ArticleChemistry & biology2014
Sulindac-derived RXRα modulators inhibit cancer cell growth by binding to a novel site.
Article in Chemistry & biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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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.
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.
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Who cites it
19 citing papers in PubMed.
- Synthesis and Biological Evaluation of Marine-Inspired Benzothiazole Derivatives as Retinoid X Receptor-α Antagonists with Anti-Cancer Activities.Marine drugs · 2025Article
- RXRActa pharmaceutica Sinica. B · 2025Article
- α-Mangostin Induces Apoptosis and Inhibits Metastasis of Breast Cancer Cells via Regulating RXRα-AKT Signaling Pathway.Frontiers in pharmacology · 2021Article
- Delineation of the molecular determinants of the unique allosteric binding site of the orphan nuclear receptor RORγt.The Journal of biological chemistry · 2020Article
- Sulindac-derived retinoid X receptor-α modulator attenuates atherosclerotic plaque progression and destabilization in ApoEBritish journal of pharmacology · 2019Article
- BI1071, a Novel Nur77 Modulator, Induces Apoptosis of Cancer Cells by Activating the Nur77-Bcl-2 Apoptotic Pathway.Molecular cancer therapeutics · 2019Article
- Discovery of atorvastatin as a tetramer stabilizer of nuclear receptor RXRα through structure-based virtual screening.Bioorganic chemistry · 2019Article
- Oncogenic potential of truncated RXRα during colitis-associated colorectal tumorigenesis by promoting IL-6-STAT3 signaling.Nature communications · 2019Article
- Tetrazoles via Multicomponent Reactions.Chemical reviews · 2019Review
- 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
- LncRNA DANCR upregulates PI3K/AKT signaling through activating serine phosphorylation of RXRA.Cell death & disease · 2018Article
- Retinoid X Receptor Antagonists.International journal of molecular sciences · 2018Review
- Overview of the structure-based non-genomic effects of the nuclear receptor RXRα.Cellular & molecular biology letters · 2018Review
- Article
- Modulation of nongenomic activation of PI3K signalling by tetramerization of N-terminally-cleaved RXRα.Nature communications · 2017Article
- Celastrol-Induced Nur77 Interaction with TRAF2 Alleviates Inflammation by Promoting Mitochondrial Ubiquitination and Autophagy.Molecular cell · 2017Article
- Targeting truncated RXRα for cancer therapy.Acta biochimica et biophysica Sinica · 2016Review
- Nitrostyrene Derivatives Act as RXRα Ligands to Inhibit TNFα Activation of NF-κB.Cancer research · 2015Article
- Regulation of the nongenomic actions of retinoid X receptor-α by targeting the coregulator-binding sites.Acta pharmacologica Sinica · 2015Review
Corrections and comments
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Authors and funding
17 authors.
Funding
Abstract
Retinoid X receptor-alpha (RXRα), an intriguing and unique drug target, can serve as an intracellular target mediating the anticancer effects of certain nonsteroidal anti-inflammatory drugs (NSAIDs), including sulindac. We report the synthesis and characterization of two sulindac analogs, K-8008 and K-8012, which exert improved anticancer activities over sulindac in a RXRα-dependent manner. The analogs inhibit the interaction of the N-terminally truncated RXRα (tRXRα) with the p85α subunit of PI3K, leading to suppression of AKT activation and induction of apoptosis. Crystal structures of the RXRα ligand-binding domain (LBD) with K-8008 or K-8012 reveal that both compounds bind to tetrameric RXRα LBD at a site different from the classical ligand-binding pocket. Thus, these results identify K-8008 and K-8012 as tRXRα modulators and define a binding mechanism for regulating the nongenomic action of tRXRα.
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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.