ArticleBioorganic & medicinal chemistry2013
Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery.
Article in Bioorganic & medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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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
14 citing papers in PubMed, 23 citations in OpenAlex.
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- Development of BODIPY FL SNS 032 as a Versatile Probe for Constitutive Androstane Receptor and Multiple Kinases.ACS medicinal chemistry letters · 2024Article
- Chemogenomics for NR1 nuclear hormone receptors.Nature communications · 2024Article
- Chemical Screening of Nuclear Receptor Modulators.International journal of molecular sciences · 2020Review
- AutophagySMDB: a curated database of small molecules that modulate protein targets regulating autophagy.Autophagy · 2019Article
- Identification of FDA-approved drugs targeting the Farnesoid X Receptor.Scientific reports · 2019Article
- Synthesis and biological evaluation of novel SIPI-7623 derivatives as farnesoid X receptor (FXR) antagonists.Molecular diversity · 2019Article
- Antitumor activity of novel pyrazole-based small molecular inhibitors of the STAT3 pathway in patient derived high grade glioma cells.PloS one · 2019Article
- Alteration of RNA Splicing by Small-Molecule Inhibitors of the Interaction between NHP2L1 and U4.SLAS discovery : advancing life sciences R & D · 2018Article
- Differential modulation of FXR activity by chlorophacinone and ivermectin analogs.Toxicology and applied pharmacology · 2016Article
- CINPA1 is an inhibitor of constitutive androstane receptor that does not activate pregnane X receptor.Molecular pharmacology · 2015Article
- Nuclear bile acid signaling through the farnesoid X receptor.Cellular and molecular life sciences : CMLS · 2015Review
- Quantitative high-throughput profiling of environmental chemicals and drugs that modulate farnesoid X receptor.Scientific reports · 2014Article
- Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor.Bioorganic & medicinal chemistry · 2014Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
FXR (farnesoid X receptor, NRIH4), a nuclear receptor, plays a major role in the control of cholesterol metabolism. FXR ligands have been investigated in preclinical studies for targeted therapy against metabolic diseases, but have shown limitations. Therefore, there is a need for new agonist or antagonist ligands of FXR, both for potential clinical applications, as well as to further elucidate its biological functions. Here we describe the use of the X-ray crystal structure of FXR complexed with the potent small molecule agonist GW4064 to design and synthesize a novel fluorescent, high-affinity probe (DY246) for time resolved fluorescence resonance energy transfer (TR-FRET) assays. We then used the TR-FRET assay for high throughput screening of a library of over 5000 bioactive compounds. From this library, we identified 13 compounds that act as putative FXR transcriptional antagonists.
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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.