Evidence map›Paper›PMID 31483651›Full record

ArticleJournal of medicinal chemistry2019

Heteroaryl Phosphonates as Noncovalent Inhibitors of Both Serine- and Metallocarbapenemases.

Orville A Pemberton, Priyadarshini Jaishankar, Afroza Akhtar, Jessie L Adams, Lindsey N Shaw, Adam R Renslo, Yu Chen

Open access · greenAbstract 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 17 papers.

0numbers the graph read from it
0cells of the map it votes in
17citing papers in PubMed
1.4field-weighted citation impact, top 21% 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

17 citing papers in PubMed, 47 citations in OpenAlex.

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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

7 authors at 2 institutions in 1 country.

Orville A PembertonDepartment of Molecular Medicine , University of South Florida Morsani College of Medicine , 12901 Bruce B. Downs Boulevard, MDC 3522 , Tampa , Florida 33612 , United States.
Priyadarshini JaishankarDepartment of Pharmaceutical Chemistry and Small Molecule Discovery Center , University of California, San Francisco , 600 16th Street, Genentech Hall N574 , San Francisco , California 94158 , United States.
Afroza AkhtarDepartment of Molecular Medicine , University of South Florida Morsani College of Medicine , 12901 Bruce B. Downs Boulevard, MDC 3522 , Tampa , Florida 33612 , United States.
Jessie L AdamsDepartment of Cell Biology, Microbiology & Molecular Biology , University of South Florida , 4202 E. Fowler Avenue , Tampa , Florida 33620 , United States.
Lindsey N ShawDepartment of Cell Biology, Microbiology & Molecular Biology , University of South Florida , 4202 E. Fowler Avenue , Tampa , Florida 33620 , United States.ORCID 0000-0002-0629-8990
Adam R RensloDepartment of Pharmaceutical Chemistry and Small Molecule Discovery Center , University of California, San Francisco , 600 16th Street, Genentech Hall N574 , San Francisco , California 94158 , United States.ORCID 0000-0002-1240-2846
Yu ChenDepartment of Molecular Medicine , University of South Florida Morsani College of Medicine , 12901 Bruce B. Downs Boulevard, MDC 3522 , Tampa , Florida 33612 , United States.ORCID 0000-0002-5115-3600
University of South Florida · USUniversity of California, San Francisco · US

Funding

Engaging University of California Stakeholders for Biorespository ResearchUL1TR000004 · NCATS · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI GRANDIS, JENNIFER RUBIN · 2012 to 2015
$78.0M
Evolution and inhibition of beta-lactamase activity in antibiotic resistanceR01AI103158 · NIAID · UNIVERSITY OF SOUTH FLORIDA · PI CHEN, YU · 2013 to 2017
$2.0M
The Role and Regulation of Extracellular Proteases in Staphylococcus aureusR01AI124458 · NIAID · UNIVERSITY OF SOUTH FLORIDA · PI SHAW, LINDSEY NEIL · 2017 to 2020
$1.7M
NCATS NIH HHS UL1 TR000004NIAID NIH HHS R01 AI103158NIAID NIH HHS R01 AI124458
6 · The paper itself

Abstract

Gram-negative pathogens expressing serine β-lactamases (SBLs) and metallo-β-lactamases (MBLs), especially those with carbapenemase activity, threaten the clinical utility of almost all β-lactam antibiotics. Here we describe the discovery of a heteroaryl phosphonate scaffold that exhibits noncovalent cross-class inhibition of representative carbapenemases, specifically the SBL KPC-2 and the MBLs NDM-1 and VIM-2. The most potent lead, compound

Indexed as

Anti-Bacterial AgentsBacterial Proteinsbeta-Lactamase Inhibitorsbeta-Lactamasesbeta-LactamsCrystallography, X-RayDrug DesignEnterobacter cloacaeEscherichia coliHEK293 CellsHumansImipenemKlebsiella pneumoniaeLigandsMicrosomes, LiverMolecular ConformationAnti-Bacterial AgentsBacterial Proteinsbeta-lactamase bla(vim-2)beta-Lactamase Inhibitorsbeta-lactamase KPC-2beta-lactamase NDM-1beta-Lactamasesbeta-LactamscarbapenemaseImipenemLigandsOrganophosphonates

Identifiers

PMID31483651
PMCPMC7175962
OpenAlexW2971664148

What OpenQuestion holds

Textmetadata
LicenceTDM
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.