ArticleEMBO reports2004
Rational design of RAR-selective ligands revealed by RARbeta crystal stucture.
Article in EMBO reports, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers, 1 of them a synthesis that pooled it.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
30 citing papers in PubMed, 1 synthesis or guideline pooled it, 86 citations in OpenAlex.
- Exploring the interactions of antihistamine with retinoic acid receptor beta (RARB) by molecular dynamics simulations and genome-wide meta-analysis.Journal of molecular graphics & modelling · 2023Pooled it
- New Fluorescent Synthetic Retinoids as Potential RAR Agonists with Anticancer, Molecular Docking and ADME Assessments.Journal of fluorescence · 2025Article
- Development of the retinoic acid receptor alpha-specific antagonist YCT-529 for male contraception: A brief review.Contraception · 2025Review
- Article
- Structural overview and perspectives of the nuclear receptors, a major family as the direct targets for small-molecule drugs.Acta biochimica et biophysica Sinica · 2022Article
- Recent advances in the design of RAR α and RAR β agonists as orally bioavailable drugs. A review.Bioorganic & medicinal chemistry · 2020Review
- Article
- Retinoic acid receptor antagonists for male contraception: current status†.Biology of reproduction · 2020Review
- Regulation of RXR-RAR Heterodimers by RXR- and RAR-Specific Ligands and Their Combinations.Cells · 2019Article
- Probing biological activity through structural modelling of ligand-receptor interactions of 2,4-disubstituted thiazole retinoids.Bioorganic & medicinal chemistry · 2018Article
- The molecular basis of the interactions between synthetic retinoic acid analogues and the retinoic acid receptors.MedChemComm · 2017Article
- Article
- Nuclear retinoid receptors and pregnancy: placental transfer, functions, and pharmacological aspects.Cellular and molecular life sciences : CMLS · 2016Review
- Evolutionary diversification of retinoic acid receptor ligand-binding pocket structure by molecular tinkering.Royal Society open science · 2016Article
- Aldo-Keto Reductase Family 1 Member B10 Inhibitors: Potential Drugs for Cancer Treatment.Recent patents on anti-cancer drug discovery · 2016Review
- An Unexpected Mode Of Binding Defines BMS948 as A Full Retinoic Acid Receptor β (RARβ, NR1B2) Selective Agonist.PloS one · 2015Article
- Coactivator recruitment of AhR/ARNT1.International journal of molecular sciences · 2014Review
- Dual RXR Agonists and RAR Antagonists Based on the Stilbene Retinoid Scaffold.ACS medicinal chemistry letters · 2014Article
- Retinoic acid actions through mammalian nuclear receptors.Chemical reviews · 2014Review
- Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
13 authors at 5 institutions in 4 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The crystal structure of the ligand-binding domain of RARbeta, a suspect tumour suppressor, reveals important features that distinguish it from the two other RAR isotypes. The most striking difference is an extra cavity allowing RARbeta to bind more bulky agonists. Accordingly, we identified a ligand that shows RARbeta selectivity with a 100-fold higher affinity to RARbeta than to alpha or gamma isotypes. The structural differences between the three RAR ligand-binding pockets revealed a rationale explaining how a single retinoid can be at the same time an RARalpha, gamma antagonist and an RARbeta agonist. In addition, we demonstrate how to generate an RARbeta antagonist by gradually modifying the bulkiness of a single substitution. Together, our results provide structural guidelines for the synthesis of RARbeta-selective agonists and antagonists, allowing for the first time to address pharmacologically the tumour suppressor role of RARbeta in vitro and in animal models.
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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.