Beta-1 adrenergic receptor

Details

Name
Beta-1 adrenergic receptor
Kind
protein
Synonyms
  • ADRB1R
  • B1AR
  • Beta-1 adrenoceptor
  • Beta-1 adrenoreceptor
Gene Name
ADRB1
UniProtKB Entry
P08588Swiss-Prot
Organism
Humans
NCBI Taxonomy ID
9606
Amino acid sequence
>lcl|BSEQ0055676|Beta-1 adrenergic receptor
MGAGVLVLGASEPGNLSSAAPLPDGAATAARLLVPASPPASLLPPASESPEPLSQQWTAG
MGLLMALIVLLIVAGNVLVIVAIAKTPRLQTLTNLFIMSLASADLVMGLLVVPFGATIVV
WGRWEYGSFFCELWTSVDVLCVTASIETLCVIALDRYLAITSPFRYQSLLTRARARGLVC
TVWAISALVSFLPILMHWWRAESDEARRCYNDPKCCDFVTNRAYAIASSVVSFYVPLCIM
AFVYLRVFREAQKQVKKIDSCERRFLGGPARPPSPSPSPVPAPAPPPGPPRPAAAAATAP
LANGRAGKRRPSRLVALREQKALKTLGIIMGVFTLCWLPFFLANVVKAFHRELVPDRLFV
FFNWLGYANSAFNPIIYCRSPDFRKAFQGLLCCARRAARRRHATHGDRPRASGCLARPGP
PPSPGAASDDDDDDVVGATPPARLLEPWAGCNGGAAADSDSSLDEPCRPGFASESKV
Number of residues
477
Molecular Weight
51222.97
Theoretical pI
9.03
GO Classification
Functions
alpha-2A adrenergic receptor binding / beta-adrenergic receptor activity / beta1-adrenergic receptor activity / PDZ domain binding / protein heterodimerization activity
Processes
adenylate cyclase-activating adrenergic receptor signaling pathway / brown fat cell differentiation / diet induced thermogenesis / fear response / heat generation / negative regulation of multicellular organism growth / positive regulation of heart rate by epinephrine-norepinephrine / positive regulation of the force of heart contraction by epinephrine-norepinephrine / response to cold
Components
early endosome / plasma membrane
General Function
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling. Involved in the regulation of sleep/wake behaviors (PubMed:31473062)
Specific Function
alpha-2A adrenergic receptor binding
Pfam Domain Function
Signal Regions
Not Available
Transmembrane Regions
56-84 94-120 133-154 173-196 223-248 320-349 355-377
Cellular Location
Cell membrane
Gene sequence
>lcl|BSEQ0010189|Beta-1 adrenergic receptor (ADRB1)
ATGGGCGCGGGGGTGCTCGTCCTGGGCGCCTCCGAGCCCGGTAACCTGTCGTCGGCCGCA
CCGCTCCCCGACGGCGCGGCCACCGCGGCGCGGCTGCTGGTGCCCGCGTCGCCGCCCGCC
TCGTTGCTGCCTCCCGCCAGCGAAAGCCCCGAGCCGCTGTCTCAGCAGTGGACAGCGGGC
ATGGGTCTGCTGATGGCGCTCATCGTGCTGCTCATCGTGGCGGGCAATGTGCTGGTGATC
GTGGCCATCGCCAAGACGCCGCGGCTGCAGACGCTCACCAACCTCTTCATCATGTCCCTG
GCCAGCGCCGACCTGGTCATGGGGCTGCTGGTGGTGCCGTTCGGGGCCACCATCGTGGTG
TGGGGCCGCTGGGAGTACGGCTCCTTCTTCTGCGAGCTGTGGACCTCAGTGGACGTGCTG
TGCGTGACGGCCAGCATCGAGACCCTGTGTGTCATTGCCCTGGACCGCTACCTCGCCATC
ACCTCGCCCTTCCGCTACCAGAGCCTGCTGACGCGCGCGCGGGCGCGGGGCCTCGTGTGC
ACCGTGTGGGCCATCTCGGCCCTGGTGTCCTTCCTGCCCATCCTCATGCACTGGTGGCGG
GCGGAGAGCGACGAGGCGCGCCGCTGCTACAACGACCCCAAGTGCTGCGACTTCGTCACC
AACCGGGCCTACGCCATCGCCTCGTCCGTAGTCTCCTTCTACGTGCCCCTGTGCATCATG
GCCTTCGTGTACCTGCGGGTGTTCCGCGAGGCCCAGAAGCAGGTGAAGAAGATCGACAGC
TGCGAGCGCCGTTTCCTCGGCGGCCCAGCGCGGCCGCCCTCGCCCTCGCCCTCGCCCGTC
CCCGCGCCCGCGCCGCCGCCCGGACCCCCGCGCCCCGCCGCCGCCGCCGCCACCGCCCCG
CTGGCCAACGGGCGTGCGGGTAAGCGGCGGCCCTCGCGCCTCGTGGCCCTGCGCGAGCAG
AAGGCGCTCAAGACGCTGGGCATCATCATGGGCGTCTTCACGCTCTGCTGGCTGCCCTTC
TTCCTGGCCAACGTGGTGAAGGCCTTCCACCGCGAGCTGGTGCCCGACCGCCTCTTCGTC
TTCTTCAACTGGCTGGGCTACGCCAACTCGGCCTTCAACCCCATCATCTACTGCCGCAGC
CCCGACTTCCGCAAGGCCTTCCAGGGACTGCTCTGCTGCGCGCGCAGGGCTGCCCGCCGG
CGCCACGCGACCCACGGAGACCGGCCGCGCGCCTCGGGCTGTCTGGCCCGGCCCGGACCC
CCGCCATCGCCCGGGGCCGCCTCGGACGACGACGACGACGATGTCGTCGGGGCCACGCCG
CCCGCGCGCCTGCTGGAGCCCTGGGCCGGCTGCAACGGCGGGGCGGCGGCGGACAGCGAC
TCGAGCCTGGACGAGCCGTGCCGCCCCGGCTTCGCCTCGGAATCCAAGGTGTAG
Chromosome Location
10
Locus
10q25.3
External Identifiers
ResourceLink
UniProtKB IDP08588
UniProtKB Entry NameADRB1_HUMAN
GenBank Protein ID178200
GenBank Gene IDJ03019
GeneCard IDADRB1
GenAtlas IDADRB1
HGNC IDHGNC:285
PDB ID(s)2LSQ, 7BTS, 7BU6, 7BU7, 7BVQ
KEGG IDhsa:153
IUPHAR/Guide To Pharmacology ID28
NCBI Gene ID153
General References
  1. Frielle T, Collins S, Daniel KW, Caron MG, Lefkowitz RJ, Kobilka BK: Cloning of the cDNA for the human beta 1-adrenergic receptor. Proc Natl Acad Sci U S A. 1987 Nov;84(22):7920-4. [Article]
  2. Moore JD, Mason DA, Green SA, Hsu J, Liggett SB: Racial differences in the frequencies of cardiac beta(1)-adrenergic receptor polymorphisms: analysis of c145A>G and c1165G>C. Hum Mutat. 1999 Sep 19;14(3):271. [Article]
  3. Deloukas P, Earthrowl ME, Grafham DV, Rubenfield M, French L, Steward CA, Sims SK, Jones MC, Searle S, Scott C, Howe K, Hunt SE, Andrews TD, Gilbert JG, Swarbreck D, Ashurst JL, Taylor A, Battles J, Bird CP, Ainscough R, Almeida JP, Ashwell RI, Ambrose KD, Babbage AK, Bagguley CL, Bailey J, Banerjee R, Bates K, Beasley H, Bray-Allen S, Brown AJ, Brown JY, Burford DC, Burrill W, Burton J, Cahill P, Camire D, Carter NP, Chapman JC, Clark SY, Clarke G, Clee CM, Clegg S, Corby N, Coulson A, Dhami P, Dutta I, Dunn M, Faulkner L, Frankish A, Frankland JA, Garner P, Garnett J, Gribble S, Griffiths C, Grocock R, Gustafson E, Hammond S, Harley JL, Hart E, Heath PD, Ho TP, Hopkins B, Horne J, Howden PJ, Huckle E, Hynds C, Johnson C, Johnson D, Kana A, Kay M, Kimberley AM, Kershaw JK, Kokkinaki M, Laird GK, Lawlor S, Lee HM, Leongamornlert DA, Laird G, Lloyd C, Lloyd DM, Loveland J, Lovell J, McLaren S, McLay KE, McMurray A, Mashreghi-Mohammadi M, Matthews L, Milne S, Nickerson T, Nguyen M, Overton-Larty E, Palmer SA, Pearce AV, Peck AI, Pelan S, Phillimore B, Porter K, Rice CM, Rogosin A, Ross MT, Sarafidou T, Sehra HK, Shownkeen R, Skuce CD, Smith M, Standring L, Sycamore N, Tester J, Thorpe A, Torcasso W, Tracey A, Tromans A, Tsolas J, Wall M, Walsh J, Wang H, Weinstock K, West AP, Willey DL, Whitehead SL, Wilming L, Wray PW, Young L, Chen Y, Lovering RC, Moschonas NK, Siebert R, Fechtel K, Bentley D, Durbin R, Hubbard T, Doucette-Stamm L, Beck S, Smith DR, Rogers J: The DNA sequence and comparative analysis of human chromosome 10. Nature. 2004 May 27;429(6990):375-81. [Article]
  4. Pak Y, Pham N, Rotin D: 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 Nov;22(22):7942-52. [Article]
  5. He J, Bellini M, Xu J, Castleberry AM, Hall RA: Interaction with cystic fibrosis transmembrane conductance regulator-associated ligand (CAL) inhibits beta1-adrenergic receptor surface expression. J Biol Chem. 2004 Nov 26;279(48):50190-6. Epub 2004 Sep 9. [Article]
  6. Cheng SB, Quinn JA, Graeber CT, Filardo EJ: 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 Jun 24;286(25):22441-55. doi: 10.1074/jbc.M111.224071. Epub 2011 May 2. [Article]
  7. Mason DA, Moore JD, Green SA, Liggett SB: A gain-of-function polymorphism in a G-protein coupling domain of the human beta1-adrenergic receptor. J Biol Chem. 1999 Apr 30;274(18):12670-4. [Article]
  8. Borjesson M, Magnusson Y, Hjalmarson A, Andersson B: 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 Nov;21(22):1853-8. [Article]
  9. Ranade K, Jorgenson E, Sheu WH, Pei D, Hsiung CA, Chiang FT, Chen YD, Pratt R, Olshen RA, Curb D, Cox DR, Botstein D, Risch N: A polymorphism in the beta1 adrenergic receptor is associated with resting heart rate. Am J Hum Genet. 2002 Apr;70(4):935-42. Epub 2002 Feb 18. [Article]

Associated Data

Drug Relations
DrugDrug groupPharmacological action?TypeActionsDetails
Esmololapproved, withdrawnyestargetantagonistDetails
Betaxololapproved, investigationalyestargetantagonistDetails
IsoetharineapprovedyestargetagonistDetails
Metoprololapproved, investigationalyestargetantagonistDetails
AtenololapprovedyestargetantagonistDetails
TimololapprovedyestargetantagonistDetails
Propranololapproved, investigationalyestargetantagonistDetails
BisoprololapprovedyestargetantagonistDetails
DobutamineapprovedyestargetagonistDetails
Alprenololexperimental, withdrawnyestargetantagonistDetails
Pindololapproved, investigationalyestargetpartial agonistDetails
Isoprenalineapproved, investigationalyestargetagonistDetails
ArbutamineapprovedyestargetagonistDetails
Acebutololapproved, investigationalyestargetpartial agonistDetails
NadololapprovedyestargetantagonistDetails
LevobunololapprovedyestargetantagonistDetails
MetipranololapprovedyestargetantagonistDetails
Carteololapprovedyestargetantagonistpartial agonistDetails
LabetalolapprovedyestargetantagonistDetails
Epinephrineapproved, vet_approvedyestargetagonistDetails
Carvedilolapproved, investigationalyestargetantagonistDetails
Desipramineapproved, investigationalunknowntargetotherDetails
BevantololexperimentalyestargetantagonistDetails
PractololapprovedyestargetantagonistDetails
OxprenololapprovedyestargetantagonistDetails
Penbutololapproved, investigationalyestargetantagonistpartial agonistDetails
NorepinephrineapprovedyestargetagonistDetails
DronedaroneapprovedunknowntargetantagonistDetails
Nebivololapproved, investigationalyestargetantagonistDetails
Droxidopaapproved, investigationalyestargetagonistDetails
PW2101investigationalunknowntargetDetails
Albuterolapproved, vet_approvedunknowntargetagonistDetails
SotalolapprovedyestargetantagonistDetails
PirbuterolapprovedunknowntargetagonistDetails
Fenoterolapproved, investigationalunknowntargetagonistDetails
Phenylpropanolamineapproved, vet_approved, withdrawnunknowntargetagonistDetails
Clenbuterolapproved, investigational, vet_approvedunknowntargetagonistDetails
4-{[(2S)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-3H-indole-2-carbonitrileexperimentalunknowntargetDetails
2-HYDROXYMETHYL-6-OCTYLSULFANYL-TETRAHYDRO-PYRAN-3,4,5-TRIOLexperimentalunknowntargetDetails
Bopindololexperimentalyestargetantagonistpartial agonistDetails
BupranololexperimentalyestargetantagonistDetails
Pseudoephedrineapprovedunknowntargetagonistpartial agonistDetails
Celiprololapproved, investigationalyestargetantagonistDetails
Ephedra sinica rootnutraceuticalyestargetagonistDetails
AsenapineapprovedunknowntargetantagonistDetails
LoxapineapprovedunknowntargetbinderDetails
CabergolineapprovedunknowntargetbinderDetails
Vortioxetineapproved, investigationalunknowntargetligandDetails
BefunololexperimentalunknowntargetDetails
Formoterolapproved, investigationalunknowntargetagonistDetails
Salmeterolapprovedunknowntargetinverse agonistDetails
TerbutalineapprovedunknowntargetantagonistDetails
PutrescineexperimentalunknowntargetDetails
SpermidineexperimentalunknowntargetDetails
Spermineexperimental, nutraceuticalunknowntargetDetails
PropafenoneapprovedunknowntargetantagonistDetails
Levobetaxololapproved, investigationalyestargetantagonistDetails
Xamoterolapprovedyestargetpartial agonistDetails
ArotinololinvestigationalyestargetantagonistDetails
Lamotrigineapproved, investigationalunknowntargetinhibitorDetails
RacepinephrineapprovedyestargetagonistDetails
DL-MethylephedrineapprovedyestargetagonistDetails
Ranolazineapproved, investigationalnotargetantagonistDetails
Aripiprazoleapproved, investigationalunknowntargetligandDetails
EphedrineapprovedyestargetagonistDetails
MirabegronapprovedunknowntargetagonistDetails
IloperidoneapprovedunknowntargetantagonistDetails
BethanidineapprovedyestargetantagonistDetails
DichloroisoproterenolinvestigationalyestargetinhibitorDetails
BucindololinvestigationalyestargetmodulatorDetails
BretyliumapprovedyestargetantagonistDetails
DipivefrinapprovedyestargetantagonistDetails
AnisodamineinvestigationalyestargetmodulatorDetails
RaubasineexperimentalyestargetmodulatorDetails
Protokylolapproved, vet_approvedyestargetmodulatorDetails