ArticleThe Journal of biological chemistry2011
Danthron functions as a retinoic X receptor antagonist by stabilizing tetramers of the receptor.
Article in The Journal of biological chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 55 citations in OpenAlex.
- Retinoid-X receptor action and disruption in development.Developmental biology · 2026Review
- Redistribution of super-enhancers promotes malignancy in human hepatocellular carcinoma.Journal of advanced research · 2026Article
- Simple Fluorescence Labeling Method Enables Detection of Intracellular Distribution and Expression Level of Retinoid X Receptors.ACS medicinal chemistry letters · 2024Article
- ZebrafishFrontiers in cell and developmental biology · 2024Article
- Article
- Review
- Farnesoid X receptor: a potential therapeutic target in multiple organs.Histology and histopathology · 2020Review
- A revisited version of the apo structure of the ligand-binding domain of the human nuclear receptor retinoic X receptor α.Acta crystallographica. Section F, Structural biology communications · 2019Article
- Retinoid X Receptor Antagonists.International journal of molecular sciences · 2018Review
- Identification of danthron as an isoform-specific inhibitor of HEME OXYGENASE-1/cytochrome P450 reductase interaction with anti-tumor activity.Journal of biomedical science · 2018Article
- Overview of the structure-based non-genomic effects of the nuclear receptor RXRα.Cellular & molecular biology letters · 2018Review
- Modulation of nongenomic activation of PI3K signalling by tetramerization of N-terminally-cleaved RXRα.Nature communications · 2017Article
- Antagonist-perturbation mechanism for activation function-2 fixed motifs: active conformation and docking mode of retinoid X receptor antagonists.Journal of computer-aided molecular design · 2017Article
- Targeting truncated RXRα for cancer therapy.Acta biochimica et biophysica Sinica · 2016Review
- NSC-640358 acts as RXRα ligand to promote TNFα-mediated apoptosis of cancer cell.Protein & cell · 2015Article
- Regulation of the nongenomic actions of retinoid X receptor-α by targeting the coregulator-binding sites.Acta pharmacologica Sinica · 2015Review
- Latanoprost effectively ameliorates glucose and lipid disorders in db/db and ob/ob mice.Diabetologia · 2013Article
- Danthron activates AMP-activated protein kinase and regulates lipid and glucose metabolism in vitro.Acta pharmacologica Sinica · 2013Article
- Synthesis and SAR study of modulators inhibiting tRXRα-dependent AKT activation.European journal of medicinal chemistry · 2013Article
- Danthron triggers ROS and mitochondria-mediated apoptotic death in C6 rat glioma cells through caspase cascades, apoptosis-inducing factor and endonuclease G multiple signaling.Neurochemical research · 2012Article
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Retinoic X receptor (RXR) is a promising target for drug discovery against cancer and metabolic syndromes. Here, we identified a specific RXRα antagonist, danthron, from the traditional Chinese medicine rhubarb. Danthron repressed all tested RXRα-involved response element transcription, including the RXRE, PPRE, FXRE, and LXRE. Results from native PAGE and isothermal titration calorimetry (ITC)-based assays indicated that danthron bound to the tetrameric RXRα-LBD in a specific stoichimetric ratio, and such a binding could influence the corepressor SMRT affinity to the receptor. Additionally, a unique tetrameric structure of the apo-RXRα ligand-binding domain (LBD) was determined, which exhibited a larger tetramer interface and different ligand-binding pocket size compared with the one previously reported. Together with the biochemical and biophysical results, the determined crystal structure of danthron-soaked RXRα-LBD suggested a new mechanism for danthron antagonism to tetrameric RXRα. Moreover, the in vivo efficient improvement of insulin sensitivity by danthron was observed in diet-induced obese (DIO) mice. Thus, our findings were expected to supply new insights into the structural basis of RXRα antagonist for its further potential therapeutic application.
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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.