Structure, Function, and Regulation of the Three β‐Adrenergic Receptors
Open accessAbstract
Three β‐adrenergic receptor subtypes are now known to be functionally expressed in mammals. All three belong to the R 7 G family of receptors coupled to G‐proteins, and characterized by an extracellular glycosylated N‐terminal and an intracellular C‐terminal region and seven transmembrane domains, linked by three exta‐ and three intracellular loops. The catecholamine ligand binding domain, studied using affinity‐labeling and site‐directed mutagenesis, is a pocket lined by residues belonging to the transmembrane domains. The region responsible for the interaction with the Gs protein which, when activated, stimulates adenylyl cyclase, is composed of residues belonging to the parts most proximal to the membrane of intracellular loop i 3 and the C‐terminal region. The pharmacology of the three subtypes is quite distinct: in fact most of the potent β 1/β 2 antagonists (the well known β blockers) act as agonists on β 3. The subtype is resistant to short‐term desensitization mediated by phosphorylation through PKA or βARK, in stark contrast to the β 1 or β 2 subtypes. Various compounds (dexamethasone, butyrate, insulin) up regulate β 1 or β 1 subtypes while down‐regulating β 3 whose expression strictly correlates with differentiation of 3T3‐F442A fibroblasts into adipocytes, thus confirming that the expression of the three subtypes may each be regulated independently to exert a specific physiologic role in different tissues or at different stages of development.
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The α1 adrenergic receptors mediate endogenous functions of catecholamines, which involve coupling to G proteins followed by activation of phospholipase Cβ and protein kinase C.
“The α1 adrenergic receptors mediate endogenous functions of catecholamines, which involve coupling to G proteins followed by activation of phospholipase Cβ and protein kinase C 31.”
From Akt-dependent anabolic activity of natural and synthetic brassinosteroids in rat skeletal muscle cells (2011) · cites this paper as [31]
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Psychedelics in Psychiatry: Neuroplastic, Immunomodulatory, and Neurotransmitter Mechanisms
Inserra, A., De Gregorio, D., & Gobbi, G. (2021) · Pharmacological Reviews · doi:10.1124/pharmrev.120.000056 · Cited by 232 · see citing works
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- Authors
- Strosberg, A. D.
- Affiliations
- Centre National de la Recherche Scientifique (FR)
- Corresponding author
- Strosberg, A. Donny
- Venue
- Obesity Research
- Publisher
- Wiley
- Published
- 1995-11
- Volume
- 3
- Issue
- S4
- Pages
- 501S-505S
- ISSN
- 1071-7323 (ISSN-L)
- 1550-8528
- OpenAlex
- W2150629018
- Cited by
- 24
- References
- 28
- Citations by year
- 2023: 1 · 2020: 5 · 2013: 1 · 2012: 1
- FWCI
- 0.09
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Obesity Research (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Health Sciences › Medicine › Physiology › Adipose Tissue and Metabolism
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
- Keywords
- beta-adrenergic receptors, beta3-adrenergic receptor, beta1-adrenergic receptor, beta2-adrenergic receptor, G protein-coupled receptors, receptor structure, ligand-binding domain, Gs protein coupling, adenylate cyclase, beta-blockers, receptor desensitization, receptor phosphorylation, receptor up-regulation, adipogenesis, dexamethasone, butyrate, insulin
- MeSH terms
- Amino Acid Sequence, Animals, Homeostasis, Humans, Molecular Sequence Data, Receptors, Adrenergic, beta, Gene Expression
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