• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

通过抗分枝杆菌药物发现中的二次筛选实现更快的通过/不通过决策。

Enabling faster Go/No-Go decisions through secondary screens in anti-mycobacterial drug discovery.

作者信息

Mukherjee Raju, Chandra Pal Anup, Banerjee Mousumi

机构信息

Division of Biology, Indian Institute of Science Education and Research, Karakambadi Road, Tirupati, 517507, India.

Division of Biology, Indian Institute of Science Education and Research, Karakambadi Road, Tirupati, 517507, India.

出版信息

Tuberculosis (Edinb). 2017 Sep;106:44-52. doi: 10.1016/j.tube.2017.06.004. Epub 2017 Jun 30.

DOI:10.1016/j.tube.2017.06.004
PMID:28802404
Abstract

Management of tuberculosis, already a global health emergency, is becoming increasingly challenging with extensive misuse of second line drugs and their inaccessibility to eighty percent of the eligible patients. Rising statistics of antimicrobial resistance underscores the need for a set of completely new and more effective class of compounds with novel mechanisms of action that can be administered in combination to replace and shorten the present intensive six months regimen. In this review, we stress on the importance and the successes of phenotypic screening for discovery of anti-mycobacterial compound and discuss the importance of performing secondary screens and counter screens to get early estimate on compound's potentials for a successful development. We also highlight the recent advances and the related caveats in the assays that have been developed and discuss new screening modalities that can be incorporated during hit-selection to gain a quick insight into the mechanism of action, thus enabling quicker decisions in a hit triage.

摘要

结核病的管理已然是一场全球卫生紧急事件,随着二线药物的广泛滥用以及80%的符合条件患者无法获取这些药物,其管理正变得愈发具有挑战性。抗菌药物耐药性统计数据的不断上升凸显了对一类全新且更有效的化合物的需求,这类化合物具有新颖的作用机制,可联合使用以替代并缩短目前为期六个月的强化治疗方案。在本综述中,我们强调了表型筛选在发现抗分枝杆菌化合物方面的重要性和成功之处,并讨论了进行二次筛选和反筛选以尽早评估化合物成功开发潜力的重要性。我们还突出了已开发检测方法的最新进展及相关注意事项,并讨论了在命中选择过程中可纳入的新筛选模式,以便快速洞察作用机制,从而在命中物分类中做出更快决策。

相似文献

1
Enabling faster Go/No-Go decisions through secondary screens in anti-mycobacterial drug discovery.通过抗分枝杆菌药物发现中的二次筛选实现更快的通过/不通过决策。
Tuberculosis (Edinb). 2017 Sep;106:44-52. doi: 10.1016/j.tube.2017.06.004. Epub 2017 Jun 30.
2
Perspective: Challenges and opportunities in TB drug discovery from phenotypic screening.观点:基于表型筛选的结核病药物研发中的挑战与机遇
Bioorg Med Chem. 2015 Aug 15;23(16):5087-97. doi: 10.1016/j.bmc.2014.12.031. Epub 2014 Dec 24.
3
The future for early-stage tuberculosis drug discovery.早期结核病药物发现的未来。
Future Microbiol. 2015;10(2):217-29. doi: 10.2217/fmb.14.125.
4
Mycobacterium tuberculosis High-Throughput Screening.结核分枝杆菌高通量筛选
Methods Mol Biol. 2016;1439:181-95. doi: 10.1007/978-1-4939-3673-1_12.
5
The role of the time-kill kinetics assay as part of a preclinical modeling framework for assessing the activity of anti-tuberculosis drugs.时间杀菌动力学测定作为评估抗结核药物活性的临床前建模框架一部分的作用。
Tuberculosis (Edinb). 2017 Jul;105:80-85. doi: 10.1016/j.tube.2017.04.010. Epub 2017 Apr 27.
6
Identification and validation of novel drug targets in Mycobacterium tuberculosis.结核分枝杆菌中新药物靶点的鉴定与验证
Drug Discov Today. 2017 Mar;22(3):503-509. doi: 10.1016/j.drudis.2016.09.010. Epub 2016 Sep 17.
7
Bioluminescent Reporters for Rapid Mechanism of Action Assessment in Tuberculosis Drug Discovery.用于结核病药物发现中快速作用机制评估的生物发光报告基因
Antimicrob Agents Chemother. 2016 Oct 21;60(11):6748-6757. doi: 10.1128/AAC.01178-16. Print 2016 Nov.
8
Why are membrane targets discovered by phenotypic screens and genome sequencing in Mycobacterium tuberculosis?为什么在结核分枝杆菌中通过表型筛选和基因组测序发现膜靶标?
Tuberculosis (Edinb). 2013 Nov;93(6):569-88. doi: 10.1016/j.tube.2013.09.003. Epub 2013 Sep 18.
9
drug discovery models for relevant for host infection.用于宿主感染相关的药物发现模型。
Expert Opin Drug Discov. 2020 Mar;15(3):349-358. doi: 10.1080/17460441.2020.1707801. Epub 2020 Jan 3.
10
The relevance of persisters in tuberculosis drug discovery.潜伏者在结核病药物发现中的相关性。
Microbiology (Reading). 2019 May;165(5):492-499. doi: 10.1099/mic.0.000760. Epub 2019 Feb 18.

引用本文的文献

1
Innovation Experiences from Africa-Led Drug Discovery at the Holistic Drug Discovery and Development (H3D) Centre.整体药物发现与开发(H3D)中心的非洲主导药物发现创新经验。
ACS Med Chem Lett. 2022 Jul 11;13(8):1221-1230. doi: 10.1021/acsmedchemlett.2c00142. eCollection 2022 Aug 11.
2
Editorial: Tuberculosis Drug Discovery & Development: Drug Targets, Chemical Matter, and Approaches.社论:结核病药物的发现与开发:药物靶点、化学物质及方法
Front Cell Infect Microbiol. 2021 Sep 9;11:755459. doi: 10.3389/fcimb.2021.755459. eCollection 2021.