Beta-1 adrenergic receptor

UniProt P08588 Organism Homo sapiens Gene ADRB1, ADRB1R, B1AR

Also known as: ADRB1, ADRB1R, B1AR

Function

G protein-coupled receptor for catecholamines that couples to G(s) proteins to activate adenylate cyclase and cAMP-dependent pathway. Binds epinephrine and norepinephrine with approximately equal affinity. Mediates the activation of Ras via binding with cAMP-dependent RAPGEF2. As part of the sympathetic nervous system, plays a role in the physiologic regulation of cardiac functions such as stimulation of cardiomyocyte contraction. Also delivers proapoptotic signals in cardiomyocytes (By similarity). Involved in the regulation of sleep/wake behaviors.

Classification

Family (Pfam): PF00001 7tm_1
InterPro: ADR_fam, ADRB1_rcpt, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM
Functional cluster: G Protein-Coupled Receptors

Experimental structures · PDB · 7

2LSQ NMR
7BTS X-ray 3.13A
7BU6 X-ray 2.70A
7BU7 X-ray 2.60A
7BVQ X-ray 2.50A
8S2T EM 3.30A
9L84 EM 3.22A

A predicted model is available from AlphaFold.

Gene Ontology · 18

Disease associations

OMIM:607276 RAW:OMIM_607276

Drugs targeting this protein · 49

Related proteins · sequence + function similarity

Co-cited proteins · studied together in the literature

Beta-1 adrenergic receptor 1 shared papers
Beta-2 adrenergic receptor 1 shared papers
Beta-1 adrenergic receptor 1 shared papers
G protein-coupled estrogen receptor 1 1 shared papers
Golgi-associated PDZ and coiled-coil motif-containing protein 1 shared papers
Disks large homolog 4 1 shared papers
Rap guanine nucleotide exchange factor 2 1 shared papers
C-X-C chemokine receptor type 4 1 shared papers
Rap guanine nucleotide exchange factor 2 1 shared papers
Guanine nucleotide-binding protein G(s) subunit alpha isoforms short 1 shared papers

Literature · 11 cited papers

Binding pathway determines norepinephrine selectivity for the human beta1AR over beta2AR. Cell Res. · 2021
A rare mutation of beta1-adrenergic receptor affects sleep/wake behaviors. Neuron · 2019
Down-modulation of the G-protein-coupled estrogen receptor, GPER, from the cell surface occurs via a trans-Golgi-proteasome pathway. J. Biol. Chem. · 2011
Interaction with cystic fibrosis transmembrane conductance regulator-associated ligand (CAL) inhibits beta1-adrenergic receptor surface expression. J. Biol. Chem. · 2004
The DNA sequence and comparative analysis of human chromosome 10. Nature · 2004
Direct binding of the beta1 adrenergic receptor to the cyclic AMP-dependent guanine nucleotide exchange factor CNrasGEF leads to Ras activation. Mol. Cell. Biol. · 2002
A polymorphism in the beta1 adrenergic receptor is associated with resting heart rate. Am. J. Hum. Genet. · 2002
A novel polymorphism in the gene coding for the beta(1)-adrenergic receptor associated with survival in patients with heart failure. Eur. Heart J. · 2000
Racial differences in the frequencies of cardiac beta(1)-adrenergic receptor polymorphisms: analysis of c145A>G and c1165G>C. Hum. Mutat. · 1999
A gain-of-function polymorphism in a G-protein coupling domain of the human beta1-adrenergic receptor. J. Biol. Chem. · 1999
Cloning of the cDNA for the human beta 1-adrenergic receptor. Proc. Natl. Acad. Sci. U.S.A. · 1987

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