ArticleStructure (London, England : 1993)2012
Crystal structures of a stabilized β1-adrenoceptor bound to the biased agonists bucindolol and carvedilol.
Article in Structure (London, England : 1993), 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 99 papers.
What it found
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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
99 citing papers in PubMed, 222 citations in OpenAlex.
- Comparative analysis of ligand binding affinities and functional profiles at recombinant human β-adrenergic receptor subtypes 1, 2, and 3.The Journal of pharmacology and experimental therapeutics · 2026Review
- Structural Mechanism of an Efficacy Photoswitch Targeting the βAngewandte Chemie (International ed. in English) · 2026Article
- βmedRxiv : the preprint server for health sciences · 2025Article
- Ligand-induced conformational changes in the β1-adrenergic receptor revealed by hydrogen-deuterium exchange mass spectrometry.Nature communications · 2024Article
- Carvedilol Activates a Myofilament Signaling Circuitry to Restore Cardiac Contractility in Heart Failure.JACC. Basic to translational science · 2024Article
- GOLEM: Automated and Robust Cryo-EM-Guided Ligand Docking with Explicit Water Molecules.Journal of chemical information and modeling · 2024Article
- G Protein-Coupled Receptor-Ligand Pose and Functional Class Prediction.International journal of molecular sciences · 2024Article
- Genetic Variants of Adrenoceptors.Handbook of experimental pharmacology · 2024Review
- Structures of Adrenoceptors.Handbook of experimental pharmacology · 2024Review
- IUPHAR themed review: Opioid efficacy, bias, and selectivity.Pharmacological research · 2023Review
- A Novel "Activation Switch" Motif Common to All Aminergic Receptors.Journal of chemical information and modeling · 2023Review
- Article
- Caged-carvedilol as a new tool for visible-light photopharmacology of β-adrenoceptors in native tissues.iScience · 2022Article
- Gi-protein-coupled βActa biochimica et biophysica Sinica · 2022Review
- Conformational selection guides β-arrestin recruitment at a biased G protein-coupled receptor.Science (New York, N.Y.) · 2022Article
- Structural basis of GPCR coupling to distinct signal transducers: implications for biased signaling.Trends in biochemical sciences · 2022Review
- Discovery of a functionally selective ghrelin receptor (GHSRProceedings of the National Academy of Sciences of the United States of America · 2022Article
- Sequence coevolution and structure stabilization modulate olfactory receptor expression.Biophysical journal · 2022Article
- Adrenergic receptors gene polymorphisms and autonomic nervous control of heart and vascular tone.Physiological research · 2021Review
- Article
39 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The β(1)-adrenoceptor (β(1)AR) is the site of action of beta blockers used in the treatment of cardiac-related illnesses. Two beta blockers, carvedilol and bucindolol, show distinctive activities compared to other beta blockers and have been proposed as treatments tailored to the Arg/Gly389(8.56) polymorphism of the human β(1)AR. Both carvedilol and bucindolol are classified as biased agonists, because they stimulate G protein-independent signaling, while acting as either inverse or partial agonists of the G protein pathway. We have determined the crystal structures of a thermostabilized avian β(1)AR mutant bound to bucindolol and to carvedilol at 3.2 and 2.3 Å resolution, respectively. In comparison to other beta blockers, bucindolol and carvedilol interact with additional residues, in extracellular loop 2 and transmembrane helix 7, which may promote G protein-independent signaling. The structures also suggest that there may be a structural explanation for the pharmacological differences arising from the Arg/Gly389(8.56) polymorphism.
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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.