ArticleStructure (London, England : 1993)2011
Helix 11 dynamics is critical for constitutive androstane receptor activity.
Article in Structure (London, England : 1993), 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 26 citations in OpenAlex.
- Genome-wide analysis reveals ligand-dependent allostery in RARα:RXR-mediated transcriptional regulation.Cell reports · 2026Article
- Diindoles produced from commensal microbiota metabolites function as endogenous CAR/Nr1i3 ligands.Nature communications · 2024Article
- Increased Molecular Flexibility Widens the Gap betweenACS medicinal chemistry letters · 2022Article
- Noncanonical Constitutive Androstane Receptor Signaling in Gene Regulation.International journal of molecular sciences · 2020Review
- A molecular switch regulating transcriptional repression and activation of PPARγ.Nature communications · 2020Article
- Drug discovery technologies to identify and characterize modulators of the pregnane X receptor and the constitutive androstane receptor.Drug discovery today · 2019Review
- Defining a conformational ensemble that directs activation of PPARγ.Nature communications · 2018Article
- Allosteric pathways in nuclear receptors - Potential targets for drug design.Pharmacology & therapeutics · 2018Review
- DNA-induced unfolding of the thyroid hormone receptor α A/B domain through allostery.FEBS open bio · 2017Article
- Regulation of PXR and CAR by protein-protein interaction and signaling crosstalk.Expert opinion on drug metabolism & toxicology · 2016Review
- The Promiscuity of Allosteric Regulation of Nuclear Receptors by Retinoid X Receptor.The journal of physical chemistry. B · 2016Article
- Structural mechanism for signal transduction in RXR nuclear receptor heterodimers.Nature communications · 2015Article
- Mapping allostery through computational glycine scanning and correlation analysis of residue-residue contacts.Biochemistry · 2015Article
- Agonist ligands mediate the transcriptional response of nuclear receptor heterodimers through distinct stoichiometric assemblies with coactivators.The Journal of biological chemistry · 2014Article
- Small molecule modulation of nuclear receptor conformational dynamics: implications for function and drug discovery.Molecular pharmacology · 2013Review
- Structural basis for negative cooperativity within agonist-bound TR:RXR heterodimers.Proceedings of the National Academy of Sciences of the United States of America · 2012Article
- Differential hydrogen/deuterium exchange mass spectrometry analysis of protein-ligand interactions.Expert review of proteomics · 2011Review
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
The constitutive androstane receptor (CAR) transactivation can occur in the absence of exogenous ligand and this activity is enhanced by agonists TCPOBOP and meclizine. We use biophysical and cell-based assays to show that increased activity of CAR(TCPOBOP) relative to CAR(meclizine) corresponds to a higher affinity of CAR(TCPOBOP) for the steroid receptor coactivator-1. Additionally, steady-state fluorescence spectra suggest conformational differences between CAR(TCPOBOP):RXR and CAR(meclizine):RXR. Hydrogen/deuterium exchange (HDX) data indicate that the CAR activation function 2 (AF-2) is more stable in CAR(TCPOBOP):RXR and CAR(meclizine):RXR than in CAR:RXR. HDX kinetics also show significant differences between CAR(TCPOBOP):RXR and CAR(meclizine):RXR. Unlike CAR(meclizine):RXR, CAR(TCPOBOP):RXR shows a higher overall stabilization that extends into RXR. We identify residues 339-345 in CAR as an allosteric regulatory site with a greater magnitude reduction in exchange kinetics in CAR(TCPOBOP):RXR than CAR(meclizine):RXR. Accordingly, assays with mutations on CAR at leucine-340 and leucine-343 confirm this region as an important determinant of CAR activity.
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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.