ArticleAssay and drug development technologies2009
Identification of pregnane X receptor ligands using time-resolved fluorescence resonance energy transfer and quantitative high-throughput screening.
Article in Assay and drug development technologies, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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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.
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Who cites it
27 citing papers in PubMed, 62 citations in OpenAlex.
- Chemical Screening of Nuclear Receptor Modulators.International journal of molecular sciences · 2020Review
- Targeting the pregnane X receptor using microbial metabolite mimicry.EMBO molecular medicine · 2020Article
- Drug discovery technologies to identify and characterize modulators of the pregnane X receptor and the constitutive androstane receptor.Drug discovery today · 2019Review
- Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.PloS one · 2019Article
- Using TR-FRET to Investigate Protein-Protein Interactions: A Case Study of PXR-Coregulator Interaction.Advances in protein chemistry and structural biology · 2018Review
- High-Throughput Screening Identifies 1,4,5-Substituted 1,2,3-Triazole Analogs as Potent and Specific Antagonists of Pregnane X Receptor.Assay and drug development technologies · 2017Article
- Quantitative High-Throughput Screening Using a Coincidence Reporter Biocircuit.Current protocols in neuroscience · 2017Article
- Mechanisms of xenobiotic receptor activation: Direct vs. indirect.Biochimica et biophysica acta · 2016Review
- Targeting xenobiotic receptors PXR and CAR in human diseases.Drug discovery today · 2015Review
- Estrogen receptor alpha/co-activator interaction assay: TR-FRET.Methods in molecular biology (Clifton, N.J.) · 2015Article
- Molecular characterization of PXR and two sulfotransferases and hepatic transcripts of PXR, two sulfotransferases and CYP3A responsive to bisphenol A in rare minnow Gobiocypris rarus.Molecular biology reports · 2014Article
- Development of BODIPY FL vindoline as a novel and high-affinity pregnane X receptor fluorescent probe.Bioconjugate chemistry · 2014Article
- Targeting nuclear receptors with marine natural products.Marine drugs · 2014Review
- A vinblastine fluorescent probe for pregnane X receptor in a time-resolved fluorescence resonance energy transfer assay.Analytical biochemistry · 2013Article
- Differential regulation of CYP3A4 promoter activity by a new class of natural product derivatives binding to pregnane X receptor.Biochemical pharmacology · 2013Article
- Physicochemical characterization of a thermostable alcohol dehydrogenase from Pyrobaculum aerophilum.PloS one · 2013Article
- Article
- Firefly luciferase in chemical biology: a compendium of inhibitors, mechanistic evaluation of chemotypes, and suggested use as a reporter.Chemistry & biology · 2012Article
- Titration-based screening for evaluation of natural product extracts: identification of an aspulvinone family of luciferase inhibitors.Chemistry & biology · 2011Article
- A quantitative high-throughput screen identifies novel inhibitors of the interaction of thyroid receptor beta with a peptide of steroid receptor coactivator 2.Journal of biomolecular screening · 2011Article
Corrections and comments
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Authors and funding
13 authors at 2 institutions in 1 country.
Funding
Abstract
The human pregnane X nuclear receptor (PXR) is a xenobiotic-regulated receptor that is activated by a range of diverse chemicals, including antibiotics, antifungals, glucocorticoids, and herbal extracts. PXR has been characterized as an important receptor in the metabolism of xenobiotics due to induction of cytochrome P450 isozymes and activation by a large number of prescribed medications. Developing methodologies that can efficiently detect PXR ligands will be clinically beneficial to avoid potential drug-drug interactions. To facilitate the identification of PXR ligands, a time-resolved fluorescence resonance energy transfer (TR-FRET) assay was miniaturized to a 1,536-well microtiter plate format to employ quantitative high-throughput screening (qHTS). The optimized 1,536-well TR-FRET assay showed Z'-factors of >or=0.5. Seven- to 15-point concentration-response curves (CRCs) were generated for 8,280 compounds using both terbium and fluorescein emission data, resulting in the generation of 241,664 data points. The qHTS method allowed us to retrospectively examine single concentration screening datasets to assess the sensitivity and selectivity of the PXR assay at different compound screening concentrations. Furthermore, nonspecific assay artifacts such as concentration-based quenching of the terbium signal and compound fluorescence were identified through the examination of CRCs for specific emission channels. The CRC information was also used to define chemotypes associated with PXR ligands. This study demonstrates the feasibility of profiling thousands of compounds against PXR using the TR-FRET assay in a high-throughput format.
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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.