ArticleJournal of medicinal chemistry2023
Discovery of Potent Tetrazole Free Fatty Acid Receptor 2 Antagonists.
Alice Valentini, Katrine Schultz-Knudsen, Anders Højgaard Hansen, Argyro Tsakoumagkou, Laura Jenkins, Henriette B Christensen, Asmita Manandhar, Graeme Milligan, Trond Ulven, Elisabeth Rexen Ulven
Open access · hybridAbstract read
In one paragraphArticle in Journal of medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
0.2field-weighted citation impact, top 49% of its field
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 registryThe 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 literatureWho cites it
0 citing papers in PubMed, 1 citations in OpenAlex.
No citing paper in PubMed yet.
4 · The recordCorrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
5 · Who and what moneyAuthors and funding
10 authors at 3 institutions in 2 countries.
Alice ValentiniDepartment of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
Katrine Schultz-KnudsenDepartment of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
Anders Højgaard HansenDepartment of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, DK-5230 Odense M, Denmark.
Argyro TsakoumagkouDepartment of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
Laura JenkinsCentre for Translational Pharmacology, School of Molecular Biosciences, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom.
Henriette B ChristensenDepartment of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, DK-5230 Odense M, Denmark.
Asmita ManandharDepartment of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
Graeme MilliganCentre for Translational Pharmacology, School of Molecular Biosciences, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom.ORCID 0000-0002-6946-3519 Trond UlvenDepartment of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.ORCID 0000-0002-8135-1755 Elisabeth Rexen UlvenDepartment of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.ORCID 0000-0003-1243-7587 University of Copenhagen · DKUniversity of Glasgow · GBUniversity of Southern Denmark · DK
Funding
Biotechnology and Biological Sciences Research Council BB/X001814/1
6 · The paper itselfAbstract
The free fatty acid receptor 2 (FFA2), also known as GPR43, mediates effects of short-chain fatty acids and has attracted interest as a potential target for treatment of various metabolic and inflammatory diseases. Herein, we report the results from bioisosteric replacement of the carboxylic acid group of the established FFA2 antagonist CATPB and SAR investigations around these compounds, leading to the discovery of the first high-potency FFA2 antagonists, with the preferred compound TUG-2304 (
Indexed as
Fatty Acids, NonesterifiedReceptors, Cell SurfacePropionatesReceptors, G-Protein-CoupledFatty Acids, NonesterifiedFFAR2 protein, humanPropionatesReceptors, Cell SurfaceReceptors, G-Protein-Coupled
Identifiers
PMID37129317
PMCPMC10547238
OpenAlexW4367668423
What OpenQuestion holds
Textmetadata
LicenceCC BY
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