcription, DNA replication, repair and recombination makes significant, has opened a new arena to find the drugs targeting Mtb. The current study aims to identify potential inhibitors of NAPs through a computational approach. In the present work we worked on the eight NAPs of Mtb, namely, Lsr2, EspR, HupB, HNS, NapA, mIHF and NapM. The structural modelling and analysis of these NAPs were carried out. Moreover, molecular interaction were checked and binding energy was identified for 2500 FDA-approved drugs that were selected for antagonist analysis to choose novel inhibitors targeting NAPs of Mtb. Drugs including Amikacin, streptomycin, kanamycin, and isoniazid along with eight FDA-approved molecules that were found to be potential novel targets for these mycobacterial NAPs and have an impact on their functions. The potentiality of several anti-tubercular drugs as therapeutic agents identified through computational modelling and simulation unlocks a new gateway for accomplishing the goal to treat TB.

摘要

计算工具在结核病(TB)新型药物靶标的识别中的应用一直是一个很有前途的研究领域。结核病是一种由结核分枝杆菌(Mtb)引起的慢性传染病,主要发生在肺部,它是人类历史上最成功的病原体之一。TB 广泛出现的耐药性使其成为全球性挑战,对新药的需求变得至关重要。核小体相关蛋白(NAPs)在维持基因组物质的结构和调节转录、DNA 复制、修复和重组等各种细胞过程中发挥着重要作用,为寻找针对 Mtb 的药物开辟了新的领域。本研究旨在通过计算方法来识别潜在的 NAPs 抑制剂。在本工作中,我们研究了 Mtb 的八种 NAPs,即 Lsr2、EspR、HupB、HNS、NapA、mIHF 和 NapM。对这些 NAPs 进行了结构建模和分析。此外,还检查了分子相互作用,并确定了 2500 种 FDA 批准药物的结合能,这些药物被选为拮抗剂分析,以选择针对 Mtb NAPs 的新型抑制剂。包括阿米卡星、链霉素、卡那霉素和异烟肼在内的药物以及八种被发现对这些分枝杆菌 NAPs 具有潜在作用并影响其功能的 FDA 批准分子被认为是新型抑制剂。通过计算建模和模拟鉴定出几种抗结核药物作为治疗剂的潜力,为实现治疗结核病的目标开辟了新的途径。

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