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对圣杯的探索:新型抗结核化学实体、靶点与策略

The quest for the holy grail: new antitubercular chemical entities, targets and strategies.

作者信息

Huszár Stanislav, Chibale Kelly, Singh Vinayak

机构信息

Drug Discovery and Development Centre (H3D), University of Cape Town, Rondebosch 7701, South Africa.

Drug Discovery and Development Centre (H3D), University of Cape Town, Rondebosch 7701, South Africa; South African Medical Research Council Drug Discovery and Development Research Unit, Department of Chemistry and Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa.

出版信息

Drug Discov Today. 2020 Apr;25(4):772-780. doi: 10.1016/j.drudis.2020.02.003. Epub 2020 Feb 13.

DOI:10.1016/j.drudis.2020.02.003
PMID:32062007
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7215093/
Abstract

Tuberculosis (TB) remains the leading cause of death from an infectious disease worldwide. TB therapy is complicated by the protracted treatment regimens, development of resistance coupled with toxicity and insufficient sterilizing capacity of current drugs. Although considerable progress has been made on establishing a TB drug pipeline, the high attrition rate reinforces the need to continually replenish the pipeline with high-quality leads that act through inhibition of novel targets. In this review, we highlight some of the key advances that have assisted TB drug discovery with novel chemical matter, targets and strategies - to fuel the TB drug pipeline.

摘要

结核病(TB)仍然是全球传染病致死的主要原因。结核病治疗因疗程漫长、耐药性的产生、药物毒性以及现有药物杀菌能力不足而变得复杂。尽管在建立结核病药物研发线方面已经取得了相当大的进展,但高淘汰率凸显了持续用通过抑制新靶点起作用的高质量先导化合物来充实研发线的必要性。在本综述中,我们重点介绍了一些关键进展,这些进展借助新型化学物质、靶点和策略推动了结核病药物研发,为结核病药物研发线提供动力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d2d1/7215093/6326f168acb9/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d2d1/7215093/66278ee6b5c7/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d2d1/7215093/bf328c5e4837/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d2d1/7215093/6326f168acb9/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d2d1/7215093/66278ee6b5c7/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d2d1/7215093/bf328c5e4837/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d2d1/7215093/6326f168acb9/gr3.jpg

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用于下一代结核病治疗的纳米增强型MbtI抑制剂
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Target Identification in Anti-Tuberculosis Drug Discovery.抗结核药物发现中的靶点鉴定。
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