Beta-3 adrenergic receptor
Also known as: ADRB3, ADRB3R, B3AR
Function
G protein-coupled receptor for catecholamines that couples to both G(s) and G(i) proteins, leading to either activation or inhibition of adenylate cyclase and cAMP-dependent pathway, respectively. The rank order of potency for physiological agonists is norepinephrine > epinephrine. Involved in the regulation of thermogenesis and lipolysis in brown and white adipose tissue, after coupling to G(s) proteins and stimulation of the cAMP-PKA axis (By similarity). Also activates lipolytic process by coupling to G(i) proteins and consequent initiation of the ERK1/2 MAP kinase cascade. Participates in relaxation of the blood vessels and the urinary bladder. Also mediates negative inotropic effects in cardiomyocytes through activation of an NO synthase pathway and subsequent increase in cGMP levels, possibly involving G(i/o) protein-mediated coupling.
Classification
- Family (Pfam)
- PF00001 7tm_1
- InterPro
- ADR_fam, ADRB3_rcpt, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM
- Functional cluster
- G Protein-Coupled Receptors
Experimental structures · PDB · 2
A predicted model is available from AlphaFold.
Gene Ontology · 25
- GO:0005886 plasma membrane
- GO:0043235 receptor complex
- GO:0031699 beta-3 adrenergic receptor binding
- GO:0004939 beta-adrenergic receptor activity
- GO:0015052 beta3-adrenergic receptor activity
- GO:0051379 epinephrine binding
- GO:0003925 G protein activity
- GO:0051380 norepinephrine binding
- GO:0042803 protein homodimerization activity
- GO:0071880 adenylate cyclase-activating adrenergic receptor signaling pathway
- GO:0071881 adenylate cyclase-inhibiting adrenergic receptor signaling pathway
- GO:0007193 adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway
- GO:0007188 adenylate cyclase-modulating G protein-coupled receptor signaling pathway
- GO:0005975 carbohydrate metabolic process
- GO:0042755 eating behavior
- GO:0006112 energy reserve metabolic process
- GO:0007187 G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger
- GO:0006091 generation of precursor metabolites and energy
- GO:0055118 negative regulation of cardiac muscle contraction
- GO:0045986 negative regulation of smooth muscle contraction
- GO:0002025 norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure
- GO:0120162 positive regulation of cold-induced thermogenesis
- GO:0070374 positive regulation of ERK1 and ERK2 cascade
- GO:0050996 positive regulation of lipid catabolic process
- GO:0043410 positive regulation of MAPK cascade
Drugs targeting this protein · 23
- LABETALOL HYDROCHLORIDE antagonist
- HYDROXYAMPHETAMINE HYDROBROMIDE agonist
- DIPIVEFRIN HYDROCHLORIDE agonist
- CARTEOLOL HYDROCHLORIDE antagonist
- CARVEDILOL PHOSPHATE antagonist
- DILEVALOL HYDROCHLORIDE antagonist
- EPINEPHRINE BITARTRATE agonist
- NOREPINEPHRINE BITARTRATE agonist
- EPHEDRINE SULFATE agonist
- ISOPROTERENOL HYDROCHLORIDE agonist
- LY377604 agonist
- SOLABEGRON agonist
- MIRABEGRON agonist
- DROXIDOPA agonist
- RITOBEGRON agonist
- VIBEGRON agonist
- EPHEDRINE HYDROCHLORIDE agonist
- RAFABEGRON agonist
- MEPHENTERMINE SULFATE agonist
- ISOPROTERENOL SULFATE agonist
- AMIBEGRON HYDROCHLORIDE agonist
- EPINEPHRINE agonist
- CARVEDILOL antagonist
Related proteins · sequence + function similarity
- Beta-3 adrenergic receptor 1.00
- Beta-3 adrenergic receptor 0.99
- Beta-3 adrenergic receptor 0.99
- Beta-3 adrenergic receptor 0.99
- Beta-3 adrenergic receptor 0.99
- Beta-3 adrenergic receptor 0.98
- Beta-3 adrenergic receptor 0.98
- Beta-3 adrenergic receptor 0.98
- Beta-3 adrenergic receptor 0.97
- Beta-3 adrenergic receptor 0.95
- 5-hydroxytryptamine receptor 6 0.94
- 5-hydroxytryptamine receptor 6 0.94
Co-cited proteins · studied together in the literature
- Beta-3 adrenergic receptor 3 shared papers
- Beta-3 adrenergic receptor 1 shared papers
- Arrestin domain-containing protein 3 1 shared papers
- Arrestin domain-containing protein 4 1 shared papers
- Arrestin domain-containing protein 3 1 shared papers
- Apolipoprotein A-IV 1 shared papers
- Dopamine beta-hydroxylase 1 shared papers
- Thromboxane-A synthase 1 shared papers
- Apolipoprotein C-II 1 shared papers
- Alpha-adducin 1 shared papers
- Apolipoprotein C-I 1 shared papers
- E-selectin 1 shared papers
Literature · 13 cited papers
- The arrestin domain-containing 3 protein regulates body mass and energy expenditure. Cell Metab. · 2011
- The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
- Patterns of single-nucleotide polymorphisms in candidate genes for blood-pressure homeostasis. Nat. Genet. · 1999
- The beta3-adrenergic receptor activates mitogen-activated protein kinase in adipocytes through a Gi-dependent mechanism. J. Biol. Chem. · 1999
- Functional and molecular biological evidence for a possible beta3-adrenoceptor in the human detrusor muscle. Br. J. Pharmacol. · 1999
- The negative inotropic effect of beta3-adrenoceptor stimulation is mediated by activation of a nitric oxide synthase pathway in human ventricle. J. Clin. Invest. · 1998
- Association of Trp64Arg mutation of the beta3-adrenergic-receptor with NIDDM and body weight gain. Diabetologia · 1996
- Pharmacological characterization of a recently described human beta 3-adrenergic receptor mutant. Endocrinology · 1996
- Molecular cloning of a human beta 3-adrenergic receptor cDNA. FEBS Lett. · 1993
- The promoter and intron/exon structure of the human and mouse beta 3-adrenergic-receptor genes. Eur. J. Biochem. · 1993
- Genetic variation in the beta 3-adrenergic receptor and an increased capacity to gain weight in patients with morbid obesity. N. Engl. J. Med. · 1995
- Molecular characterization of the human beta 3-adrenergic receptor. Science · 1989
- … and 1 more in the literature graph