Strategies for Designing Novel Anti-Tubercular Drugs with Special Reference to Mycobacterial MelF (Rv1936) as a Target

R. Dharra, Mehta Pk
{"title":"Strategies for Designing Novel Anti-Tubercular Drugs with Special Reference to Mycobacterial MelF (Rv1936) as a Target","authors":"R. Dharra, Mehta Pk","doi":"10.4172/2161-1068.1000262","DOIUrl":null,"url":null,"abstract":"Tuberculosis (TB) is a major public health problem throughout the world. There is an immediate need to device novel anti-tubercular drugs (ATDs). Whole cell screening (WCS) and target based screening (TBS) approaches are widely used to devise new ATDs. WCS is considered relatively a favourable strategy but it lacks in the precise target knowledge, whereas the target based hit compounds may not ensure the drugability. In this manuscript, we have discussed the potent inhibitors designed against the mycobacterial MelF (Rv1936) by using the TBS as well as virtual ligand screening, which also revealed synergistic effect with the first-line bactericidal drugs, i.e., isoniazid and rifampicin.","PeriodicalId":74235,"journal":{"name":"Mycobacterial diseases : tuberculosis & leprosy","volume":"8 1","pages":"1-3"},"PeriodicalIF":0.0000,"publicationDate":"2018-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"1","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Mycobacterial diseases : tuberculosis & leprosy","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.4172/2161-1068.1000262","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 1

Abstract

Tuberculosis (TB) is a major public health problem throughout the world. There is an immediate need to device novel anti-tubercular drugs (ATDs). Whole cell screening (WCS) and target based screening (TBS) approaches are widely used to devise new ATDs. WCS is considered relatively a favourable strategy but it lacks in the precise target knowledge, whereas the target based hit compounds may not ensure the drugability. In this manuscript, we have discussed the potent inhibitors designed against the mycobacterial MelF (Rv1936) by using the TBS as well as virtual ligand screening, which also revealed synergistic effect with the first-line bactericidal drugs, i.e., isoniazid and rifampicin.
以分枝杆菌MelF (Rv1936)为靶点的新型抗结核药物的设计策略
结核病(TB)是全世界的一个主要公共卫生问题。迫切需要研制新型抗结核药物(ATDs)。全细胞筛选(WCS)和基于靶标的筛选(TBS)方法被广泛用于设计新的ATDs。WCS被认为是一种相对有利的策略,但它缺乏精确的靶点知识,而基于靶点的hit化合物可能无法确保其可药物性。在本文中,我们讨论了利用TBS和虚拟配体筛选设计的针对分枝杆菌MelF (Rv1936)的强效抑制剂,并显示了与一线杀菌药物异烟肼和利福平的协同作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 求助全文
来源期刊
自引率
0.00%
发文量
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信