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Antimicrob Agents Chemother. 1996 Feb;40(2):473-6. doi: 10.1128/AAC.40.2.473.
2
The interaction between coumarin drugs and DNA gyrase.香豆素类药物与DNA回旋酶之间的相互作用。
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4
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5
Mechanism of inhibition of DNA gyrase by cyclothialidine, a novel DNA gyrase inhibitor.新型DNA回旋酶抑制剂环硫噻吨抑制DNA回旋酶的机制
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Characterization of the binding site for cyclothialidine on the B subunit of DNA gyrase.环噻硫腙在DNA促旋酶B亚基上结合位点的表征
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The high-resolution crystal structure of a 24-kDa gyrase B fragment from E. coli complexed with one of the most potent coumarin inhibitors, clorobiocin.来自大肠杆菌的一个24千道尔顿的促旋酶B片段与最有效的香豆素抑制剂之一氯新生霉素复合后的高分辨率晶体结构。
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Discoordinate gene expression of gyrA and gyrB in response to DNA gyrase inhibition in Escherichia coli.大肠杆菌中gyrA和gyrB基因表达失调以响应DNA回旋酶抑制作用。
J Basic Microbiol. 1997;37(1):53-69. doi: 10.1002/jobm.3620370109.
10
DNA gyrase activities from Rhodobacter capsulatus: analysis of target(s) of coumarins and cloning of the gyrB locus.荚膜红细菌的DNA促旋酶活性：香豆素作用靶点分析及gyrB基因座的克隆
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Exploiting bacterial DNA gyrase as a drug target: current state and perspectives.利用细菌 DNA 拓扑异构酶作为药物靶点：现状与展望。
Appl Microbiol Biotechnol. 2011 Nov;92(3):479-97. doi: 10.1007/s00253-011-3557-z. Epub 2011 Sep 9.
2
Gene expression changes triggered by exposure of Haemophilus influenzae to novobiocin or ciprofloxacin: combined transcription and translation analysis.流感嗜血杆菌暴露于新生霉素或环丙沙星引发的基因表达变化：转录与翻译联合分析
Genome Res. 2001 Jan;11(1):28-42. doi: 10.1101/gr.157701.

本文引用的文献

1
Clerocidin, a terpenoid antibiotic, inhibits bacterial DNA gyrase.clerocidin是一种萜类抗生素，可抑制细菌DNA回旋酶。
J Antibiot (Tokyo). 1993 Mar;46(3):526-30. doi: 10.7164/antibiotics.46.526.
2
The 43-kilodalton N-terminal fragment of the DNA gyrase B protein hydrolyzes ATP and binds coumarin drugs.DNA 回旋酶 B 蛋白的 43 千道尔顿 N 端片段可水解 ATP 并结合香豆素类药物。
Biochemistry. 1993 Mar 16;32(10):2717-24. doi: 10.1021/bi00061a033.
3
The interaction between coumarin drugs and DNA gyrase.香豆素类药物与DNA回旋酶之间的相互作用。
Mol Microbiol. 1993 Aug;9(4):681-6. doi: 10.1111/j.1365-2958.1993.tb01728.x.
4
Biological characterization of cyclothialidine, a new DNA gyrase inhibitor.新型DNA回旋酶抑制剂环噻硫腚的生物学特性
Antimicrob Agents Chemother. 1993 Dec;37(12):2656-61. doi: 10.1128/AAC.37.12.2656.
5
The 24 kDa N-terminal sub-domain of the DNA gyrase B protein binds coumarin drugs.
Mol Microbiol. 1994 May;12(3):365-73. doi: 10.1111/j.1365-2958.1994.tb01026.x.
6
Crystallization of inhibitor complexes of an N-terminal 24 kDa fragment of the DNA gyrase B protein.DNA 解旋酶 B 蛋白 N 端 24 kDa 片段抑制剂复合物的结晶
J Mol Biol. 1994 Aug 5;241(1):128-30. doi: 10.1006/jmbi.1994.1480.
7
Cyclothialidine and its congeners: a new class of DNA gyrase inhibitors.环硫噻吨及其同系物：一类新型的DNA回旋酶抑制剂。
Pharmacol Ther. 1993 Nov;60(2):367-80. doi: 10.1016/0163-7258(93)90017-8.
8
Mechanism of inhibition of DNA gyrase by cyclothialidine, a novel DNA gyrase inhibitor.新型DNA回旋酶抑制剂环硫噻吨抑制DNA回旋酶的机制
Antimicrob Agents Chemother. 1994 Sep;38(9):1966-73. doi: 10.1128/AAC.38.9.1966.
9
Nucleotide binding to the 43-kilodalton N-terminal fragment of the DNA gyrase B protein.核苷酸与DNA促旋酶B蛋白43千道尔顿N端片段的结合。
Biochemistry. 1995 Aug 1;34(30):9801-8. doi: 10.1021/bi00030a018.
10
DNA gyrase: affinity chromatography on novobiocin-Sepharose and catalytic properties.DNA 回旋酶：新生霉素 - 琼脂糖亲和层析及催化特性
Nucleic Acids Res. 1981 Aug 11;9(15):3589-603. doi: 10.1093/nar/9.15.3589.

新型细菌DNA回旋酶抑制剂GR122222X的作用模式

Mode of action of GR122222X, a novel inhibitor of bacterial DNA gyrase.

作者信息

Oram M, Dosanjh B, Gormley N A, Smith C V, Fisher L M, Maxwell A, Duncan K

机构信息

Department of Cellular and Molecular Sciences, University of London, United Kingdom.

出版信息

Antimicrob Agents Chemother. 1996 Feb;40(2):473-6. doi: 10.1128/AAC.40.2.473.

DOI:10.1128/AAC.40.2.473
PMID:8834902
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC163138/
Abstract

GR122222X is a potent inhibitor of the supercoiling reaction of bacterial DNA gyrase. We show that this compound binds stoichiometrically to inactivate the ATPase activity of a 43-kDa N-terminal fragment of the B subunit and competitively inhibits the binding of a radiolabelled coumarin drug to N-terminal fragments of GyrB. These and other data suggest that GR122222X has a mode of action similar, but not identical, to that of coumarin antibiotics.

摘要

GR122222X是细菌DNA促旋酶超螺旋反应的强效抑制剂。我们发现该化合物以化学计量方式结合，使B亚基43 kDa N端片段的ATP酶活性失活，并竞争性抑制放射性标记香豆素药物与GyrB N端片段的结合。这些及其他数据表明，GR122222X的作用模式与香豆素类抗生素相似，但并不完全相同。