ArticleNuclear receptor signaling2012
Use of differential scanning fluorimetry as a high-throughput assay to identify nuclear receptor ligands.
Article in Nuclear receptor signaling, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 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
22 citing papers in PubMed, 41 citations in OpenAlex.
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- Aurora 2.0: A fluorogenic dye library for expanding the capability of protein-adaptive differential scanning fluorimetry (paDSF).SLAS discovery : advancing life sciences R & D · 2025Article
- Structural insights into peptidoglycan glycosidase EtgA binding to the inner rod protein EscI of the type III secretion system via a designed EscI-EtgA fusion protein.Protein science : a publication of the Protein Society · 2024Article
- Thermal unfolding methods in drug discovery.Biophysics reviews · 2023Review
- Biophysical and pharmacokinetic characterization of a small-molecule inhibitor of RUNX1/ETO tetramerization with anti-leukemic effects.Scientific reports · 2022Article
- Nanoscale, automated, high throughput synthesis and screening for the accelerated discovery of protein modifiers.RSC medicinal chemistry · 2021Article
- Target-Directed Approaches for Screening Small Molecules against RNA Targets.SLAS discovery : advancing life sciences R & D · 2020Review
- Selective Modulation of Dynamic Protein Complexes.Cell chemical biology · 2020Review
- Chemical Screening of Nuclear Receptor Modulators.International journal of molecular sciences · 2020Review
- Fluorescence-based investigations of RNA-small molecule interactions.Methods (San Diego, Calif.) · 2019Article
- Comparative analysis of xenobiotic metabolising N-acetyltransferases from ten non-human primates as in vitro models of human homologues.Scientific reports · 2018Article
- Cellular and Biophysical Pipeline for the Screening of Peroxisome Proliferator-Activated Receptor Beta/Delta Agonists: Avoiding False Positives.PPAR research · 2018Article
- Affinity purification with metabolomic and proteomic analysis unravels diverse roles of nucleoside diphosphate kinases.Journal of experimental botany · 2017Article
- An APE1 inhibitor reveals critical roles of the redox function of APE1 in KSHV replication and pathogenic phenotypes.PLoS pathogens · 2017Article
- Capture compound mass spectrometry--a powerful tool to identify novel c-di-GMP effector proteins.Journal of visualized experiments : JoVE · 2015Article
- Identification and structure-function analysis of subfamily selective G protein-coupled receptor kinase inhibitors.ACS chemical biology · 2015Article
- ROR nuclear receptors: structures, related diseases, and drug discovery.Acta pharmacologica Sinica · 2015Review
- In silico identification and pharmacological evaluation of novel endocrine disrupting chemicals that act via the ligand-binding domain of the estrogen receptor α.Toxicological sciences : an official journal of the Society of Toxicology · 2014Article
- A screening cascade to identify ERβ ligands.Nuclear receptor signaling · 2014Article
- In silico docking of forchlorfenuron (FCF) to septins suggests that FCF interferes with GTP binding.PloS one · 2014Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Identification of ligands that interact with nuclear receptors is both a major biological problem and an important initial step in drug discovery. Several in vitro and in vivo techniques are commonly used to screen ligand candidates against nuclear receptors; however, none of the current assays allow screening without modification of either the protein and/or the ligand in a high-throughput fashion. Differential scanning fluorimetry (DSF) allows unmodified potential ligands to be screened as 10µL reactions in 96-well format against partially purified protein, revealing specific interactors. As a proof of principle, we used a commercially-available nuclear receptor ligand candidate chemical library to identify interactors of the human estrogen receptor α ligand binding domain (ERα LBD). Compounds that interact specifically with ERα LBD stabilize the protein and result in an elevation of the thermal denaturation point, as monitored by the environmentally-sensitive dye SYPRO orange. We successfully identified all three compounds in the library that have previously been identified to interact with ERα, with no false positive results.
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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.