Introduction of ADRA1B
Alpha-1-adrenergic receptor (alpha-1-ARs) is a member of the G protein-coupled receptor superfamily. 3 alpha-1-AR subtypes are divided into alpha1A, alpha1B, and alpha1D receptors. All subtypes signal through the Gq/11 family of G-proteins but show different patterns of activation. They activate mitogenic responses and regulate growth and proliferation of many cells. Adrenoceptor Alpha 1B (ADRA1B) is encoded by the gene ADRA1B. ADRA1B is regulated by Alpha-1 adrenergic receptors and Monoamine GPCRs. Gene Ontology annotations related to ADRA1A include alpha1-adrenergic receptor activity and G-protein coupled receptor activity.
|Basic Information of ADRA1B|
|Protein Name||Alpha-1B adrenergic receptor|
|Aliases||Alpha-1B adrenoreceptor, Alpha-1B adrenoceptor|
|Organism||Homo sapiens (Human)|
Function of ADRA1B Membrane Protein
Upon agonist stimulation, ADRA1B couple to Gq proteins, calcium signaling and protein kinase C activation. Subsequently, the receptors are phosphorylated, desensitized, and internalized. ADRA1B contributes to vasoconstriction in humans. Alpha1A adrenergic receptors are the prime mediators of vasoconstriction induced by activation of the sympathetic nervous system and thus play an important role in blood pressure regulation. Among the α1- AR- pathway genes, variants in the α1B-AR were most significantly associated with blood pressure and hypertension, while variants in the α1A-AR were not, suggesting that genetic variants in the α1B-AR, rather than in the α1A-AR subtype, may contribute to interindividual variability in regulation of vascular tone and blood pressure control.
Fig.1 The adrenergic receptors which subserve the responses of the sympathetic nervous system have been divided into two discrete subtypes: alpha adrenergic receptors and beta adrenergic receptors.
Application of ADRA1B Membrane Protein in Literature
1. Alfonzo-Méndez MA., et al. Protein Kinase C Activation Promotes α1B-Adrenoceptor Internalization and Late Endosome Trafficking through Rab9 Interaction. Role in Heterologous Desensitization. Mol Pharmacol. 2017, 91(4): 296-306. PubMed ID: 28082304
This article reports that protein kinase C regulates the transfer of α1B-adrenergic to late endosomes and that Rab9 regulates this process and is involved in G protein-mediated signaling turn-off.
2. Adefurin A., et al. Genetic variation in the alpha1B-adrenergic receptor and vascular response. Pharmacogenomics J. 2016, 17(4): 366-371. PubMed ID: 27089938
Authors in this group verified that ADRA1B rs10070745 was significantly associated with vasoconstrictor responses after adrenergic stimulation and contributed to the ethnic difference in phenylephrine sensitivity.
3. Tanaka K., et al. α1B-Adrenoceptor signalling regulates bone formation through the up-regulation of CCAAT/enhancer-binding protein δ expression in osteoblasts. Br J Pharmacol. 2016, 173(6): 1058-69. PubMed ID: 26750808
The result indicates that α1B-adrenoceptor signaling is essential for bone formation and regulates cellular proliferation through mechanisms associated with the up-regulation of Cebpd in osteoblasts.
4. Böhmer T., et al. The α1B-adrenoceptor subtype mediates adrenergic vasoconstriction in mouse retinal arterioles with damaged endothelium. Br J Pharmacol. 2014, 171(16): 3858-67. PubMed ID: 24749494
Authors in this group demonstrate that α1-adrenoceptor-mediated vasoconstriction in murine retinal arterioles is buffered by the endothelium. The α1B-adrenoceptor may represent a target that selectively regulates retinal blood flow in ocular diseases associated with endothelial dysfunction.
5. Castillo-Badillo JA., et al. Sphingosine 1-phosphate-mediated α1B-adrenoceptor desensitization and phosphorylation. Direct and paracrine/autocrine actions. Biochim Biophys Acta. 2012, 1823(2): 245-54. PubMed ID: 22019450
This article reveals that S1P is able to induce α1B-adrenergic receptor internalization and that its autocrine/paracrine generation was relevant for internalization induced by IGF-I.
ADRA1B Preparation Options
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