Evidence map›Paper›PMID 28314097›Full record

ArticleACS chemical biology2017

Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays.

Petar O Nikiforov, Michal Blaszczyk, Sachin Surade, Helena I Boshoff, Andaleeb Sajid, Vincent Delorme, Nathalie Deboosere, Priscille Brodin, Alain R Baulard, Clifton E Barry and 2 more

Abstract read
In one paragraph

Article in ACS chemical biology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

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.

2 · The registry

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.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

13 citing papers in PubMed.

  1. Article
  2. Article
  3. Review
  4. Article
  5. Review
  6. Review
  7. Transcriptional regulation and drug resistance inFrontiers in cellular and infection microbiology · 2022
    Review
  8. Article
  9. Review
  10. Using Fragment-Based Approaches to Discover New Antibiotics.SLAS discovery : advancing life sciences R & D · 2018
    Article
  11. Review
  12. Review
  13. Target Identification ofFrontiers in pharmacology · 2017
    Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

12 authors.

Petar O NikiforovDepartment of Chemistry, University of Cambridge , Lensfield Road, Cambridge CB2 1EW, U.K.
Michal BlaszczykDepartment of Biochemistry, University of Cambridge , 80 Tennis Court Road, Cambridge CB2 1GA, U.K.
Sachin SuradeDepartment of Biochemistry, University of Cambridge , 80 Tennis Court Road, Cambridge CB2 1GA, U.K.
Helena I BoshoffTuberculosis Research Section, Laboratory of Clinical Infectious Diseases, National Institute of Allergy and Infectious Diseases, National Institutes of Health , Bethesda, Maryland 20892, United States.
Andaleeb SajidTuberculosis Research Section, Laboratory of Clinical Infectious Diseases, National Institute of Allergy and Infectious Diseases, National Institutes of Health , Bethesda, Maryland 20892, United States.
Vincent DelormeCNRS, Inserm, CHU Lille, Institut Pasteur de Lille, U1019 - UMR 8204 - CIIL - Center for Infection and Immunity of Lille, Université de Lille , F-59000 Lille, France.
Nathalie DeboosereCNRS, Inserm, CHU Lille, Institut Pasteur de Lille, U1019 - UMR 8204 - CIIL - Center for Infection and Immunity of Lille, Université de Lille , F-59000 Lille, France.
Priscille BrodinCNRS, Inserm, CHU Lille, Institut Pasteur de Lille, U1019 - UMR 8204 - CIIL - Center for Infection and Immunity of Lille, Université de Lille , F-59000 Lille, France.
Alain R BaulardCNRS, Inserm, CHU Lille, Institut Pasteur de Lille, U1019 - UMR 8204 - CIIL - Center for Infection and Immunity of Lille, Université de Lille , F-59000 Lille, France.
Clifton E BarryTuberculosis Research Section, Laboratory of Clinical Infectious Diseases, National Institute of Allergy and Infectious Diseases, National Institutes of Health , Bethesda, Maryland 20892, United States.
Tom L BlundellDepartment of Biochemistry, University of Cambridge , 80 Tennis Court Road, Cambridge CB2 1GA, U.K.
Chris AbellDepartment of Chemistry, University of Cambridge , Lensfield Road, Cambridge CB2 1EW, U.K.ORCID 0000-0001-9174-1987

Funding

Development Of New Chemotherapeutics For TuberculosisZIAAI000693 · NIAID · NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES · PI BARRY, CLIFTON · 2009 to 2025
$20.1M
6 · The paper itself

Abstract

Small-molecule inhibitors of the mycobacterial transcriptional repressor EthR have previously been shown to act as boosters of the second-line antituberculosis drug ethionamide. Fragment-based drug discovery approaches have been used in the past to make highly potent EthR inhibitors with ethionamide boosting activity both in vitro and ex vivo. Herein, we report the development of fragment-sized EthR ligands with nanomolar minimum effective concentration values for boosting the ethionamide activity in Mycobacterium tuberculosis whole-cell assays.

Indexed as

Antitubercular AgentsBacterial ProteinsDrug DiscoveryDrug SynergismEnzyme InhibitorsEthionamideLigandsMicrobial Sensitivity TestsMycobacterium tuberculosisRepressor ProteinsAntitubercular AgentsBacterial ProteinsEnzyme InhibitorsEthionamideEthR protein, Mycobacterium tuberculosisLigandsRepressor Proteins

Identifiers

PMID28314097
PMCPMC5474694

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

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.