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QcrB in Mycobacterium tuberculosis: The new drug target of antitubercular agents.结核分枝杆菌中的 QcrB:抗结核药物的新靶标。
Med Res Rev. 2021 Jul;41(4):2565-2581. doi: 10.1002/med.21779. Epub 2021 Jan 5.
2
Terminal Respiratory Oxidases: A Targetables Vulnerability of Mycobacterial Bioenergetics?终端呼吸氧化酶:分枝杆菌生物能量学的可靶向弱点?
Front Cell Infect Microbiol. 2020 Nov 23;10:589318. doi: 10.3389/fcimb.2020.589318. eCollection 2020.
3
Dual inhibition of the terminal oxidases eradicates antibiotic-tolerant Mycobacterium tuberculosis.双重抑制末端氧化酶可根除耐抗生素结核分枝杆菌。
EMBO Mol Med. 2021 Jan 11;13(1):e13207. doi: 10.15252/emmm.202013207. Epub 2020 Dec 7.
4
Comprehensive Host Cell-Based Screening Assays for Identification of Anti-Virulence Drugs Targeting and Typhimurium.用于鉴定靶向鼠伤寒沙门氏菌毒力的抗毒力药物的基于宿主细胞的综合筛选试验
Microorganisms. 2020 Jul 22;8(8):1096. doi: 10.3390/microorganisms8081096.
5
Telacebec (Q203), a New Antituberculosis Agent.替拉塞贝克(Q203),一种新型抗结核药物。
N Engl J Med. 2020 Mar 26;382(13):1280-1281. doi: 10.1056/NEJMc1913327.
6
Identification of 4-Amino-Thieno[2,3-]Pyrimidines as QcrB Inhibitors in Mycobacterium tuberculosis.鉴定结核分枝杆菌中的 QcrB 抑制剂 4-氨基噻吩并[2,3-d]嘧啶。
mSphere. 2019 Sep 11;4(5):e00606-19. doi: 10.1128/mSphere.00606-19.
7
Extremely Low Hit Rate in a Diverse Chemical Drug Screen Targeting Mycobacterium abscessus.针对脓肿分枝杆菌的多样化化学药物筛选中极低的命中率
Antimicrob Agents Chemother. 2019 Oct 22;63(11). doi: 10.1128/AAC.01008-19. Print 2019 Nov.
8
Pyrazolo[1,5- a]pyridine Inhibitor of the Respiratory Cytochrome bcc Complex for the Treatment of Drug-Resistant Tuberculosis.用于治疗耐药结核病的呼吸细胞色素bcc复合物的吡唑并[1,5-a]吡啶抑制剂
ACS Infect Dis. 2019 Feb 8;5(2):239-249. doi: 10.1021/acsinfecdis.8b00225. Epub 2018 Dec 11.
9
No Evidence for Acquired Mutations Associated with Cytochrome Inhibitor Resistance in 13,559 Clinical Mycobacterium tuberculosis Complex Isolates.在13559株临床结核分枝杆菌复合群分离株中,无证据表明存在与细胞色素抑制剂耐药相关的获得性突变。
Antimicrob Agents Chemother. 2018 Dec 21;63(1). doi: 10.1128/AAC.01317-18. Print 2019 Jan.
10
Exploiting the synthetic lethality between terminal respiratory oxidases to kill and clear host infection.利用末端呼吸氧化酶之间的合成致死性来杀死和清除宿主感染。
Proc Natl Acad Sci U S A. 2017 Jul 11;114(28):7426-7431. doi: 10.1073/pnas.1706139114. Epub 2017 Jun 26.

鉴定两种新型结核分枝杆菌细胞色素复合物抑制剂。

Characterization of Two Novel Inhibitors of the Mycobacterium tuberculosis Cytochrome Complex.

机构信息

Department I of Internal Medicine, Medical Faculty and University Hospital Cologne, University of Cologne, Cologne, Germany.

Center for Molecular Medicine Cologne (CMMC), University of Cologne, Cologne, Germany.

出版信息

Antimicrob Agents Chemother. 2023 Jul 18;67(7):e0025123. doi: 10.1128/aac.00251-23. Epub 2023 Jun 26.

DOI:10.1128/aac.00251-23
PMID:37358461
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10353358/
Abstract

Drug-resistant tuberculosis is a global health care threat calling for novel effective treatment options. Here, we report on two novel cytochrome inhibitors (MJ-22 and B6) targeting the Mycobacterium tuberculosis respiratory chain with excellent intracellular activities in human macrophages. Both hit compounds revealed very low mutation frequencies and distinct cross-resistance patterns with other advanced cytochrome inhibitors.

摘要

耐多药结核病是一种全球卫生保健威胁,需要新型有效的治疗选择。在这里,我们报告了两种新型细胞色素 抑制剂(MJ-22 和 B6),它们针对分枝杆菌呼吸链,在人巨噬细胞中有极好的细胞内活性。这两种命中化合物显示出非常低的突变频率和与其他先进的细胞色素 抑制剂的不同交叉耐药模式。