Evidence map›Paper›PMID 39074100›Full record

ArticlePloS one2024

Identification of drug-like molecules targeting the ATPase activity of dynamin-like EHD4.

Saif Mohd, Andreas Oder, Edgar Specker, Martin Neuenschwander, Jens Peter Von Kries, Oliver Daumke

Abstract read
In one paragraph

Article in PloS one, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

2 citing papers in PubMed.

  1. Article
  2. 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

6 authors.

Saif MohdStructural Biology, Max Delbrück Center for Molecular Medicine in the Helmholtz Association, Berlin, Germany.
Andreas OderScreening Unit, Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany.
Edgar SpeckerScreening Unit, Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany.
Martin NeuenschwanderScreening Unit, Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany.
Jens Peter Von KriesScreening Unit, Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany.
Oliver DaumkeStructural Biology, Max Delbrück Center for Molecular Medicine in the Helmholtz Association, Berlin, Germany.ORCID 0000-0002-6190-1414

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Eps15 (epidermal growth factor receptor pathway substrate 15) homology domain-containing proteins (EHDs) comprise a family of eukaryotic dynamin-related ATPases that participate in various endocytic membrane trafficking pathways. Dysregulation of EHDs function has been implicated in various diseases, including cancer. The lack of small molecule inhibitors which acutely target individual EHD members has hampered progress in dissecting their detailed cellular membrane trafficking pathways and their function during disease. Here, we established a Malachite green-based assay compatible with high throughput screening to monitor the liposome-stimulated ATPase of EHD4. In this way, we identified a drug-like molecule that inhibited EHD4's liposome-stimulated ATPase activity. Structure activity relationship (SAR) studies indicated sites of preferred substitutions for more potent inhibitor synthesis. Moreover, the assay optimization in this work can be applied to other dynamin family members showing a weak and liposome-dependent nucleotide hydrolysis activity.

Indexed as

Adenosine TriphosphatasesLiposomesDynaminsHumansHydrolysisRosaniline DyesStructure-Activity RelationshipAdenosine TriphosphatasesDynaminsLiposomesmalachite greenRosaniline Dyes

Identifiers

PMID39074100
PMCPMC11285977

What Socratic holds

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Registered trials

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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 Socratic graph.