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Nusbiarylins Inhibit Transcription and Target Virulence Factors in Bacterial Pathogen Staphylococcus aureus

Chu, Adrian Jun ; Qiu, Yangyi ; Harper, Rachel ; Lin, Lin ; Ma, Cong ; Yang, Xiao

International journal of molecular sciences, 2020-08, Vol.21 (16), p.5772 [Periódico revisado por pares]

Switzerland: MDPI AG

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Nusbiarylins Inhibit Transcription and Target Virulence Factors in Bacterial Pathogen Staphylococcus aureus
Autor: Chu, Adrian Jun ; Qiu, Yangyi ; Harper, Rachel ; Lin, Lin ; Ma, Cong ; Yang, Xiao
Assuntos: Adenosine Triphosphate - biosynthesis ; Animals ; Anti-Bacterial Agents - chemistry ; Anti-Bacterial Agents - pharmacokinetics ; Anti-Bacterial Agents - pharmacology ; antibiotic ; antimicrobial agent ; Antimicrobial agents ; Bacteria ; Bacterial Proteins - metabolism ; Drug development ; drug discovery ; Erythrocytes - drug effects ; Exotoxins - metabolism ; Gene expression ; Gene Expression Regulation, Bacterial - drug effects ; Genes, Essential ; Hemolysis - drug effects ; Kinases ; Kinetics ; Leukocidin ; Metabolism ; Methicillin ; Microbial Sensitivity Tests ; MRSA ; Multidrug resistance ; nusbiarylin ; Pathogenesis ; Pathogens ; Proteins ; Rabbits ; Rifampin - pharmacology ; RNA polymerase ; Staphylococcus aureus ; Staphylococcus aureus - drug effects ; Staphylococcus aureus - genetics ; Staphylococcus aureus - pathogenicity ; Staphylococcus infections ; Time Factors ; Toxins ; Transcription factors ; Transcription, Genetic - drug effects ; Virulence ; Virulence - drug effects ; Virulence - genetics ; Virulence factors ; Virulence Factors - metabolism ; α-Toxin
É parte de: International journal of molecular sciences, 2020-08, Vol.21 (16), p.5772
Descrição: The emergence of multidrug resistance in the clinically significant pathogen is a global health burden, compounded by a diminishing drug development pipeline, and a lack of approved novel antimicrobials. Our previously reported first-in-class bacterial transcription inhibitors "nusbiarylins" presented a promising prospect towards the discovery of novel antimicrobial agents with a novel mechanism. Here we investigated and characterised the lead nusbiarylin compound, MC4, and several of its chemical derivatives in both methicillin-resistant (MRSA) and the type strains, demonstrating their capacity for the arrest of growth and cellular respiration, impairment of RNA and intracellular protein levels at subinhibitory concentrations. In some instances, derivatives of MC4 were also shown to attenuate the production of staphylococcal virulence factors in vitro, such as the exoproteins α-toxin and Panton-Valentine Leukocidin (PVL). Trends observed from quantitative PCR assays suggested that nusbiarylins elicited these effects possibly by acting via but not limited to the modulation of global regulatory pathways, such as the regulon, which coordinates the expression of genes associated with virulence. Our findings encourage the continued development of more potent compounds within this novel family of bacterial transcription inhibitors.
Editor: Switzerland: MDPI AG
Idioma: Inglês

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Nusbiarylins Inhibit Transcription and Target Virulence Factors in Bacterial Pathogen Staphylococcus aureus

Chu, Adrian Jun ; Qiu, Yangyi ; Harper, Rachel ; Lin, Lin ; Ma, Cong ; Yang, Xiao

Switzerland: MDPI AG

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