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咪唑衍生物作为一种新型翻译抑制剂

Imidazole Derivative As a Novel Translation Inhibitor.

作者信息

Lukianov D A, Buev V S, Ivanenkov Y A, Kartsev V G, Skvortsov D A, Osterman I A, Sergiev P V

机构信息

Skolkovo Institute of Science and Technology, Center of Life Sciences, Skolkovo, 143028 Russia.

Lomonosov Moscow State University, Chemistry Department, Moscow, 119991 Russia.

出版信息

Acta Naturae. 2022 Apr-Jun;14(2):71-77. doi: 10.32607/actanaturae.11654.

DOI:10.32607/actanaturae.11654
PMID:35923569
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9307981/
Abstract

Searching for novel compounds with antibiotic activity and understanding their mechanism of action is extremely important. The ribosome is one of the main targets for antibiotics in bacterial cells. Even if the molecule does not suit the clinical application for whatever reasons, an investigation of its mechanism of action can deepen our understanding of the ribosome function. Such data can inform us on how the already used translational inhibitors can be modified. In this study, we demonstrate that 1-(2-oxo-2-((4-phenoxyphenyl).

摘要

寻找具有抗生素活性的新型化合物并了解其作用机制极其重要。核糖体是细菌细胞中抗生素的主要靶点之一。即使该分子由于任何原因不适合临床应用,对其作用机制的研究也可以加深我们对核糖体功能的理解。这些数据可以告诉我们如何对已使用的翻译抑制剂进行修饰。在本研究中,我们证明了1-(2-氧代-2-((4-苯氧基苯基)。 (注:原文最后似乎不完整)

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5f6a/9307981/132ffecbdc55/AN20758251-14-02-071-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5f6a/9307981/5a4cd16046b7/AN20758251-14-02-071-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5f6a/9307981/5ba62dcd6771/AN20758251-14-02-071-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5f6a/9307981/eaa03e2eaa03/AN20758251-14-02-071-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5f6a/9307981/6a1e7774b4a3/AN20758251-14-02-071-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5f6a/9307981/132ffecbdc55/AN20758251-14-02-071-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5f6a/9307981/5a4cd16046b7/AN20758251-14-02-071-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5f6a/9307981/5ba62dcd6771/AN20758251-14-02-071-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5f6a/9307981/eaa03e2eaa03/AN20758251-14-02-071-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5f6a/9307981/6a1e7774b4a3/AN20758251-14-02-071-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5f6a/9307981/132ffecbdc55/AN20758251-14-02-071-g005.jpg

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本文引用的文献

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Nat Chem Biol. 2020 Oct;16(10):1071-1077. doi: 10.1038/s41589-020-0578-x. Epub 2020 Jun 29.
2
Ribosome-Targeting Antibiotics: Modes of Action, Mechanisms of Resistance, and Implications for Drug Design.核糖体靶向抗生素:作用模式、耐药机制及对药物设计的启示。
Annu Rev Biochem. 2018 Jun 20;87:451-478. doi: 10.1146/annurev-biochem-062917-011942. Epub 2018 Mar 23.
3
Klebsazolicin inhibits 70S ribosome by obstructing the peptide exit tunnel.
参与生物化学和光电子学研究:酰基乙炔基环烷[]吡咯与 Δ-吡咯啉通过[3+2]环加成反应构建吡咯并[1',2':2,3]咪唑并[1,5-]吲哚和环庚[4,5]吡咯并[1,2-]吡咯并[1,2-]咪唑。
Int J Mol Sci. 2023 Feb 8;24(4):3404. doi: 10.3390/ijms24043404.
4
Conjugates of Chloramphenicol Amine and Berberine as Antimicrobial Agents.氯霉素胺与小檗碱的共轭物作为抗菌剂
Antibiotics (Basel). 2022 Dec 22;12(1):15. doi: 10.3390/antibiotics12010015.
克雷伯唑菌素通过阻塞肽出口通道来抑制70S核糖体。
Nat Chem Biol. 2017 Oct;13(10):1129-1136. doi: 10.1038/nchembio.2462. Epub 2017 Aug 28.
4
Sorting Out Antibiotics' Mechanisms of Action: a Double Fluorescent Protein Reporter for High-Throughput Screening of Ribosome and DNA Biosynthesis Inhibitors.梳理抗生素的作用机制:用于核糖体和DNA生物合成抑制剂高通量筛选的双荧光蛋白报告基因
Antimicrob Agents Chemother. 2016 Nov 21;60(12):7481-7489. doi: 10.1128/AAC.02117-16. Print 2016 Dec.
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The challenge of efflux-mediated antibiotic resistance in Gram-negative bacteria.革兰氏阴性菌中由外排介导的抗生素耐药性挑战。
Clin Microbiol Rev. 2015 Apr;28(2):337-418. doi: 10.1128/CMR.00117-14.
6
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Tools for characterizing bacterial protein synthesis inhibitors.用于表征细菌蛋白质合成抑制剂的工具。
Antimicrob Agents Chemother. 2013 Dec;57(12):5994-6004. doi: 10.1128/AAC.01673-13. Epub 2013 Sep 16.
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