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THCz : Small molecules with antimicrobial activity that block cell wall lipid intermediates
- Reithuber, Elisabeth (author)
-
- Wixe, Torbjörn (author)
- Umeå universitet,Kemiska institutionen
- Ludwig, Kevin C. (author)
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- Muller, Anna (author)
- Grein, Fabian (author)
- Nannapaneni, Priyanka (author)
- Schneider, Tanja (author)
- Normark, Staffan (author)
- Mellroth, Peter (author)
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- (creator_code:org_t)
- 2021-11-16
- 2021
- English.
- In: Proceedings of the National Academy of Sciences of the United States of America. - : National Academy of Sciences of the United States of America. - 0027-8424 .- 1091-6490. ; 118:47
- Journal article (peer-reviewed)
Abstract
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- Emerging antibiotic resistance demands identification of novel antibacterial compound classes. A bacterial whole-cell screen based on pneumococcal autolysin-mediated lysis induction was developed to identify potential bacterial cell wall synthesis inhibitors. A hit class comprising a 1-amino substituted tetrahydrocarbazole (THCz) scaffold, containing two essential amine groups, displayed bactericidal activity against a broad range of gram-positive and selected gram-negative pathogens in the low micromolar range. Mode of action studies revealed that THCz inhibit cell envelope synthesis by targeting undecaprenyl pyrophosphate-containing lipid intermediates and thus simultaneously inhibit peptidoglycan, teichoic acid, and polysaccharide capsule biosynthesis. Resistance did not readily develop in vitro, and the ease of synthesizing and modifying these small molecules, as compared to natural lipid II-binding antibiotics, makes THCz promising scaffolds for development of cell wall-targeting antimicrobials.
Subject headings
- NATURVETENSKAP -- Biologi -- Mikrobiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Microbiology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Mikrobiologi inom det medicinska området (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Microbiology in the medical area (hsv//eng)
Keyword
- Streptococcus pneumoniae
- antibiotic resistance
- antimicrobials
- cell wall biosynthesis
- tetrahydrocarbazole
Publication and Content Type
- ref (subject category)
- art (subject category)
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