Evidence map›Paper›PMID 28825467›Full record

ArticleACS combinatorial science2017

Parallel Chemistry Approach to Identify Novel Nuclear Receptor Ligands Based on the GW0742 Scaffold.

Kelly A Teske, Ganesha Rai, Premchendar Nandhikonda, Preetpal S Sidhu, Belaynesh Feleke, Anton Simeonov, Adam Yasgar, Ajit Jadhav, David J Maloney, Leggy A Arnold

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS combinatorial science, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
0.2field-weighted citation impact, top 43% 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

1 citing paper in PubMed, 3 citations in OpenAlex.

  1. Novel VDR antagonists based on the GW0742 scaffold.Bioorganic & medicinal chemistry letters · 2018
    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

10 authors at 2 institutions in 1 country.

Kelly A TeskeDepartment of Chemistry and Biochemistry, Milwaukee Institute for Drug Discovery, University of Wisconsin , Milwaukee, Wisconsin 53211, United States.
Ganesha RaiNIH Chemical Genomics Center, National Center for Advancing Translational Sciences (NCATS), National Institutes of Health , Bethesda, Maryland 20892-3370, United States.
Premchendar NandhikondaDepartment of Chemistry and Biochemistry, Milwaukee Institute for Drug Discovery, University of Wisconsin , Milwaukee, Wisconsin 53211, United States.
Preetpal S SidhuDepartment of Chemistry and Biochemistry, Milwaukee Institute for Drug Discovery, University of Wisconsin , Milwaukee, Wisconsin 53211, United States.
Belaynesh FelekeDepartment of Chemistry and Biochemistry, Milwaukee Institute for Drug Discovery, University of Wisconsin , Milwaukee, Wisconsin 53211, United States.
Anton SimeonovNIH Chemical Genomics Center, National Center for Advancing Translational Sciences (NCATS), National Institutes of Health , Bethesda, Maryland 20892-3370, United States.
Adam YasgarNIH Chemical Genomics Center, National Center for Advancing Translational Sciences (NCATS), National Institutes of Health , Bethesda, Maryland 20892-3370, United States.
Ajit JadhavNIH Chemical Genomics Center, National Center for Advancing Translational Sciences (NCATS), National Institutes of Health , Bethesda, Maryland 20892-3370, United States.
David J MaloneyNIH Chemical Genomics Center, National Center for Advancing Translational Sciences (NCATS), National Institutes of Health , Bethesda, Maryland 20892-3370, United States.ORCID 0000-0002-5607-4178
Leggy A ArnoldDepartment of Chemistry and Biochemistry, Milwaukee Institute for Drug Discovery, University of Wisconsin , Milwaukee, Wisconsin 53211, United States.ORCID 0000-0003-1411-1572
National Institutes of Health · USUniversity of Wisconsin–Milwaukee · US

Funding

Small molecule inhibitors of the vitamin D receptor-coactivator interactionR03DA031090 · NIDA · UNIVERSITY OF WISCONSIN MILWAUKEE · PI ARNOLD, ALEXANDER · 2010 to 2011
$73k
NIDA NIH HHS R03 DA031090
6 · The paper itself

Abstract

We describe the parallel synthesis of novel analogs of GW0742, a peroxisome proliferator-activated receptor δ (PPARδ) agonist. For that purpose, modified reaction conditions were applied, such as a solid-phase palladium-catalyzed Suzuki coupling. In addition, tetrazole-based compounds were generated as a bioisostere for carboxylic acid-containing ligand GW0742. The new compounds were investigated for their ability to activate PPARδ mediated transcription and their cross-reactivity with the vitamin D receptor (VDR), another member of the nuclear receptor superfamily. We identified many potent PPARδ agonists that were less toxic than GW0742, where ∼65 of the compounds synthesized exhibited partial PPARδ activity (23-98%) with EC

Indexed as

Cell SurvivalDrug DesignHEK293 CellsHigh-Throughput Screening AssaysHumansLigandsMolecular Docking SimulationPhenolsPPAR deltaReceptors, CalcitriolSmall Molecule LibrariesStructure-Activity RelationshipSulfhydryl CompoundsTetrazolesThiazolesTranscription, Genetic(4-(((2-(3-fluoro-4-(trifluoromethyl)phenyl)-4-methyl-1,3-thiazol-5-yl)methyl)sulfanyl)-2-methylphenoxy)acetic acidLigandsPhenolsPPAR deltaReceptors, CalcitriolSmall Molecule LibrariesSulfhydryl CompoundsTetrazolesThiazolesGW0742nuclear receptorperoxisome proliferation-activated receptorssteroid receptor coactivator 2vitamin D receptor

Identifiers

PMID28825467
PMCPMC5643073
OpenAlexW2749553108

What OpenQuestion holds

Textmetadata
LicenceTDM
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.