Evidence map›Paper›PMID 38917049›Full record

ArticleJournal of medicinal chemistry2024

Development of a Potent and Selective G2A (GPR132) Agonist.

Victor Hernandez-Olmos, Jan Heering, Beatrice Marinescu, Tina Schermeng, Vladimir V Ivanov, Yurii S Moroz, Sheila Nevermann, Marius Mathes, Johanna H M Ehrler, Mohamad Wessam Alnouri and 15 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing 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

3 citing papers in PubMed.

  1. Review
  2. Article
  3. 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

25 authors.

Victor Hernandez-OlmosFraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.ORCID 0000-0002-4064-1473
Jan HeeringFraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.
Beatrice MarinescuInstitute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Street 9, 60438 Frankfurt am Main, Germany.
Tina SchermengInstitute of Biochemistry, Faculty of Life Sciences, Leipzig University, Brüderstraße 34, 04103 Leipzig, Germany.ORCID 0000-0001-7508-3574
Vladimir V IvanovEnamine Ltd, 67 Chervonotkatska Street, Kyiv 02094, Ukraine.
Yurii S MorozTaras Shevchenko National University of Kyiv, 64 Volodymyrska Street, Kyiv 01601, Ukraine.ORCID 0000-0001-6073-002X
Sheila NevermannFraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.
Marius MathesInstitute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Street 9, 60438 Frankfurt am Main, Germany.
Johanna H M EhrlerInstitute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Street 9, 60438 Frankfurt am Main, Germany.ORCID 0000-0001-7990-4042
Mohamad Wessam AlnouriDepartment of Pharmacology, Max Planck Institute for Heart and Lung Research, Ludwigstr. 43, 61231Bad Nauheim, Germany.
Markus WolfFraunhofer Institute for Translational Medicine and Pharmacology ITMP, Discovery Research ScreeningPort, Schnackenburgallee 114, 22525 Hamburg, Germany.
Alicia S HaydoDepartment of Medicine, Hematology/Oncology, Goethe University Hospital Frankfurt, Theodor-Stern-Kai 7, 60590 Frankfurt am Main, Germany.
Tessa SchmachtelDepartment of Medicine, Hematology/Oncology, Goethe University Hospital Frankfurt, Theodor-Stern-Kai 7, 60590 Frankfurt am Main, Germany.
Andrea ZalianiFraunhofer Institute for Translational Medicine and Pharmacology ITMP, Discovery Research ScreeningPort, Schnackenburgallee 114, 22525 Hamburg, Germany.
Georg HöfnerDepartment of Pharmacy, Ludwig-Maximilians-Universität München, Butenandtstr. 5-13, 81377 Munich, Germany.
Astrid KaiserInstitute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Street 9, 60438 Frankfurt am Main, Germany.
Manfred Schubert-ZsilaveczInstitute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Street 9, 60438 Frankfurt am Main, Germany.
Annette G Beck-SickingerInstitute of Biochemistry, Faculty of Life Sciences, Leipzig University, Brüderstraße 34, 04103 Leipzig, Germany.ORCID 0000-0003-4560-8020
Stefan OffermannsDepartment of Pharmacology, Max Planck Institute for Heart and Lung Research, Ludwigstr. 43, 61231Bad Nauheim, Germany.
Philipp GribbonFraunhofer Institute for Translational Medicine and Pharmacology ITMP, Discovery Research ScreeningPort, Schnackenburgallee 114, 22525 Hamburg, Germany.
Michael A RiegerFraunhofer Institute for Translational Medicine and Pharmacology ITMP, Discovery Research ScreeningPort, Schnackenburgallee 114, 22525 Hamburg, Germany.
Daniel MerkDepartment of Pharmacy, Ludwig-Maximilians-Universität München, Butenandtstr. 5-13, 81377 Munich, Germany.ORCID 0000-0002-5359-8128
Marco SisignanoPharmazentrum Frankfurt/ZAFES, Institute of Clinical Pharmacology, Goethe University, Theodor-Stern-Kai 7, 60590 Frankfurt am Main, Germany.
Dieter SteinhilberFraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.
Ewgenij ProschakFraunhofer Institute for Translational Medicine and Pharmacology ITMP, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany.ORCID 0000-0003-1961-1859

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

G protein-coupled receptor G2A was postulated to be a promising target for the development of new therapeutics in neuropathic pain, acute myeloid leukemia, and inflammation. However, there is still a lack of potent, selective, and drug-like G2A agonists to be used as a chemical tool or as the starting matter for the development of drugs. In this work, we present the discovery and structure-activity relationship elucidation of a new potent and selective G2A agonist scaffold. Systematic optimization resulted in (3-(pyridin-3-ylmethoxy)benzoyl)-

Indexed as

Receptors, G-Protein-CoupledAnimalsHumansMolecular StructurePhenylalanineStructure-Activity RelationshipPhenylalanineReceptors, G-Protein-Coupled

Identifiers

PMID38917049
PMCPMC11249017

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.