ArticleJournal of medicinal chemistry2013
X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins.
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
26 citing papers in PubMed.
- Structural basis for the unexpected activity of rifamycin B against rifampicin-resistant RNA polymerase.bioRxiv : the preprint server for biology · 2026Article
- Late-Stage Functionalization of the Rifamycin Core via Click Chemistry Toward New Antibacterial Derivatives.Molecules (Basel, Switzerland) · 2026Article
- New Structure Activity Relationship Insight into the Role of the C-3 Extension on Rifamycin Antimycobacterial Activity.ChemMedChem · 2025Article
- Deciphering the Impact of Temperature on Pleiotropic Consequences of RNA Polymerase Mutations.Molecular biology and evolution · 2025Article
- Assessment of lecithin nanoliposomes addition to fresh low-density lipoprotein-based diluent for cold storage of ram semen.Iranian journal of veterinary research · 2025Article
- Amino acid substitutions in the region between RpoB clusters II and III on rifampin susceptibility in Haemophilus influenzae.European journal of clinical microbiology & infectious diseases : official publication of the European Society of Clinical Microbiology · 2023Article
- Pervasive genotype-by-environment interactions shape the fitness effects of antibiotic resistance mutations.Proceedings. Biological sciences · 2023Article
- Going Retro, Going Viral: Experiences and Lessons in Drug Discovery from COVID-19.Molecules (Basel, Switzerland) · 2022Article
- Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.Journal of medicinal chemistry · 2022Article
- Universal functions of the σ finger in alternative σ factors during transcription initiation by bacterial RNA polymerase.RNA biology · 2021Article
- Article
- Molecular basis for RNA polymerase-dependent transcription complex recycling by the helicase-like motor protein HelD.Nature communications · 2020Article
- Rewiring of growth-dependent transcription regulation by a point mutation in region 1.1 of the housekeeping σ factor.Nucleic acids research · 2020Article
- Inhibition of RNA Polymerase by Rifampicin and Rifamycin-Like Molecules.EcoSal Plus · 2020Article
- Review
- Structural Basis of Mycobacterium tuberculosis Transcription and Transcription Inhibition.Molecular cell · 2017Article
- Novel Chemical Scaffolds for Inhibition of Rifamycin-Resistant RNA Polymerase Discovered from High-Throughput Screening.SLAS discovery : advancing life sciences R & D · 2017Article
- Structural basis for rifamycin resistance of bacterial RNA polymerase by the three most clinically important RpoB mutations found in Mycobacterium tuberculosis.Molecular microbiology · 2017Article
- Rifamycin Resistance in Clostridium difficile Is Generally Associated with a Low Fitness Burden.Antimicrobial agents and chemotherapy · 2016Article
- Bacterial Transcription as a Target for Antibacterial Drug Development.Microbiology and molecular biology reviews : MMBR · 2016Review
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
Rifampin, a semisynthetic rifamycin, is the cornerstone of current tuberculosis treatment. Among many semisynthetic rifamycins, benzoxazinorifamycins have great potential for TB treatment due to their superior affinity for wild-type and rifampin-resistant Mycobacterium tuberculosis RNA polymerases and their reduced hepatic Cyp450 induction activity. In this study, we have determined the crystal structures of the Escherichia coli RNA polymerase complexes with two benzoxazinorifamycins. The ansa-naphthalene moieties of the benzoxazinorifamycins bind in a deep pocket of the β subunit, blocking the path of the RNA transcript. The C3'-tail of benzoxazinorifamycin fits a cavity between the β subunit and σ factor. We propose that in addition to blocking RNA exit, the benzoxazinorifamycin C3'-tail changes the σ region 3.2 loop position, which influences the template DNA at the active site, thereby reducing the efficiency of transcription initiation. This study supports expansion of structure-activity relationships of benzoxazinorifamycins inhibition of RNA polymerase toward uncovering superior analogues with development potential.
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