ArticleProceedings of the National Academy of Sciences of the United States of America2013
Identification of a small molecule with activity against drug-resistant and persistent tuberculosis.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 98 papers.
What it found
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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.
The trial behind it
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
98 citing papers in PubMed, 226 citations in OpenAlex.
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- Mechanism of the M. tuberculosis DprE1-DprE2 epimerase complex and inhibition by anti-tubercular drugs.Nature chemical biology · 2026Article
- Biofilm Associated Persistence and Drug Tolerance in Mycobacteria Within Host Microenvironments.APMIS : acta pathologica, microbiologica, et immunologica Scandinavica · 2026Review
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- Scaffold Hopping in Tuberculosis Drug Discovery: Principles, Applications, and Case Studies.Journal of medicinal chemistry · 2025Review
- Bibliometric and Visualization Analysis of DprE1 Inhibitors to Combat Tuberculosis.Drug design, development and therapy · 2025Article
- Novel hybrids of 1,2,3-triazole-benzoxazole: design, synthesis, and assessment of DprE1 enzyme inhibitors using fluorometric assay and computational analysis.Journal of enzyme inhibition and medicinal chemistry · 2024Article
- The conserved σD envelope stress response monitors multiple aspects of envelope integrity in corynebacteria.PLoS genetics · 2024Article
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- 3,5-disubstituted pyridines with potent activity against drug-resistantFuture medicinal chemistry · 2024Article
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- Discovery of pyrimidine-tethered benzothiazole derivatives as novel anti-tubercular agents towards multi- and extensively drug resistantJournal of enzyme inhibition and medicinal chemistry · 2023Article
- Synthesis and Structure-Activity Relationships of a New Class of Oxadiazoles Targeting DprE1 as Antitubercular Agents.ACS medicinal chemistry letters · 2023Article
- Deciphering the biosynthesis of a novel lipid in Mycobacterium tuberculosis expands the known roles of the nitroreductase superfamily.The Journal of biological chemistry · 2023Article
- Target Identification in Anti-Tuberculosis Drug Discovery.International journal of molecular sciences · 2023Review
- Assay development and inhibition of theMicrobiology (Reading, England) · 2023Article
- Implications of Fragment-Based Drug Discovery in Tuberculosis and HIV.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Recent Advances of DprE1 Inhibitors againstACS omega · 2022Review
- Interrogation of the Pathogen Box reveals small molecule ligands against the mycobacterial trehalose transporter LpqY-SugABC.RSC medicinal chemistry · 2022Article
38 more citing papers are in PubMed but not listed here.
Corrections and comments
- Commented on by
- Erratum issuedRobbins, Scott H [added]; Barnes, S Whitney [added]; Walker, John R [added]; Johnson, Kai [corrected to Johnsson, Kai]
Authors and funding
28 authors at 10 institutions in 4 countries.
Funding
Abstract
A cell-based phenotypic screen for inhibitors of biofilm formation in mycobacteria identified the small molecule TCA1, which has bactericidal activity against both drug-susceptible and -resistant Mycobacterium tuberculosis (Mtb) and sterilizes Mtb in vitro combined with rifampicin or isoniazid. In addition, TCA1 has bactericidal activity against nonreplicating Mtb in vitro and is efficacious in acute and chronic Mtb infection mouse models both alone and combined with rifampicin or isoniazid. Transcriptional analysis revealed that TCA1 down-regulates genes known to be involved in Mtb persistence. Genetic and affinity-based methods identified decaprenyl-phosphoryl-β-D-ribofuranose oxidoreductase DprE1 and MoeW, enzymes involved in cell wall and molybdenum cofactor biosynthesis, respectively, as targets responsible for the activity of TCA1. These in vitro and in vivo results indicate that this compound functions by a unique mechanism and suggest that TCA1 may lead to the development of a class of antituberculosis agents.
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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.