Evidence map›Paper›PMID 33710875›Full record

ArticleACS infectious diseases2021

A Long Residence Time Enoyl-Reductase Inhibitor Explores an Extended Binding Region with Isoenzyme-Dependent Tautomer Adaptation and Differential Substrate-Binding Loop Closure.

Sandra Eltschkner, Josef Kehrein, Thien Anh Le, Shabnam Davoodi, Benjamin Merget, Sneha Basak, Jonas D Weinrich, Johannes Schiebel, Peter J Tonge, Bernd Engels and 2 more

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS infectious diseases, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.4field-weighted citation impact, top 45% 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

4 citing papers in PubMed, 7 citations in OpenAlex.

  1. Altered residence time as a cause of drug resistance.Current opinion in structural biology · 2026
    Review
  2. Review
  3. Review
  4. 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 at 3 institutions in 3 countries.

Sandra EltschknerRudolf Virchow Center for Integrative and Translational Bioimaging, Institute for Structural Biology, University of Würzburg, 97080 Würzburg, Germany.
Josef KehreinInstitute of Pharmacy and Food Chemistry, University of Würzburg, 97074 Würzburg, Germany.
Thien Anh LeInstitute of Physical and Theoretical Chemistry, University of Würzburg, 97074 Würzburg, Germany.
Shabnam DavoodiInstitute for Chemical Biology and Drug Discovery, Department of Chemistry, Stony Brook University, Stony Brook, New York 11794, United States.
Benjamin MergetInstitute of Pharmacy and Food Chemistry, University of Würzburg, 97074 Würzburg, Germany.
Sneha BasakInstitute for Chemical Biology and Drug Discovery, Department of Chemistry, Stony Brook University, Stony Brook, New York 11794, United States.
Jonas D WeinrichRudolf Virchow Center for Integrative and Translational Bioimaging, Institute for Structural Biology, University of Würzburg, 97080 Würzburg, Germany.
Johannes SchiebelRudolf Virchow Center for Integrative and Translational Bioimaging, Institute for Structural Biology, University of Würzburg, 97080 Würzburg, Germany.
Peter J TongeInstitute for Chemical Biology and Drug Discovery, Department of Chemistry, Stony Brook University, Stony Brook, New York 11794, United States.
Bernd EngelsInstitute of Physical and Theoretical Chemistry, University of Würzburg, 97074 Würzburg, Germany.ORCID 0000-0003-3057-389X
Christoph SotrifferInstitute of Pharmacy and Food Chemistry, University of Würzburg, 97074 Würzburg, Germany.ORCID 0000-0003-4713-4068
Caroline KiskerRudolf Virchow Center for Integrative and Translational Bioimaging, Institute for Structural Biology, University of Würzburg, 97080 Würzburg, Germany.ORCID 0000-0002-0216-6026
University of Würzburg · DEStony Brook University · USLund University · SE

Funding

Mechanism of Slow Onset Enzyme Inhibition and Translation to Time-Dependent Drug ActivityR01GM102864 · NIGMS · STATE UNIVERSITY NEW YORK STONY BROOK · PI TONGE, PETER J · 2012 to 2021
$2.6M
NIGMS NIH HHS R01 GM102864
6 · The paper itself

Abstract

The enoyl-acyl carrier protein (ACP) reductase (ENR) is a key enzyme within the bacterial fatty-acid synthesis pathway. It has been demonstrated that small-molecule inhibitors carrying the diphenylether (DPE) scaffold bear a great potential for the development of highly specific and effective drugs against this enzyme class. Interestingly, different substitution patterns of the DPE scaffold have been shown to lead to varying effects on the kinetic and thermodynamic behavior toward ENRs from different organisms. Here, we investigated the effect of a 4'-pyridone substituent in the context of the slow tight-binding inhibitor SKTS1 on the inhibition of the

Indexed as

IsoenzymesEnzyme InhibitorsIsomerismMycobacterium tuberculosisOxidoreductasesStaphylococcus aureusEnzyme InhibitorsIsoenzymesOxidoreductasesdiphenyletherenoyl-ACP reductaseMycobacterium tuberculosisresidence timeStaphylococcus aureustautomerization

Identifiers

PMID33710875
PMCPMC8791450
OpenAlexW3135496908

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.