ArticleJournal of medicinal chemistry2012
Discovery of the first irreversible small molecule inhibitors of the interaction between the vitamin D receptor and coactivators.
Article in Journal of medicinal chemistry, 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
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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
22 citing papers in PubMed, 46 citations in OpenAlex.
- PFAS:VDR interactions and immunotoxicity through disruption of monocyte differentiation.Archives of toxicology · 2026Article
- Developing novel indoles as antitubercular agents and simulated annealing-based analysis of their binding with MmpL3.Future medicinal chemistry · 2025Article
- Characterization of allosteric modulators that disrupt androgen receptor co-activator protein-protein interactions to alter transactivation-Drug leads for metastatic castration resistant prostate cancer.SLAS discovery : advancing life sciences R & D · 2023Article
- Biological evaluation and synthesis of calcitroic acid.Bioorganic chemistry · 2021Review
- Steroid receptor/coactivator binding inhibitors: An update.Molecular and cellular endocrinology · 2019Review
- Alternative binding sites at the vitamin D receptor and their ligands.Molecular and cellular endocrinology · 2019Review
- Molecular Dynamics Simulations Revealed the Regulation of Ligands to the Interactions between Androgen Receptor and Its Coactivator.Journal of chemical information and modeling · 2018Article
- Confirmation of high-throughput screening data and novel mechanistic insights into VDR-xenobiotic interactions by orthogonal assays.Scientific reports · 2018Article
- Novel VDR antagonists based on the GW0742 scaffold.Bioorganic & medicinal chemistry letters · 2018Article
- Parallel Chemistry Approach to Identify Novel Nuclear Receptor Ligands Based on the GW0742 Scaffold.ACS combinatorial science · 2017Article
- Fluorescence polarization assays in high-throughput screening and drug discovery: a review.Methods and applications in fluorescence · 2016Article
- Avoiding Fluorescence Assay Interference-The Case for Diaphorase.Assay and drug development technologies · 2016Review
- Synthesis and evaluation of vitamin D receptor-mediated activities of cholesterol and vitamin D metabolites.European journal of medicinal chemistry · 2016Article
- Inhibitors for the Vitamin D Receptor-Coregulator Interaction.Vitamins and hormones · 2016Review
- Antitumor Activity of 3-Indolylmethanamines 31B and PS121912.Anticancer research · 2015Article
- Anticancer activity of VDR-coregulator inhibitor PS121912.Cancer chemotherapy and pharmacology · 2014Article
- Development of novel Vitamin D Receptor-Coactivator Inhibitors.ACS medicinal chemistry letters · 2014Article
- IDENTIFICATION OF VDR ANTAGONISTS AMONG NUCLEAR RECEPTOR LIGANDS USING VIRTUAL SCREENING.Nuclear receptor research · 2014Article
- Modulation of Transcription mediated by the Vitamin D Receptor and the Peroxisome Proliferator-Activated Receptor δ in the presence of GW0742 analogs.Journal of biomolecular research & therapeutics · 2014Article
- High-throughput identification of promiscuous inhibitors from screening libraries with the use of a thiol-containing fluorescent probe.Journal of biomolecular screening · 2013Article
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 1 country.
Funding
Abstract
The vitamin D receptor (VDR) is a nuclear hormone receptor that regulates cell proliferation, cell differentiation, and calcium homeostasis. The receptor is activated by vitamin D analogues that induce the disruption of VDR-corepressor binding and promote VDR-coactivator interactions. The interactions between VDR and coregulators are essential for VDR-mediated transcription. Small molecule inhibition of VDR-coregulator binding represents an alternative method to the traditional ligand-based approach in order to modulate the expression of VDR target genes. A high throughput fluorescence polarization screen that quantifies the inhibition of binding between VDR and a fluorescently labeled steroid receptor coactivator 2 peptide was applied to discover the new small molecule VDR-coactivator inhibitors, 3-indolylmethanamines. Structure-activity relationship studies with 3-indolylmethanamine analogues were used to determine their mode of VDR-binding and to produce the first VDR-selective and irreversible VDR-coactivator inhibitors with the ability to regulate the transcription of the human VDR target gene TRPV6.
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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.