ArticleScientific reports2014
Quantitative high-throughput profiling of environmental chemicals and drugs that modulate farnesoid X receptor.
Article in Scientific reports, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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.
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.
Who cites it
28 citing papers in PubMed, 46 citations in OpenAlex.
- Synergistic action of cilnidipine and bexarotene in mitigating cholestatic liver damage: role of FXR signaling cascade.Naunyn-Schmiedeberg's archives of pharmacology · 2025Article
- A small intestinal bile acid modulates the gut microbiome to improve host metabolic phenotypes following bariatric surgery.Cell host & microbe · 2024Article
- Repurposing drugs as COVID-19 therapies: A toxicity evaluation.Drug discovery today · 2022Review
- Use of Tox21 Screening Data to Evaluate the COVID-19 Drug Candidates for Their Potential Toxic Effects and Related Pathways.Frontiers in pharmacology · 2022Review
- A Quantitative High-Throughput Screening Data Analysis Pipeline for Activity Profiling.Methods in molecular biology (Clifton, N.J.) · 2022Article
- Confirmation of high-throughput screening data and novel mechanistic insights into FXR-xenobiotic interactions by orthogonal assays.Current research in toxicology · 2022Article
- Farnesoid X receptor alpha (FXRα) is a critical actor of the development and pathologies of the male reproductive system.Cellular and molecular life sciences : CMLS · 2019Review
- Identification of Compounds That Inhibit Estrogen-Related Receptor Alpha Signaling Using High-Throughput Screening Assays.Molecules (Basel, Switzerland) · 2019Article
- Identification of FDA-approved drugs targeting the Farnesoid X Receptor.Scientific reports · 2019Article
- Identification of Modulators That Activate the Constitutive Androstane Receptor From the Tox21 10K Compound Library.Toxicological sciences : an official journal of the Society of Toxicology · 2019Article
- Bioactivity Signatures of Drugs vs. Environmental Chemicals Revealed by Tox21 High-Throughput Screening Assays.Frontiers in big data · 2019Article
- The NCATS BioPlanet - An Integrated Platform for Exploring the Universe of Cellular Signaling Pathways for Toxicology, Systems Biology, and Chemical Genomics.Frontiers in pharmacology · 2019Article
- Comprehensive Analyses and Prioritization of Tox21 10K Chemicals Affecting Mitochondrial Function by in-Depth Mechanistic Studies.Environmental health perspectives · 2018Article
- Confirmation of high-throughput screening data and novel mechanistic insights into VDR-xenobiotic interactions by orthogonal assays.Scientific reports · 2018Article
- Expanding biological space coverage enhances the prediction of drug adverse effects in human using in vitro activity profiles.Scientific reports · 2018Article
- Identification of Estrogen-Related Receptor α Agonists in the Tox21 Compound Library.Endocrinology · 2018Article
- Omics-Based Platform for Studying Chemical Toxicity Using Stem Cells.Journal of proteome research · 2018Article
- Cellular and Biophysical Pipeline for the Screening of Peroxisome Proliferator-Activated Receptor Beta/Delta Agonists: Avoiding False Positives.PPAR research · 2018Article
- Targeting nuclear receptors for the treatment of fatty liver disease.Pharmacology & therapeutics · 2017Review
- Identifying environmental chemicals as agonists of the androgen receptor by using a quantitative high-throughput screening platform.Toxicology · 2017Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 4 institutions in 1 country.
Funding
Abstract
The farnesoid X receptor (FXR) regulates the homeostasis of bile acids, lipids, and glucose. Because endogenous chemicals bind and activate FXR, it is important to examine which xenobiotic compounds would disrupt normal receptor function. We used a cell-based human FXR β-lactamase (Bla) reporter gene assay to profile the Tox21 10K compound collection of environmental chemicals and drugs. Structure-activity relationships of FXR-active compounds revealed by this screening were then compared against the androgen receptor, estrogen receptor α, peroxisome proliferator-activated receptors δ and γ, and the vitamin D receptor. We identified several FXR-active structural classes including anthracyclines, benzimidazoles, dihydropyridines, pyrethroids, retinoic acids, and vinca alkaloids. Microtubule inhibitors potently decreased FXR reporter gene activity. Pyrethroids specifically antagonized FXR transactivation. Anthracyclines affected reporter activity in all tested assays, suggesting non-specific activity. These results provide important information to prioritize chemicals for further investigation, and suggest possible modes of action of compounds in FXR signaling.
Indexed as
Identifiers
What OpenQuestion holds
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.