Evidence map›Paper›PMID 35340861›Full record

ArticleChemical science2022

Cooperativity as quantification and optimization paradigm for nuclear receptor modulators.

Pim J de Vink, Auke A Koops, Giulia D'Arrigo, Gabriele Cruciani, Francesca Spyrakis, Luc Brunsveld

Open access · diamondAbstract read
In one paragraph

Article in Chemical science, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.

0numbers the graph read from it
0cells of the map it votes in
12citing papers in PubMed
2.6field-weighted citation impact, top 10% 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

12 citing papers in PubMed, 14 citations in OpenAlex.

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  12. Exploring Ligand Binding Domain Dynamics in the NRs Superfamily.International journal of molecular sciences · 2022
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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 at 3 institutions in 2 countries.

Pim J de VinkLaboratory of Chemical Biology, Department of Biomedical Engineering and Institute for Complex Molecular Systems, Eindhoven University of Technology P. O. Box 513 5600MB Eindhoven The Netherlands l.brunsveld@tue.nl.ORCID https://orcid.org/0000-0001-6822-6995
Auke A KoopsLaboratory of Chemical Biology, Department of Biomedical Engineering and Institute for Complex Molecular Systems, Eindhoven University of Technology P. O. Box 513 5600MB Eindhoven The Netherlands l.brunsveld@tue.nl.ORCID https://orcid.org/0000-0003-0125-2085
Giulia D'ArrigoLaboratory of Chemical Biology, Department of Biomedical Engineering and Institute for Complex Molecular Systems, Eindhoven University of Technology P. O. Box 513 5600MB Eindhoven The Netherlands l.brunsveld@tue.nl.ORCID https://orcid.org/0000-0002-1113-2266
Gabriele CrucianiDepartment of Chemistry, Biology and Biotechnology, University of Perugia Via Elce di Sotto 8 06123 Perugia Italy.
Francesca SpyrakisDepartment of Drug Science and Technology, University of Turin via Giuria 9 10125 Turin Italy francesca.spyrakis@unito.it.
Luc BrunsveldLaboratory of Chemical Biology, Department of Biomedical Engineering and Institute for Complex Molecular Systems, Eindhoven University of Technology P. O. Box 513 5600MB Eindhoven The Netherlands l.brunsveld@tue.nl.ORCID https://orcid.org/0000-0001-5675-511X
Eindhoven University of Technology · NLUniversity of Turin · ITUniversity of Perugia · IT

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Nuclear Receptors (NRs) are highly relevant drug targets, for which small molecule modulation goes beyond a simple ligand/receptor interaction. NR-ligands modulate Protein-Protein Interactions (PPIs) with coregulator proteins. Here we bring forward a cooperativity mechanism for small molecule modulation of NR PPIs, using the Peroxisome Proliferator Activated Receptor γ (PPARγ), which describes NR-ligands as allosteric molecular glues. The cooperativity framework uses a thermodynamic model based on three-body binding events, to dissect and quantify reciprocal effects of NR-coregulator binding (

Identifiers

PMID35340861
PMCPMC8890100
OpenAlexW4206221822

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC
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.