Evidence map›Paper›PMID 36615235›Full record

ArticleMolecules (Basel, Switzerland)2022

Straightforward Access to a New Class of Dual DYRK1A/CLK1 Inhibitors Possessing a Simple Dihydroquinoline Core.

Mihaela-Liliana Ţînţaş, Ludovic Peauger, Florent Alix, Cyril Papamicaël, Thierry Besson, Jana Sopková-de Oliveira Santos, Vincent Gembus, Vincent Levacher

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2022. 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
0.1field-weighted citation impact, top 55% 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

2 citing papers in PubMed, 2 citations in OpenAlex.

  1. Review
  2. Review
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

8 authors at 2 institutions in 1 country.

Mihaela-Liliana ŢînţaşINSA Rouen Normandie, Univ. Rouen Normandie, CNRS UMR 6014 COBRA, FR 3038, F-76000 Rouen, France.ORCID 0000-0003-4167-8080
Ludovic PeaugerVFP Therapies, 15 rue François Couperin, 76000 Rouen, France.ORCID 0000-0002-1425-1471
Florent AlixVFP Therapies, 15 rue François Couperin, 76000 Rouen, France.
Cyril PapamicaëlINSA Rouen Normandie, Univ. Rouen Normandie, CNRS UMR 6014 COBRA, FR 3038, F-76000 Rouen, France.ORCID 0000-0001-6884-6844
Thierry BessonINSA Rouen Normandie, Univ. Rouen Normandie, CNRS UMR 6014 COBRA, FR 3038, F-76000 Rouen, France.ORCID 0000-0003-3025-6659
Jana Sopková-de Oliveira SantosUNICAEN, CERMN (Centre d'Etudes et de Recherche sur le Médicament de Normandie), Normandie Univ., Bd Becquerel, F-14032 Caen, France.ORCID 0000-0002-4829-8120
Vincent GembusVFP Therapies, 15 rue François Couperin, 76000 Rouen, France.
Vincent LevacherINSA Rouen Normandie, Univ. Rouen Normandie, CNRS UMR 6014 COBRA, FR 3038, F-76000 Rouen, France.ORCID 0000-0002-6429-1965
Centre National de la Recherche Scientifique · FRNormandie Université · FR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The DYRK (Dual-specificity tyrosine phosphorylation-regulated kinase) family of protein kinases is involved in the pathogenesis of several neurodegenerative diseases. Among them, the DYRK1A protein kinase is thought to be implicated in Alzheimer's disease (AD) and Down syndrome, and as such, has emerged as an appealing therapeutic target. DYRKs are a subset of the CMGC (CDK, MAPKK, GSK3 and CLK) group of kinases. Within this group of kinases, the CDC2-like kinases (CLKs), such as CLK1, are closely related to DYRKs and have also sparked great interest as potential therapeutic targets for AD. Based on inhibitors previously described in the literature (namely TG003 and INDY), we report in this work a new class of dihydroquinolines exhibiting inhibitory activities in the nanomolar range on

Indexed as

Protein Kinase InhibitorsQuinonesAlzheimer DiseaseDown SyndromeDyrk KinasesGlycogen Synthase Kinase 3HumansMolecular Docking SimulationPhosphorylationProtein Serine-Threonine KinasesProtein-Tyrosine Kinases1,4-dihydroquinoneClk dual-specificity kinasesDyrk KinasesGlycogen Synthase Kinase 3Protein Kinase InhibitorsProtein Serine-Threonine KinasesProtein-Tyrosine KinasesQuinonesAlzheimer’s diseaseantioxidantdihydroquinolineDown syndromedual inhibitorhCLK1hDYRK1Amolecular dockingradical scavenger

Identifiers

PMID36615235
PMCPMC9822041
OpenAlexW4313502618

What Socratic holds

Textmetadata
LicenceCC BY
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 Socratic graph.