Synthesis and biological evaluation of novel N-2,4-dimethoxyphenyl dithiolopyrrolone derivatives as bacterial RNA polymerase inhibitors
Sign Up to like & getrecommendations! Published in 2020 at "Medicinal Chemistry Research"
DOI: 10.1007/s00044-020-02550-3
Abstract: Eighteen novel N-2,4-dimethoxyphenyl dithiolopyrrolone derivatives inhibiting bacterial RNA polymerase (RNAP) were synthesized based on dithiolopyrrolone scaffold. Some compounds displayed potent antimicrobial activity against Gram-positive bacteria of Staphylococcus aureus and Streptococcus pneumoniae, but not the Gram-negative… read more here.
Keywords: dithiolopyrrolone; bacterial rna; rna polymerase; dithiolopyrrolone derivatives ... See more keywords
Antibacterial Nucleoside-Analog Inhibitor of Bacterial RNA Polymerase
Sign Up to like & getrecommendations! Published in 2017 at "Cell"
DOI: 10.1016/j.cell.2017.05.042
Abstract: Drug-resistant bacterial pathogens pose an urgent public-health crisis. Here, we report the discovery, from microbial-extract screening, of a nucleoside-analog inhibitor that inhibits bacterial RNA polymerase (RNAP) and exhibits antibacterial activity against drug-resistant bacterial pathogens: pseudouridimycin (PUM).… read more here.
Keywords: inhibitor; bacterial rna; rna polymerase; nucleoside analog ... See more keywords
Systematic probing of the bacterial RNA structurome to reveal new functions.
Sign Up to like & getrecommendations! Published in 2017 at "Current opinion in microbiology"
DOI: 10.1016/j.mib.2017.01.003
Abstract: RNA folds into intricate structures. Recent discoveries using next-generation sequencing (NGS) approaches have revealed unprecedented structural complexity with a pivotal role in regulating RNA function and stability. Here, we present new discoveries from the transcriptome-wide… read more here.
Keywords: systematic probing; bacterial rna; rna; structurome reveal ... See more keywords
Evaluation of Bacterial RNA Polymerase Inhibitors in a Staphylococcus aureus-based Wound-Infection Model in SKH1 Mice.
Sign Up to like & getrecommendations! Published in 2020 at "ACS infectious diseases"
DOI: 10.1021/acsinfecdis.0c00034
Abstract: Chronic wounds infected with pathogens such as Staphylococcus aureus represent a worldwide health concern, especially in patients with a compromised immune system. As antimicrobial resistance has become an immense global problem, novel antibiotics are urgently… read more here.
Keywords: staphylococcus aureus; infection model; bacterial rna; rna polymerase ... See more keywords
Mechanisms of antibiotics inhibiting bacterial RNA polymerase.
Sign Up to like & getrecommendations! Published in 2019 at "Biochemical Society transactions"
DOI: 10.1042/bst20180499
Abstract: Transcription, the first phase of gene expression, is performed by the multi-subunit RNA polymerase (RNAP). Bacterial RNAP is a validated target for clinical antibiotics. Many natural and synthetic compounds are now known to target RNAP,… read more here.
Keywords: antibiotics inhibiting; mechanisms antibiotics; bacterial rna; polymerase ... See more keywords
Structural Insights into the Role of Pseudouridimycin Binding in Disruption of Bacterial RNA Polymerase Bridge Helix Conformational Arrangement.
Sign Up to like & getrecommendations! Published in 2022 at "Current pharmaceutical biotechnology"
DOI: 10.2174/1389201023666220511211433
Abstract: BACKGROUND The bridge helix (BH) is a crucial region involved in bacterial RNA polymerase (RNAP) catalysis. It plays an essential role in the nucleotide addition cycle (NAC) by performing many modulated rearrangements and conformational changes.… read more here.
Keywords: role; bacterial rna; bridge helix; pum ... See more keywords
An Optimized Workflow for the Discovery of New Antimicrobial Compounds Targeting Bacterial RNA Polymerase Complex Formation
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DOI: 10.3390/antibiotics11101449
Abstract: Bacterial resistance represents a major health problem worldwide and there is an urgent need to develop first-in-class compounds directed against new therapeutic targets. We previously developed a drug-discovery platform to identify new antimicrobials able to… read more here.
Keywords: rna polymerase; rna; bacterial rna; optimized workflow ... See more keywords
First-In-Class Inhibitors Targeting the Interaction between Bacterial RNA Polymerase and Sigma Initiation Factor Affect the Viability and Toxin Release of Streptococcus pneumoniae
Sign Up to like & getrecommendations! Published in 2019 at "Molecules"
DOI: 10.3390/molecules24162902
Abstract: Novel antimicrobial classes are in desperate need for clinical management of infections caused by increasingly prevalent multi-drug resistant pathogens. The protein-protein interaction between bacterial RNA polymerase (RNAP) and the housekeeping sigma initiation factor is essential… read more here.
Keywords: interaction bacterial; bacterial rna; rna polymerase; initiation factor ... See more keywords