Evidence map›Paper›PMID 38751642›Full record

ArticleACS pharmacology & translational science2024

Ethaverine and Papaverine Target Cyclin-Dependent Kinase 5 and Inhibit Lung Cancer Cell Proliferation and Migration.

Arthur Laure, Chloé Royet, Frederic Bihel, Blandine Baratte, Stéphane Bach, Marion Peyressatre, May C Morris

Abstract read
In one paragraph

Article in ACS pharmacology & translational science, 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. Review
  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

7 authors.

Arthur LaureInstitut des Biomolécules Max Mousseron, CNRS, UMR 5247, Université de Montpellier, 1919 Route de Mende, 34293 Montpellier, France.
Chloé RoyetInstitut des Biomolécules Max Mousseron, CNRS, UMR 5247, Université de Montpellier, 1919 Route de Mende, 34293 Montpellier, France.
Frederic BihelLaboratoire d'Innovation Thérapeutique, IMS, UMR 7200, CNRS, Université de Strasbourg, 67401 Illkirch, France.
Blandine BaratteCNRS, FR2424, Plateforme de criblage KISSf (Kinase Inhibitor Specialized Screening Facility), Sorbonne Université, Station Biologique de Roscoff, 29680 Roscoff, France.
Stéphane BachCNRS, FR2424, Plateforme de criblage KISSf (Kinase Inhibitor Specialized Screening Facility), Sorbonne Université, Station Biologique de Roscoff, 29680 Roscoff, France.ORCID https://orcid.org/0000-0002-7186-7483
Marion PeyressatreInstitut des Biomolécules Max Mousseron, CNRS, UMR 5247, Université de Montpellier, 1919 Route de Mende, 34293 Montpellier, France.
May C MorrisInstitut des Biomolécules Max Mousseron, CNRS, UMR 5247, Université de Montpellier, 1919 Route de Mende, 34293 Montpellier, France.ORCID https://orcid.org/0000-0001-8106-9728

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

CDK5 kinase plays a central role in the regulation of neuronal functions, and its hyperactivation has been associated with neurodegenerative pathologies and more recently with several human cancers, in particular lung cancer. However, ATP-competitive inhibitors targeting CDK5 are poorly selective and suffer limitations, calling for new classes of inhibitors. In a screen for allosteric modulators of CDK5, we identified ethaverine and closely related derivative papaverine and showed that they inhibit cell proliferation and migration of non small cell lung cancer cell lines. Moreover the efficacy of these compounds is significantly enhanced when combined with the ATP-competitive inhibitor roscovitine, suggesting an additive dual mechanism of inhibition targeting CDK5. These compounds do not affect CDK5 stability, but thermodenaturation studies performed with A549 cell extracts infer that they interact with CDK5

Identifiers

PMID38751642
PMCPMC11091981

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.