Targeting Gene Transcription Prevents Antibiotic Resistance

Innovative strategies are needed to curb the global health challenge of antibiotic resistance. The World Health Organization predicts that antibiotic resistance could lead to millions of deaths annually. Pharmaceutical experience has shown that modest alterations of commonly-used broad-spectrum anti...

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Main Author: Paul F. Agris
Format: Article
Language:English
Published: MDPI AG 2025-03-01
Series:Antibiotics
Subjects:
Online Access:https://www.mdpi.com/2079-6382/14/4/345
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author Paul F. Agris
author_facet Paul F. Agris
author_sort Paul F. Agris
collection DOAJ
description Innovative strategies are needed to curb the global health challenge of antibiotic resistance. The World Health Organization predicts that antibiotic resistance could lead to millions of deaths annually. Pharmaceutical experience has shown that modest alterations of commonly-used broad-spectrum antibiotics readily elicit resistant strains. Thus, continued simple iterative improvements on current antibiotics are not sustainable. Traditional strategies target single sites with the goal of a broad-spectrum antibiotic. In comparison, a novel strategy targets multiple sites in single- or multidrug-resistant Gram-positive bacterial pathogens. The objective is to exploit the mechanisms by which pathogenic bacteria require genes for transcriptional regulation. Transcription regulatory factors can be manipulated and their functions disrupted to hamper bacterial viability. Some transcription factors regulate one or more steps in metabolic pathways. Transcription factors are not always proteins; some are small-molecule metabolites triggering genetic functions through riboswitches, and others are RNAs. Novel agents have been discovered with computer-simulated docking to an unusual transcription regulatory site in nascent bacterial mRNA. These compounds exhibit innovative chemistries and modes of action that inhibit bacterial growth by binding to and blocking critical Gram-positive mRNA functions. The tRNA-dependent transcription regulation of amino acid metabolism illustrates the possibilities of novel strategies to inhibit antibiotic-resistant growth and thwart the emergence of novel resistant strains.
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spelling doaj-art-905bac9a834f4e8eaf4e9613f33ccf492025-08-20T02:28:40ZengMDPI AGAntibiotics2079-63822025-03-0114434510.3390/antibiotics14040345Targeting Gene Transcription Prevents Antibiotic ResistancePaul F. Agris0Department of Medicine, Duke University School of Medicine, Durham, NC 27710, USAInnovative strategies are needed to curb the global health challenge of antibiotic resistance. The World Health Organization predicts that antibiotic resistance could lead to millions of deaths annually. Pharmaceutical experience has shown that modest alterations of commonly-used broad-spectrum antibiotics readily elicit resistant strains. Thus, continued simple iterative improvements on current antibiotics are not sustainable. Traditional strategies target single sites with the goal of a broad-spectrum antibiotic. In comparison, a novel strategy targets multiple sites in single- or multidrug-resistant Gram-positive bacterial pathogens. The objective is to exploit the mechanisms by which pathogenic bacteria require genes for transcriptional regulation. Transcription regulatory factors can be manipulated and their functions disrupted to hamper bacterial viability. Some transcription factors regulate one or more steps in metabolic pathways. Transcription factors are not always proteins; some are small-molecule metabolites triggering genetic functions through riboswitches, and others are RNAs. Novel agents have been discovered with computer-simulated docking to an unusual transcription regulatory site in nascent bacterial mRNA. These compounds exhibit innovative chemistries and modes of action that inhibit bacterial growth by binding to and blocking critical Gram-positive mRNA functions. The tRNA-dependent transcription regulation of amino acid metabolism illustrates the possibilities of novel strategies to inhibit antibiotic-resistant growth and thwart the emergence of novel resistant strains.https://www.mdpi.com/2079-6382/14/4/345antibiotic resistancediscovery strategynovel mRNA targetmulti-targeting
spellingShingle Paul F. Agris
Targeting Gene Transcription Prevents Antibiotic Resistance
Antibiotics
antibiotic resistance
discovery strategy
novel mRNA target
multi-targeting
title Targeting Gene Transcription Prevents Antibiotic Resistance
title_full Targeting Gene Transcription Prevents Antibiotic Resistance
title_fullStr Targeting Gene Transcription Prevents Antibiotic Resistance
title_full_unstemmed Targeting Gene Transcription Prevents Antibiotic Resistance
title_short Targeting Gene Transcription Prevents Antibiotic Resistance
title_sort targeting gene transcription prevents antibiotic resistance
topic antibiotic resistance
discovery strategy
novel mRNA target
multi-targeting
url https://www.mdpi.com/2079-6382/14/4/345
work_keys_str_mv AT paulfagris targetinggenetranscriptionpreventsantibioticresistance