Beta-2 adrenergic receptor


Beta-2 adrenergic receptor

The beta-2 adrenergic receptor2 adrenoreceptor), also known as ADRB2, is an beta-adrenergic receptor, and also denotes the human gene encoding it.cite web | title = Entrez Gene: ADRB1 adrenergic, beta-1-, receptor| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=153| accessdate = ]

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Gene

The gene|ADRB2 gene is intronless. Different polymorphic forms, point mutations, and/or downregulation of this gene are associated with nocturnal asthma, obesity and type 2 diabetes. [cite web | title = Entrez Gene: ADRB2 adrenergic, beta-2-, receptor, surface| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=154| accessdate = ]

tructure

The 3D crystallographic structure (see figure to the right) of the β2-adrenergic receptor has been determined (PDB|2R4R, PDB2|2R4S, PDB2|2RH1).cite journal | author = Rasmussen SG, Choi HJ, Rosenbaum DM, Kobilka TS, Thian FS, Edwards PC, Burghammer M, Ratnala VR, Sanishvili R, Fischetti RF, Schertler GF, Weis WI, Kobilka BK | title = Crystal structure of the human β2-adrenergic G-protein-coupled receptor | journal = Nature | volume = 450 | issue = 7168 | pages = 383–7 | year = 2007 | pmid = 17952055 | doi = 10.1038/nature06325 | issn = ]

Mechanism

This receptor is directly associated with one of its ultimate effectors, the class C L-type calcium channel CaV1.2. This receptor-channel complex also contains a G protein - Gs, which activate an adenylyl cyclase, cAMP-dependent kinase, and the counterbalancing phosphatase, PP2A. The assembly of the signaling complex provides a mechanism that ensures specific and rapid signaling by this G protein-coupled receptor. A two-state biophysical and molecular model has been proposed to account for the pH and REDOX sensitivity of this and other GPCRs.cite journal | author = Rubenstein LA, Zauhar RJ, Lanzara RG | title = Molecular dynamics of a biophysical model for β2-adrenergic and G protein-coupled receptor activation | journal = J. Mol. Graph. Model. | volume = 25 | issue = 4 | pages = 396–409 | year = 2006 | pmid = 16574446 | doi = 10.1016/j.jmgm.2006.02.008 | issn = | url = http://www.bio-balance.com/JMGM_article.pdf ]

Function

Actions of the β2 receptor include:

Muscular system

Circulatory system

* Increase cardiac output (minor degree compared to β1).
**Increase heart rate in sinoatrial node (SA node) (chronotropic effect).
**Increase atrial cardiac muscle contractility. (inotropic effect).
**Increases contractility and automaticity of ventricular cardiac muscle.
*Dilate hepatic artery.
*Dilate arteries to skeletal muscle.

Digestive system

* Glycogenolysis and gluconeogenesis in liver.
* Glycogenolysis and lactate release in skeletal muscle.
* Contract sphincters of GI tract.
* Insulin secretion from pancreas.cite journal | author = Trovik TS, Vaartun A, Jorde R, Sager G | title = Dysfunction in the beta 2-adrenergic signal pathway in patients with insulin dependent diabetes mellitus (IDDM) and unawareness of hypoglycaemia | journal = Eur. J. Clin. Pharmacol. | volume = 48 | issue = 5 | pages = 327–32 | year = 1995 | pmid = 8641318 | doi = | issn = ]
* Thickened secretions from salivary glands.

Other

* Inhibit histamine-release from mast cells.
* Increase protein content of secretions from lacrimal glands.
* Increase renin secretion from kidney.
* Receptor also present in cerebellum.
* Bronchiole dilation (targeted while treating asthma attacks)

Agonists

"(Short/long)"
*spasmolytics in asthma and COPD
**salbutamol (albuterol in USA)
**bitolterol mesylate
**isoproterenol
**levalbuterol
**metaproterenol
**salmeterol
**terbutaline
**clenbuterol
*ritodrine (tocolytic)

Antagonists

"(Beta blockers)"
*butoxamine*
*propranolol (antihypertensive)

* denotes selective agonists to the receptor.

ee also

*Other adrenergic receptors
**Alpha-1 adrenergic receptor
**Alpha-2 adrenergic receptor
**Beta-1 adrenergic receptor
**Beta-3 adrenergic receptor

References

Further reading

PBB_Further_reading
citations =
*cite journal | author=Frielle T, Caron MG, Lefkowitz RJ |title=Properties of the beta 1- and beta 2-adrenergic receptor subtypes revealed by molecular cloning. |journal=Clin. Chem. |volume=35 |issue= 5 |pages= 721–5 |year= 1989 |pmid= 2541947 |doi=
*cite journal | author=Taylor DR, Kennedy MA |title=Genetic variation of the beta(2)-adrenoceptor: its functional and clinical importance in bronchial asthma. |journal=American journal of pharmacogenomics : genomics-related research in drug development and clinical practice |volume=1 |issue= 3 |pages= 165–74 |year= 2002 |pmid= 12083965 |doi=
*cite journal | author=Thibonnier M, Coles P, Thibonnier A, Shoham M |title=Molecular pharmacology and modeling of vasopressin receptors. |journal=Prog. Brain Res. |volume=139 |issue= |pages= 179–96 |year= 2002 |pmid= 12436935 |doi=
*cite journal | author=Ge D, Huang J, He J, "et al." |title=beta2-Adrenergic receptor gene variations associated with stage-2 hypertension in northern Han Chinese. |journal=Ann. Hum. Genet. |volume=69 |issue= Pt 1 |pages= 36–44 |year= 2005 |pmid= 15638826 |doi= 10.1046/j.1529-8817.2003.00093.x
*cite journal | author=Muszkat M |title=Interethnic differences in drug response: the contribution of genetic variability in beta adrenergic receptor and cytochrome P4502C9. |journal=Clin. Pharmacol. Ther. |volume=82 |issue= 2 |pages= 215–8 |year= 2007 |pmid= 17329986 |doi= 10.1038/sj.clpt.6100142
*cite journal | author=Bucens D, Pain MC |title=Influence of hematocrit, blood gas tensions, and pH on pressure-flow relations in the isolated canine lung. |journal=Circ. Res. |volume=37 |issue= 5 |pages= 588–96 |year= 1976 |pmid= 154 |doi=
*cite journal | author=von Zastrow M, Kobilka BK |title=Ligand-regulated internalization and recycling of human beta 2-adrenergic receptors between the plasma membrane and endosomes containing transferrin receptors. |journal=J. Biol. Chem. |volume=267 |issue= 5 |pages= 3530–8 |year= 1992 |pmid= 1371121 |doi=
*cite journal | author=Gope R, Gope ML, Thorson A, "et al." |title=Genetic changes at the beta-2-adrenergic receptor locus on chromosome 5 in human colorectal carcinomas. |journal=Anticancer Res. |volume=11 |issue= 6 |pages= 2047–50 |year= 1992 |pmid= 1663718 |doi=
*cite journal | author=Bouvier M, Guilbault N, Bonin H |title=Phorbol-ester-induced phosphorylation of the beta 2-adrenergic receptor decreases its coupling to Gs. |journal=FEBS Lett. |volume=279 |issue= 2 |pages= 243–8 |year= 1991 |pmid= 1848190 |doi=
*cite journal | author=Yang-Feng TL, Xue FY, Zhong WW, "et al." |title=Chromosomal organization of adrenergic receptor genes. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=87 |issue= 4 |pages= 1516–20 |year= 1990 |pmid= 2154750 |doi=
*cite journal | author=Hui KK, Yu JL |title=Effects of protein kinase inhibitor, 1-(5-isoquinolinylsulfonyl)-2-methylpiperazine, on beta-2 adrenergic receptor activation and desensitization in intact human lymphocytes. |journal=J. Pharmacol. Exp. Ther. |volume=249 |issue= 2 |pages= 492–8 |year= 1989 |pmid= 2470898 |doi=
*cite journal | author=Hen R, Axel R, Obici S |title=Activation of the beta 2-adrenergic receptor promotes growth and differentiation in thyroid cells. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=86 |issue= 12 |pages= 4785–8 |year= 1989 |pmid= 2471981 |doi=
*cite journal | author=O'Dowd BF, Hnatowich M, Caron MG, "et al." |title=Palmitoylation of the human beta 2-adrenergic receptor. Mutation of Cys341 in the carboxyl tail leads to an uncoupled nonpalmitoylated form of the receptor. |journal=J. Biol. Chem. |volume=264 |issue= 13 |pages= 7564–9 |year= 1989 |pmid= 2540197 |doi=
*cite journal | author=Bristow MR, Hershberger RE, Port JD, "et al." |title=Beta 1- and beta 2-adrenergic receptor-mediated adenylate cyclase stimulation in nonfailing and failing human ventricular myocardium. |journal=Mol. Pharmacol. |volume=35 |issue= 3 |pages= 295–303 |year= 1989 |pmid= 2564629 |doi=
*cite journal | author=Emorine LJ, Marullo S, Delavier-Klutchko C, "et al." |title=Structure of the gene for human beta 2-adrenergic receptor: expression and promoter characterization. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=84 |issue= 20 |pages= 6995–9 |year= 1987 |pmid= 2823249 |doi=
*cite journal | author=Chung FZ, Wang CD, Potter PC, "et al." |title=Site-directed mutagenesis and continuous expression of human beta-adrenergic receptors. Identification of a conserved aspartate residue involved in agonist binding and receptor activation. |journal=J. Biol. Chem. |volume=263 |issue= 9 |pages= 4052–5 |year= 1988 |pmid= 2831218 |doi=
*cite journal | author=Yang SD, Fong YL, Benovic JL, "et al." |title=Dephosphorylation of the beta 2-adrenergic receptor and rhodopsin by latent phosphatase 2. |journal=J. Biol. Chem. |volume=263 |issue= 18 |pages= 8856–8 |year= 1988 |pmid= 2837466 |doi=
*cite journal | author=Kobilka BK, Dixon RA, Frielle T, "et al." |title=cDNA for the human beta 2-adrenergic receptor: a protein with multiple membrane-spanning domains and encoded by a gene whose chromosomal location is shared with that of the receptor for platelet-derived growth factor. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=84 |issue= 1 |pages= 46–50 |year= 1987 |pmid= 3025863 |doi=
*cite journal | author=Chung FZ, Lentes KU, Gocayne J, "et al." |title=Cloning and sequence analysis of the human brain beta-adrenergic receptor. Evolutionary relationship to rodent and avian beta-receptors and porcine muscarinic receptors. |journal=FEBS Lett. |volume=211 |issue= 2 |pages= 200–6 |year= 1987 |pmid= 3026848 |doi=

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