Evidence map›Paper›PMID 32658475›Full record

ArticleJournal of medicinal chemistry2020

The Structural Basis for Nonsteroidal Anti-Inflammatory Drug Inhibition of Human Dihydrofolate Reductase.

Michael R Duff, Scott A Gabel, Lars C Pedersen, Eugene F DeRose, Juno M Krahn, Elizabeth E Howell, Robert E London

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
1.1field-weighted citation impact, top 23% 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

3 citing papers in PubMed, 14 citations in OpenAlex.

  1. Article
  2. The aminosalicylate - folate connection.Drug metabolism reviews · 2024
    Review
  3. 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

7 authors at 2 institutions in 1 country.

Michael R DuffDepartment of Biochemistry & Cellular and Molecular Biology, University of Tennessee, Knoxville, Tennessee 37996, United States.ORCID 0000-0002-8581-7102
Scott A GabelGenome Integrity and Structural Biology Laboratory, National Institute of Environmental Health Sciences, National Institutes of Health, 111 T. W. Alexander Drive, Research Triangle Park, Durham, North Carolina 27709, United States.
Lars C PedersenGenome Integrity and Structural Biology Laboratory, National Institute of Environmental Health Sciences, National Institutes of Health, 111 T. W. Alexander Drive, Research Triangle Park, Durham, North Carolina 27709, United States.
Eugene F DeRoseGenome Integrity and Structural Biology Laboratory, National Institute of Environmental Health Sciences, National Institutes of Health, 111 T. W. Alexander Drive, Research Triangle Park, Durham, North Carolina 27709, United States.ORCID 0000-0003-0112-1296
Juno M KrahnGenome Integrity and Structural Biology Laboratory, National Institute of Environmental Health Sciences, National Institutes of Health, 111 T. W. Alexander Drive, Research Triangle Park, Durham, North Carolina 27709, United States.
Elizabeth E HowellDepartment of Biochemistry & Cellular and Molecular Biology, University of Tennessee, Knoxville, Tennessee 37996, United States.ORCID 0000-0001-6157-433X
Robert E LondonGenome Integrity and Structural Biology Laboratory, National Institute of Environmental Health Sciences, National Institutes of Health, 111 T. W. Alexander Drive, Research Triangle Park, Durham, North Carolina 27709, United States.ORCID 0000-0001-9108-8463
National Institutes of Health · USUniversity of Tennessee at Knoxville · US

Funding

Crystallographic studies of macromolecular structuresZICES102645 · NIEHS · NATIONAL INSTITUTE OF ENVIRONMENTAL HEALTH SCIENCES · PI PEDERSEN, LARS · 2018 to 2025
$12.6M
Nmr Studies Of Biomolecular Structure, Function, And DynamicsZIAES050111 · NIEHS · NATIONAL INSTITUTE OF ENVIRONMENTAL HEALTH SCIENCES · PI LONDON, ROBERT E · 2009 to 2020
$11.7M
Crystallographic studies of macromolecular structuresZIAES102645 · NIEHS · NATIONAL INSTITUTE OF ENVIRONMENTAL HEALTH SCIENCES · PI PEDERSEN, LARS · 2009 to 2017
$9.4M
Osmotic Pressure and Crowding Effects on Folate Mediated One Carbon MetabolismR15GM110669 · NIGMS · UNIVERSITY OF TENNESSEE KNOXVILLE · PI HOWELL, ELIZABETH E · 2014 to 2014
$323k
Intramural NIH HHS ZIA ES050111Intramural NIH HHS ZIA ES102645NIGMS NIH HHS R15 GM110669
6 · The paper itself

Abstract

Although nonsteroidal anti-inflammatory drugs (NSAIDs) target primarily cyclooxygenase enzymes, a subset of NSAIDs containing carboxylate groups also has been reported to competitively inhibit dihydrofolate reductase (DHFR). In this study, we have characterized NSAID interactions with human DHFR based on kinetic, NMR, and X-ray crystallographic methods. The NSAIDs target a region of the folate binding site that interacts with the

Indexed as

Anti-Inflammatory Agents, Non-SteroidalBinding SitesCrystallography, X-RayDrug DesignFolic AcidFolic Acid AntagonistsHumansModels, MolecularTetrahydrofolate DehydrogenaseAnti-Inflammatory Agents, Non-SteroidalFolic AcidFolic Acid AntagonistsTetrahydrofolate Dehydrogenase

Identifiers

PMID32658475
PMCPMC8404948
OpenAlexW3043309972

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.