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MmpL3抑制剂与抗结核化合物的协同相互作用

Synergistic Interactions of MmpL3 Inhibitors with Antitubercular Compounds .

作者信息

Li Wei, Sanchez-Hidalgo Andrea, Jones Victoria, de Moura Vinicius Calado Nogueira, North E Jeffrey, Jackson Mary

机构信息

Mycobacteria Research Laboratories, Department of Microbiology, Immunology and Pathology, Colorado State University, Fort Collins, Colorado, USA.

Creighton University, School of Pharmacy & Health Professions, Department of Pharmacy Sciences, Omaha, Nebraska, USA.

出版信息

Antimicrob Agents Chemother. 2017 Mar 24;61(4). doi: 10.1128/AAC.02399-16. Print 2017 Apr.

DOI:10.1128/AAC.02399-16
PMID:28115355
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5365669/
Abstract

A number of inhibitors of the essential mycolic acid transporter, MmpL3, are currently under development as potential novel antituberculosis agents. Using the checkerboard method to study the interaction profiles of various antituberculosis drugs or experimental compounds with two different chemotypes inhibiting this transporter (indolcarboxamides and adamantyl ureas), we showed that MmpL3 inhibitors act synergistically with rifampin, bedaquiline, clofazimine, and β-lactams.

摘要

作为潜在的新型抗结核药物，多种必需分枝菌酸转运蛋白MmpL3的抑制剂目前正在研发中。我们使用棋盘法研究了各种抗结核药物或实验化合物与抑制该转运蛋白的两种不同化学类型（吲哚羧酰胺和金刚烷基脲）的相互作用情况，结果表明MmpL3抑制剂与利福平、贝达喹啉、氯法齐明和β-内酰胺类药物具有协同作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d70/5365669/f598f95830c0/zac0041760290002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d70/5365669/673f7954e4da/zac004176029001a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d70/5365669/f598f95830c0/zac0041760290002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d70/5365669/673f7954e4da/zac004176029001a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d70/5365669/f598f95830c0/zac0041760290002.jpg

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ACS Infect Dis. 2016 Oct 14;2(10):702-713. doi: 10.1021/acsinfecdis.6b00095. Epub 2016 Sep 1.
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Diphenylether-Modified 1,2-Diamines with Improved Drug Properties for Development against Mycobacterium tuberculosis.具有改善药物特性的二苯醚修饰的1,2 - 二胺用于抗结核分枝杆菌的研发。
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Therapeutic Potential of the Mycobacterium tuberculosis Mycolic Acid Transporter, MmpL3.
MmpL3 抑制剂 MSU-43085 在感染的小鼠模型中具有活性。
Microbiol Spectr. 2024 Jan 11;12(1):e0367723. doi: 10.1128/spectrum.03677-23. Epub 2023 Dec 11.
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Recent advances in mycobacterial membrane protein large 3 inhibitor drug design for mycobacterial infections.分枝杆菌膜蛋白大 3 抑制剂在分枝杆菌感染药物设计中的最新进展。
Expert Opin Drug Discov. 2023 Jul;18(7):707-724. doi: 10.1080/17460441.2023.2218082. Epub 2023 Jun 4.
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Molecular Mechanisms of MmpL3 Function and Inhibition.MmpL3 功能和抑制的分子机制。
Microb Drug Resist. 2023 May;29(5):190-212. doi: 10.1089/mdr.2021.0424. Epub 2023 Feb 21.
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Anti-tuberculosis drug development targeting the cell envelope of .针对……细胞包膜的抗结核药物研发
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