ArticleThe EMBO journal2010
The transcription inhibitor lipiarmycin blocks DNA fitting into the RNA polymerase catalytic site.
Article in The EMBO journal, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
35 citing papers in PubMed, 75 citations in OpenAlex.
- Minimal Computational Framework for Systematic Identification of Antimicrobial Targets.bioRxiv : the preprint server for biology · 2026Article
- Single-stranded DNA drives σ subunit loading onto mycobacterial RNA polymerase to unlock initiation-competent conformations.Nucleic acids research · 2025Article
- Inhibition of bacterial RNA polymerase function and protein-protein interactions: a promising approach for next-generation antibacterial therapeutics.RSC medicinal chemistry · 2024Review
- 6S RNA-Dependent Susceptibility to RNA Polymerase Inhibitors.Antimicrobial agents and chemotherapy · 2022Article
- Article
- Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation.ACS medicinal chemistry letters · 2020Article
- Ureidothiophene inhibits interaction of bacterial RNA polymerase with -10 promotor element.Nucleic acids research · 2020Article
- Oxazinomycin arrests RNA polymerase at the polythymidine sequences.Nucleic acids research · 2019Article
- Mode of Action of Kanglemycin A, an Ansamycin Natural Product that Is Active against Rifampicin-Resistant Mycobacterium tuberculosis.Molecular cell · 2018Article
- Structure-function comparisons of (p)ppApp vs (p)ppGpp for Escherichia coli RNA polymerase binding sites and for rrnB P1 promoter regulatory responses in vitro.Biochimica et biophysica acta. Gene regulatory mechanisms · 2018Article
- Single-molecule analysis reveals the mechanism of transcription activation inScience advances · 2018Article
- Structural Basis of Transcription Inhibition by Fidaxomicin (Lipiarmycin A3).Molecular cell · 2018Article
- Fidaxomicin jamseLife · 2018Article
- A Thermus phage protein inhibits host RNA polymerase by preventing template DNA strand loading during open promoter complex formation.Nucleic acids research · 2018Article
- Fidaxomicin and OP-1118 Inhibit Clostridium difficile Toxin A- and B-Mediated Inflammatory Responses via Inhibition of NF-κB Activity.Antimicrobial agents and chemotherapy · 2018Article
- RNA polymerase motions during promoter melting.Science (New York, N.Y.) · 2017Article
- A Novel Spiro-Heterocyclic Compound Identified by the Silkworm Infection Model Inhibits Transcription inFrontiers in microbiology · 2017Article
- Bacterial Transcription as a Target for Antibacterial Drug Development.Microbiology and molecular biology reviews : MMBR · 2016Review
- Bacterial RNA Polymerase-DNA Interaction-The Driving Force of Gene Expression and the Target for Drug Action.Frontiers in molecular biosciences · 2016Review
- Initial events in bacterial transcription initiation.Biomolecules · 2015Review
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Worldwide spreading of drug-resistant pathogens makes mechanistic understanding of antibiotic action an urgent task. The macrocyclic antibiotic lipiarmycin (Lpm), which is under development for clinical use, inhibits bacterial RNA polymerase (RNAP) by an unknown mechanism. Using genetic and biochemical approaches, we show that Lpm targets the sigma(70) subunit region 3.2 and the RNAP beta' subunit switch-2 element, which controls the clamping of promoter DNA in the RNAP active-site cleft. Lpm abolishes isomerization of the 'closed'-promoter complex to the transcriptionally competent 'open' complex and blocks sigma(70)-stimulated RNA synthesis on promoter-less DNA templates. Lpm activity decreases when the template DNA strand is stabilized at the active site through the interaction of RNAP with the nascent RNA chain. Template DNA-strand fitting into the RNAP active-site cleft directed by the beta' subunit switch-2 element and the sigma(70) subunit region 3.2 is essential for promoter melting and for de novo initiation of RNA synthesis, and our results suggest that Lpm impedes this process.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.