ArticleACS medicinal chemistry letters2014
Development of novel Vitamin D Receptor-Coactivator Inhibitors.
Article in ACS medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 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.
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
15 citing papers in PubMed, 29 citations in OpenAlex.
- VDR Activation Suppresses Pancreatic Cancer Metastasis Through Inhibition of the ERK Signaling Pathway.Cancers · 2026Article
- Vitamin D Receptor Signaling and Ligand Modulation: Molecular Mechanisms and Therapeutic Implications.International journal of molecular sciences · 2026Review
- Comparative Analyses of the Safety Profiles of Vitamin D Receptor Agonists: A Pharmacovigilance Study Based on the EudraVigilance Database.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Enantioselective synthesis of α-tetrasubstituted (1-indolizinyl) (diaryl)-methanaminesRSC advances · 2024Article
- Enantioselective synthesis of α-tetrasubstituted (3-indolizinyl) (diaryl)methanaminesRSC advances · 2022Article
- Alternative binding sites at the vitamin D receptor and their ligands.Molecular and cellular endocrinology · 2019Review
- Vitamin D Stimulates Cardiomyocyte Proliferation and Controls Organ Size and Regeneration in Zebrafish.Developmental cell · 2019Article
- 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
- Pharmacological use of a novel scaffold, anomeric N,N-diarylamino tetrahydropyran: molecular similarity search, chemocentric target profiling, and experimental evidence.Scientific reports · 2017Article
- 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
- IDENTIFICATION OF VDR ANTAGONISTS AMONG NUCLEAR RECEPTOR LIGANDS USING VIRTUAL SCREENING.Nuclear receptor research · 2014Article
- Developmental exposure of zebrafish to vitamin D receptor acting drugs and environmental toxicants disrupts behavioral function.Neurotoxicology and teratologyArticle
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 1 country.
Funding
Abstract
Nuclear receptor coregulators are master regulators of transcription and selectively interact with the vitamin D receptor (VDR) to modulate cell differentiation, cell proliferation and calcium homeostasis. Herein, we report the syntheses and evaluation of highly potent and selective VDR-coactivator inhibitors based on a recently identified 3-indolylmethanamine scaffold. The most active compound, PS121912, selectively inhibited VDR-mediated transcription among eight other nuclear receptors tested. PS121912 is also selectively disrupting the binding between VDR and the third nuclear receptor interaction domain of the coactivator SRC2. Genetic studies revealed that PS121912 behaves like a VDR antagonist by repressing 1,25-(OH)
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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.