ArticlePloS one2011
Differential modulation of Beta-adrenergic receptor signaling by trace amine-associated receptor 1 agonists.
Article in PloS one, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 55 citations in OpenAlex.
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- Toxic Effect of Fullerene and Its Derivatives upon the Transmembrane βMolecules (Basel, Switzerland) · 2022Article
- The Ambivalent Role of Skin Microbiota and Adrenaline in Wound Healing and the Interplay between Them.International journal of molecular sciences · 2021Review
- Trace amines produced by skin bacteria accelerate wound healing in mice.Communications biology · 2020Article
- Zinc-α2-glycoprotein as an inhibitor of amine oxidase copper-containing 3.Open biology · 2020Article
- 3-Iodothyronamine and Derivatives: New Allies Against Metabolic Syndrome?International journal of molecular sciences · 2020Review
- TAAR Agonists.Cellular and molecular neurobiology · 2020Review
- Methamphetamine Activates Trace Amine Associated Receptor 1 to Regulate Astrocyte Excitatory Amino Acid Transporter-2 via Differential CREB Phosphorylation During HIV-Associated Neurocognitive Disorders.Frontiers in neurology · 2020Article
- Differential mechanisms of action of the trace amines octopamine, synephrine and tyramine on the porcine coronary and mesenteric artery.Scientific reports · 2019Article
- Accelerated pseudogenization of trace amine-associated receptor genes in primates.Genes, brain, and behavior · 2019Article
- Non-Functional Trace Amine-Associated Receptor 1 Variants in Patients With Mental Disorders.Frontiers in pharmacology · 2019Article
- 3-Iodothyronamine Activates a Set of Membrane Proteins in Murine Hypothalamic Cell Lines.Frontiers in endocrinology · 2018Article
- The Trace Amine-Associated Receptor 1 Agonist 3-Iodothyronamine Induces Biased Signaling at the Serotonin 1b Receptor.Frontiers in pharmacology · 2018Article
- Striatal Tyrosine Hydroxylase Is Stimulated via TAAR1 by 3-Iodothyronamine, But Not by Tyramine or β-Phenylethylamine.Frontiers in pharmacology · 2018Article
- 3-Iodothyronamine, a Novel Endogenous Modulator of Transient Receptor Potential Melastatin 8?Frontiers in endocrinology · 2017Review
- Investigation of Naturally Occurring Single-Nucleotide Variants in Human TAAR1.Frontiers in pharmacology · 2017Article
- Discovery and Characterization of 2-Aminooxazolines as Highly Potent, Selective, and Orally Active TAAR1 Agonists.ACS medicinal chemistry letters · 2016Article
- Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Trace amine-associated receptors (TAAR) are rhodopsin-like G-protein-coupled receptors (GPCR). TAAR are involved in modulation of neuronal, cardiac and vascular functions and they are potentially linked with neurological disorders like schizophrenia and Parkinson's disease. Subtype TAAR1, the best characterized TAAR so far, is promiscuous for a wide set of ligands and is activated by trace amines tyramine (TYR), phenylethylamine (PEA), octopamine (OA), but also by thyronamines, dopamine, and psycho-active drugs. Unfortunately, effects of trace amines on signaling of the two homologous β-adrenergic receptors 1 (ADRB1) and 2 (ADRB2) have not been clarified yet in detail. We, therefore, tested TAAR1 agonists TYR, PEA and OA regarding their effects on ADRB1/2 signaling by co-stimulation studies. Surprisingly, trace amines TYR and PEA are partial allosteric antagonists at ADRB1/2, whereas OA is a partial orthosteric ADRB2-antagonist and ADRB1-agonist. To specify molecular reasons for TAAR1 ligand promiscuity and for observed differences in signaling effects on particular aminergic receptors we compared TAAR, tyramine (TAR) octopamine (OAR), ADRB1/2 and dopamine receptors at the structural level. We found especially for TAAR1 that the remarkable ligand promiscuity is likely based on high amino acid similarity in the ligand-binding region compared with further aminergic receptors. On the other hand few TAAR specific properties in the ligand-binding site might determine differences in ligand-induced effects compared to ADRB1/2. Taken together, this study points to molecular details of TAAR1-ligand promiscuity and identified specific trace amines as allosteric or orthosteric ligands of particular β-adrenergic receptor subtypes.
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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.