ArticleJournal of medicinal chemistry2023
Exploring Fatty Acid Mimetics as NR4A Ligands.
Article in Journal of medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers, 1 of them a synthesis that pooled it.
What it found
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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.
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Who cites it
9 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Pooled it
- A Commentary on Dual Orphan Nuclear Receptor 4A1 (NR4A1) and NR4A2 Ligands.Journal of cellular immunology · 2026Article
- Diabetic Atrial Cardiomyopathy: Pathogenesis, Diagnosis, Management, AI-Driven Diagnosis, and Risk Prediction.Journal of diabetes research · 2026Review
- Identification and Validation of Inverse Agonists for Nuclear Receptor Subfamily 4 Group A Member 2.ACS omega · 2025Article
- Comprehensive Analysis of N6-Methyladenosine Methylation in Transverse Aortic Constriction-Induced Cardiac Fibrosis Based on MeRIP-Seq Analysis.Biomedicines · 2025Article
- Fatty Acid Mimetic Fragments as Liver Receptor Homologue-1 Modulators.ACS pharmacology & translational science · 2025Article
- New opportunities to overcome T cell dysfunction: the role of transcription factors and how to target them.Trends in biochemical sciences · 2024Review
- Deletion of miPEP in adipocytes protects against obesity and insulin resistance by boosting muscle metabolism.Molecular metabolism · 2024Article
- Development of Nurr1 agonists from amodiaquine by scaffold hopping and fragment growing.Communications chemistry · 2024Article
Corrections and comments
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Authors and funding
2 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The ligand-activated transcription factors Nur77, Nurr1, and NOR-1 forming the NR4A family of nuclear receptors are considered as potential targets in various pathologies, including neurodegeneration and cancer. However, chemical tools for pharmacological NR4A modulation as a prerequisite for target validation are rare. Recent findings suggest that NR4As bind fatty acid metabolites and fatty acid mimetic (FAM) drugs, opening new opportunities for NR4A modulator development. We have explored the chemical space of FAM NR4A ligands by using fragment screening, in silico analysis, and systematic structure-activity relationship evaluation. From a chemically diverse library of 92 fragments, we identified 11 new FAM NR4A agonist and inverse agonist scaffolds. Structural optimization of the most active FAM fragment yielded NR4A agonists with submicromolar potency and binding affinity, demonstrating remarkable potential of FAM as NR4A-modulating tools and drugs.
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Registered trials
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.