Introduction of ADRB1

ADRB1 membrane protein belongs to the beta receptors of the adrenergic receptor family (alpha 1, alpha 2, beta 1, and beta 2), which is responsible for mediating the physiological effects of the hormone epinephrine and the neurotransmitter norepinephrine. The beta 1 adrenergic receptor (ADRB1) is encoded by an intronless gene located on chromosome 10q24-26. It is coupled to the Gs G-protein/adenyl cyclase signal transduction pathway, a central pathway to regulating cardiac function. It has been demonstrated to be equally sensitive to epinephrine and norepinephrine.

Functions of ADRB1 Membrane Protein

ADRB1 receptors are mainly distributed on cardiac tissues such as the cardiac pacemaker and myocardium. The stimulation of these receptors results in increased heart rate (chronotropy), increased conduction (dromotropy), reduced refractoriness within the atrioventricular node, and increased contractility (iontropy). As a result, β1-receptor-mediated effects contribute importantly to the pathophysiology of numerous cardiovascular diseases, including hypertension, coronary artery disease, and heart failure. The ADRB1 receptors are also found on the juxtaglomerular cells of the kidney, where their stimulation leads to increased renin release. Beta-blockers have been found to exert beneficial effects across cardiovascular diseases, resulting in blood pressure reduction in hypertension, lowering of myocardial oxygen demand in ischemic heart disease, and attenuation of cardiac remodeling in heart failure.

Fig.1 ADRB1 bound to isoprenaline.

Applications of ADRB1 Membrane Protein in Literature

1. Swift J M., et al. Beta-1 adrenergic agonist treatment mitigates negative changes in cancellous bone microarchitecture and inhibits osteocyte apoptosis during disuse. Plos One. 2014, 9(9): e106904. PMID: 25211027

This article investigated the effects of dobutamine, a beta-1 adrenergic receptor (AR) agonist and hindlimb unloading on cancellous bone microarchitecture, tissue-level bone cell activity, and osteocyte apoptosis. The results showed that dobutamine treatment during disuse alleviated negative changes in cancellous bone microarchitecture and inhibited increases in osteocyte apoptosis.

2. Gilbert C E., et al. Three basic residues of intracellular loop 3 of the beta-1 adrenergic receptor are required for golgin-160-dependent trafficking. International Journal of Molecular Sciences. 2014, 15(2): 2929-45. PMID: 24566136

This article shows that golgin-160, a protein of the golgin family which have been implicated in the maintenance of Golgi structure and in vesicle tethering, binds directly to the third intracellular loop of the beta-1 adrenergic receptor. This process depends on three basic residues in this loop.

3. Li X., et al. Let-7e replacement yields potent anti-arrhythmic efficacy via targeting beta 1-adrenergic receptor in rat heart. Journal of Cellular & Molecular Medicine. 2014, 18(7): 1334-1343. PMID: 24758696

This study investigated the role of miRNA let-7e in the up-regulation of β1-adrenergic receptor and arrhythmogenesis in acute myocardial infarction (AMI) in rats. The results showed that miRNA let-7e inhibited AMI-induced arrhythmia in the rat. Moreover, targeting miRNA let-7e may be a promising therapeutic strategy for modulating β1-adrenergic receptor.

4. Wang J., et al. Beta-1-adrenergic receptors mediate Nrf2-HO-1-HMGB1 axis regulation to attenuate hypoxia/reoxygenation-induced cardiomyocytes injury in vitro. Cellular Physiology & Biochemistry. 2015, 35(2): 767-777. PMID: 25634756

This study showed that beta1-adrenergic receptors-mediated Nrf2-HO-1-HMGB1 axis regulation plays a vital role in H/R-induced neonatal rat cardiomyocytes injury in vitro via PI3K/p38MAPK signaling pathway.

5. Sapir A., et al. Development of an enzyme-linked immunosorbent assay and a beta-1 adrenergic receptor-based assay for monitoring the drug atenolol. Environmental Toxicology & Chemistry. 2013, 32(3): 585-593. PMID: 23180677

This article described a highly efficient, sensitive ELISA and the receptor assays for monitoring atenolol in different samples. These methods are efficient, high-throughput, and cost-effective.

ADRB1 Preparation Options

Many membrane proteins express their full activity only when correctly oriented and inserted into a lipid bilayer, which makes it necessary for reconstitution. Creative Biolabs has established a powerful Magic™ Membrane Protein platform for our clients to obtain their protein of interest in the stabilized, purified, functional formats. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-ADRB1 antibody development services.

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