Evidence map›Paper›PMID 31454231›Full record

ArticleJournal of medicinal chemistry2019

Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-β-Lactamases.

Alen Krajnc, Jürgen Brem, Philip Hinchliffe, Karina Calvopiña, Tharindi D Panduwawala, Pauline A Lang, Jos J A G Kamps, Jonathan M Tyrrell, Emma Widlake, Benjamin G Saward and 3 more

Open access · hybridAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 101 papers.

0numbers the graph read from it
0cells of the map it votes in
101citing papers in PubMed
7.8field-weighted citation impact, top 1% of its field
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

101 citing papers in PubMed, 197 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
  4. Article
  5. Article
  6. Review
  7. Article
  8. Article
  9. Review
  10. Article
  11. Review
  12. Article
  13. Review
  14. Article
  15. Review
  16. Article
  17. Evaluation ofAntimicrobial agents and chemotherapy · 2025
    Article
  18. Article
  19. Review
  20. Recent Development of Boron-Containing Small-Molecule Anticancer Agents.ACS pharmacology & translational science · 2025
    Review

41 more citing papers are in PubMed but not listed here.

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

13 authors at 2 institutions in 1 country.

Alen KrajncChemistry Research Laboratory, Department of Chemistry , University of Oxford , 12 Mansfield Road , Oxford OX1 3TA , United Kingdom.ORCID 0000-0001-7822-1944
Jürgen BremChemistry Research Laboratory, Department of Chemistry , University of Oxford , 12 Mansfield Road , Oxford OX1 3TA , United Kingdom.ORCID 0000-0002-0137-3226
Philip HinchliffeSchool of Cellular and Molecular Medicine, Biomedical Sciences Building, University Walk , University of Bristol , Bristol BS8 1TD , United Kingdom.ORCID 0000-0001-8611-4743
Karina CalvopiñaChemistry Research Laboratory, Department of Chemistry , University of Oxford , 12 Mansfield Road , Oxford OX1 3TA , United Kingdom.
Tharindi D PanduwawalaChemistry Research Laboratory, Department of Chemistry , University of Oxford , 12 Mansfield Road , Oxford OX1 3TA , United Kingdom.
Pauline A LangChemistry Research Laboratory, Department of Chemistry , University of Oxford , 12 Mansfield Road , Oxford OX1 3TA , United Kingdom.ORCID 0000-0003-3187-1469
Jos J A G KampsChemistry Research Laboratory, Department of Chemistry , University of Oxford , 12 Mansfield Road , Oxford OX1 3TA , United Kingdom.
Jonathan M TyrrellDepartment of Medical Microbiology & Infectious Disease , Institute of Infection & Immunity , UHW Main Building, Heath Park , Cardiff CF14 4XN , United Kingdom.
Emma WidlakeDepartment of Medical Microbiology & Infectious Disease , Institute of Infection & Immunity , UHW Main Building, Heath Park , Cardiff CF14 4XN , United Kingdom.
Benjamin G SawardChemistry Research Laboratory, Department of Chemistry , University of Oxford , 12 Mansfield Road , Oxford OX1 3TA , United Kingdom.
Timothy R WalshDepartment of Medical Microbiology & Infectious Disease , Institute of Infection & Immunity , UHW Main Building, Heath Park , Cardiff CF14 4XN , United Kingdom.
James SpencerSchool of Cellular and Molecular Medicine, Biomedical Sciences Building, University Walk , University of Bristol , Bristol BS8 1TD , United Kingdom.ORCID 0000-0002-4602-0571
Christopher J SchofieldChemistry Research Laboratory, Department of Chemistry , University of Oxford , 12 Mansfield Road , Oxford OX1 3TA , United Kingdom.ORCID 0000-0002-0290-6565
University of Oxford · GBUniversity of Bristol · GB

Funding

A Mechanism-Based Approach to Metallo-beta-Lactamase InhibitionR01AI100560 · NIAID · CASE WESTERN RESERVE UNIVERSITY · PI BONOMO, ROBERT A., SPENCER, JAMES · 2012 to 2022
$4.4M
Biotechnology and Biological Sciences Research Council BB/L01386X/1Biotechnology and Biological Sciences Research Council BB/M012107/1Biotechnology and Biological Sciences Research Council BB/S50676X/1Cancer Research UKMedical Research Council G1100135Medical Research Council MR/N002679/1NIAID NIH HHS R01 AI100560Wellcome Trust
6 · The paper itself

Abstract

The bicyclic boronate VNRX-5133 (taniborbactam) is a new type of β-lactamase inhibitor in clinical development. We report that VNRX-5133 inhibits serine-β-lactamases (SBLs) and some clinically important metallo-β-lactamases (MBLs), including NDM-1 and VIM-1/2. VNRX-5133 activity against IMP-1 and tested B2/B3 MBLs was lower/not observed. Crystallography reveals how VNRX-5133 binds to the class D SBL OXA-10 and MBL NDM-1. The crystallographic results highlight the ability of bicyclic boronates to inhibit SBLs and MBLs via binding of a tetrahedral (sp

Indexed as

Anti-Infective Agentsbeta-Lactamase Inhibitorsbeta-LactamasesBorinic AcidsBoronBridged Bicyclo CompoundsCarboxylic AcidsCatalytic DomainCrystallography, X-RayDrug DesignEscherichia coliHumansInhibitory Concentration 50Klebsiella pneumoniaeMagnetic Resonance SpectroscopyMicrobial Sensitivity TestsAnti-Infective Agentsbeta-Lactamase Inhibitorsbeta-LactamasesBorinic AcidsBoronBridged Bicyclo CompoundsCarboxylic AcidsOxygenSolventstaniborbactam

Identifiers

PMID31454231
PMCPMC6767355
OpenAlexW2970048441

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.