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Extensively drug-resistant tuberculosis.广泛耐药结核病
Curr Opin Infect Dis. 2009 Apr;22(2):167-73. doi: 10.1097/qco.0b013e3283229fab.
2
Probing of the cis-5-phenyl proline scaffold as a platform for the synthesis of mechanism-based inhibitors of the Staphylococcus aureus sortase SrtA isoform.探索顺式-5-苯基脯氨酸支架作为合成金黄色葡萄球菌分选酶SrtA亚型基于机制的抑制剂的平台。
Bioorg Med Chem. 2009 Apr 1;17(7):2886-93. doi: 10.1016/j.bmc.2009.02.008. Epub 2009 Feb 13.
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Type II fatty acid synthesis is not a suitable antibiotic target for Gram-positive pathogens.II型脂肪酸合成不是革兰氏阳性病原体合适的抗生素靶点。
Nature. 2009 Mar 5;458(7234):83-6. doi: 10.1038/nature07772.
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Inhibitory effect of REP3123 on toxin and spore formation in Clostridium difficile, and in vivo efficacy in a hamster gastrointestinal infection model.REP3123对艰难梭菌毒素和孢子形成的抑制作用以及在仓鼠胃肠道感染模型中的体内疗效。
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Inhibition of Acinetobacter baumannii, Staphylococcus aureus and Pseudomonas aeruginosa biofilm formation with a class of TAGE-triazole conjugates.一类TAGE-三唑共轭物对鲍曼不动杆菌、金黄色葡萄球菌和铜绿假单胞菌生物膜形成的抑制作用
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Staphylococcus aureus: a community pathogen.金黄色葡萄球菌:一种社区病原体。
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Inhibition of Lux quorum-sensing system by synthetic N-acyl-L-homoserine lactone analogous.合成的N-酰基-L-高丝氨酸内酯类似物对Lux群体感应系统的抑制作用
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An inhibitor of gram-negative bacterial virulence protein secretion.一种革兰氏阴性菌毒力蛋白分泌抑制剂。
Cell Host Microbe. 2008 Oct 16;4(4):325-36. doi: 10.1016/j.chom.2008.08.001.
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Targeting virulence traits: potential strategies to combat extraintestinal pathogenic E. coli infections.靶向毒力特性:对抗肠外致病性大肠杆菌感染的潜在策略。
Curr Opin Microbiol. 2008 Oct;11(5):409-13. doi: 10.1016/j.mib.2008.09.005. Epub 2008 Oct 14.
10
Brominated furanones inhibit biofilm formation by Salmonella enterica serovar Typhimurium.溴化呋喃酮可抑制鼠伤寒沙门氏菌生物膜的形成。
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针对毒力的抗菌药物研发的有效步骤。

Productive steps toward an antimicrobial targeting virulence.

作者信息

Barczak Amy K, Hung Deborah T

机构信息

Division of Infectious Diseases, Massachusetts General Hospital, 55 Fruit St., Boston, MA 02114, USA.

出版信息

Curr Opin Microbiol. 2009 Oct;12(5):490-6. doi: 10.1016/j.mib.2009.06.012. Epub 2009 Jul 22.

DOI:10.1016/j.mib.2009.06.012
PMID:19631578
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2763366/
Abstract

Targeting virulence factors has gained increasing attention as a potential approach to new antibiotics. Small molecule inhibitors of virulence have been shown to change the course of disease in whole organism infection models. Recently, key advances in the field include the identification of novel targets within cell signaling pathways, a new class of anti-virulence compounds that target bacterial defenses against host immunity, and a growing body of in vivo data to support the general approach of anti-virulence therapies. Additionally, there has been a distinct trend toward developing broader spectrum anti-virulence compounds, in particular agents with activity against diverse Gram-negative organisms. Herein we provide an update on the status of the field with a focus on recent advancements.

摘要

靶向毒力因子作为开发新型抗生素的一种潜在方法,已越来越受到关注。毒力小分子抑制剂已被证明可在整体生物感染模型中改变疾病进程。最近,该领域的关键进展包括在细胞信号通路中鉴定出新的靶点、一类针对细菌抵御宿主免疫的新型抗毒力化合物,以及越来越多的体内数据支持抗毒力疗法的总体方法。此外,开发更广泛谱的抗毒力化合物,特别是对多种革兰氏阴性菌有活性的药物,已成为一种明显的趋势。在此,我们重点介绍该领域的最新进展,以提供该领域现状的最新情况。