Evidence map›Paper›PMID 30153005›Full record

ArticleJournal of medicinal chemistry2018

Structure-Based Design of MptpB Inhibitors That Reduce Multidrug-Resistant Mycobacterium tuberculosis Survival and Infection Burden in Vivo.

Clare F Vickers, Ana P G Silva, Ajanta Chakraborty, Paulina Fernandez, Natalia Kurepina, Charis Saville, Yandi Naranjo, Miquel Pons, Laura S Schnettger, Maximiliano G Gutierrez and 6 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.

0numbers the graph read from it
0cells of the map it votes in
22citing 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

22 citing papers in PubMed.

  1. Article
  2. Review
  3. Article
  4. Review
  5. Article
  6. Review
  7. Article
  8. TowardMicroorganisms · 2024
    Review
  9. Combating Tuberculosis via Restoring the Host Immune Capacity by TargetingInternational journal of molecular sciences · 2024
    Review
  10. Article
  11. Article
  12. Review
  13. Article
  14. Review
  15. Review
  16. Article
  17. One Size Fits All? Not inFrontiers in cellular and infection microbiology · 2021
    Review
  18. Review
  19. Highly Potent and SelectiveJournal of medicinal chemistry · 2020
    Article
  20. Molecule Property Analyses of Active Compounds forJournal of medicinal chemistry · 2020
    Review
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

16 authors.

Clare F VickersThe School of Chemistry , University of Manchester , Manchester M13 9PL , United Kingdom.
Ana P G SilvaSchool of Biological Sciences, Faculty of Biology Medicine and Health, Manchester Academic Health Science Centre , University of Manchester , Manchester M13 9PT , United Kingdom.
Ajanta ChakrabortySchool of Biological Sciences, Faculty of Biology Medicine and Health, Manchester Academic Health Science Centre , University of Manchester , Manchester M13 9PT , United Kingdom.
Paulina FernandezSchool of Biological Sciences, Faculty of Biology Medicine and Health, Manchester Academic Health Science Centre , University of Manchester , Manchester M13 9PT , United Kingdom.
Natalia KurepinaPublic Health Research Institute , New Jersey Medical School, Rutgers University , 225 Warren Street , Newark , New Jersey 07103 , United States.
Charis SavilleSchool of Biological Sciences, Faculty of Biology Medicine and Health, Manchester Academic Health Science Centre , University of Manchester , Manchester M13 9PT , United Kingdom.
Yandi NaranjoDepartament de Química Inorgànica i Orgànica , Universitat de Barcelona , Baldiri Reixac, 10-12 , 08028 Barcelona , Spain.
Miquel PonsDepartament de Química Inorgànica i Orgànica , Universitat de Barcelona , Baldiri Reixac, 10-12 , 08028 Barcelona , Spain.ORCID 0000-0002-0586-8322
Laura S SchnettgerHost-Pathogen Interactions in Tuberculosis Laboratory , The Francis Crick Institute , 1 Midland Road , NW1 1AT London , United Kingdom.
Maximiliano G GutierrezHost-Pathogen Interactions in Tuberculosis Laboratory , The Francis Crick Institute , 1 Midland Road , NW1 1AT London , United Kingdom.
Steven ParkPublic Health Research Institute , New Jersey Medical School, Rutgers University , 225 Warren Street , Newark , New Jersey 07103 , United States.
Barry N KreiswithPublic Health Research Institute , New Jersey Medical School, Rutgers University , 225 Warren Street , Newark , New Jersey 07103 , United States.
David S PerlinPublic Health Research Institute , New Jersey Medical School, Rutgers University , 225 Warren Street , Newark , New Jersey 07103 , United States.
Eric J ThomasThe School of Chemistry , University of Manchester , Manchester M13 9PL , United Kingdom.
Jennifer S CavetSchool of Biological Sciences, Faculty of Biology Medicine and Health, Manchester Academic Health Science Centre , University of Manchester , Manchester M13 9PT , United Kingdom.
Lydia TaberneroSchool of Biological Sciences, Faculty of Biology Medicine and Health, Manchester Academic Health Science Centre , University of Manchester , Manchester M13 9PT , United Kingdom.ORCID 0000-0001-8867-455X

Funding

Therapeutics for drug resistant-bacteria: Arylpropionyl-phloroglucinolsU19AI109713 · NIAID · RBHS-NEW JERSEY MEDICAL SCHOOL · PI PERLIN, DAVID S · 2014 to 2018
$26.9M
Medical Research Council MC_PC_13070Medical Research Council MC_UP_1202/11NIAID NIH HHS U19 AI109713Wellcome Trust
6 · The paper itself

Abstract

Mycobacterium tuberculosis protein-tyrosine-phosphatase B (MptpB) is a secreted virulence factor that subverts antimicrobial activity in the host. We report here the structure-based design of selective MptpB inhibitors that reduce survival of multidrug-resistant tuberculosis strains in macrophages and enhance killing efficacy by first-line antibiotics. Monotherapy with an orally bioavailable MptpB inhibitor reduces infection burden in acute and chronic guinea pig models and improves the overall pathology. Our findings provide a new paradigm for tuberculosis treatment.

Indexed as

Drug DesignAnimalsAntitubercular AgentsBacterial ProteinsDrug Resistance, MultipleFemaleGuinea PigsMacrophagesMaleModels, MolecularMolecular StructureMycobacterium tuberculosisProtein ConformationProtein Tyrosine PhosphatasesStructure-Activity RelationshipTuberculosis, Multidrug-ResistantAntitubercular AgentsBacterial ProteinsMptpA protein, Mycobacterium tuberculosisProtein Tyrosine Phosphatases

Identifiers

PMID30153005
PMCPMC6459586

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.