GABBR2 Membrane Protein Introduction

Introduction of GABBR2

The GABBR2a receptor is one of the GABBR2, and GABBR2 is a G protein-coupled receptor subunit encoded by the GABBR2 gene in humans and regulates the GABBR of inhibitory neurotransmitters through G protein coupling. The metabolism of receptors, widely found in the central nervous system and peripheral tissues, plays an important role in many physiological processes. The structure of GABBR2 is similar to that of GABBR1, especially with 35% homology and 54% similarity at the N-terminus. Both interact with other molecules through the super-helix structure of the C-end. The relative amount of GABBR2 is 110 KDa and there are also 7 transmembrane regions. At present, among the human genes, three sheared isoforms of GABBR2 have been identified: GABBR2a, GABBR2b, and GABBR2c. The difference lies mainly in the structure of the C-terminus. However, its sheared isomers do not affect the formation of heterodimers between GABBR2 and GABBR1.

Function of GABBR2 Membrane Protein

GABBR2 has three effects on GABBR1:

• GABBR2 is transported to the cell surface by modifying the intracellular retention signal of GABBR1;
• Increases the affinity of agonists to GABBR1;
• The activation of G protein is affected by hydrophobic residues on its intracellular third ring.

The latest research shows that CGP7930 can bind to GABBR2 and activates GABBR2. CGP7930 becomes the first agonist of GABBR2. Therefore, it is speculated that GABBR2 alone can also constitute a functional receptor. GABBR2 mediates the coupling of G proteins, ligand binding leads to conformational changes, guanine nucleotide binding to G proteins triggers signaling and regulates the activity of downstream effectors. The signal inhibits adenylate cyclase, stimulates phospholipase A2, activates potassium channels, inactivates voltage-dependent calcium channels and regulates inositol phospholipid hydrolysis.

Fig.1 Structure of GABBR2 membrane protein.

Application of GABBR2 Membrane Protein in Literature

1. Yoo Y., et al. GABBR2 mutations determine phenotype in rett syndrome and epileptic encephalopathy. Ann Neurol. 2018, 82(3): 466-478. PubMed ID: 28856709
   
   

   This article reports that they identify a recurring de novo variant in GABAB receptor R2 (GABBR2) that reduces the receptor function, whereas different GABBR2 variants in EE patients possess a more profound effect in reducing receptor activity and are more responsive to agonist rescue in an animal model.

2. Niu X., et al. Genome-wide DNA Methylation Analysis Reveals GABBR2 as a Novel Epigenetic Target for EGFR 19 Deletion Lung Adenocarcinoma with Induction Erlotinib Treatment. Clin Cancer Res. 2017, 23(17): 5003-5014. PubMed ID: 28490462
   
   

   This article reveals that GABBR2 gene might be a novel potential epigenetic treatment target with induction erlotinib treatment for stage IIIa (N2) EGFR 19 deletion lung adenocarcinoma.

3. Philpott A.L., et al. A GABBR2 gene variant modifies pathophysiology in Huntington's disease. Neurosci Lett. 2016, 620: 8-13. PubMed ID: 27033668
   
   

   The article reveals a correlation between GABBR2, GABRA2, and DRD2 variants and cortical spinal cord excitability and cortical inhibition and the age of onset in HD as measured by TMS.

4. Geng Y., et al. Structure and functional interaction of the extracellular domain of human GABA(B) receptor GBR2. Nat Neurosci. 2012, 15(7): 970-8. PubMed ID: 22660477
   
   

   This article shows that the extracellular domain of GBR2 adopts a constitutive open conformation, indicating that the structural asymmetry in the active state of the GABA(B) receptor is unique to the GABAergic system.

5. Boas G.R.V., et al. GABA(B) receptor agonist only reduces ethanol drinking in light-drinking mice. Pharmacol Biochem Behav. 2012, 102(2): 233-40. PubMed ID: 22579911
   
   

   This article evaluates that "lose control of ethanol uptake" have different levels of Gabbr1 and Gabbr2 transcription that express the GABA (B1) and GABA (B2) subunits, respectively, in brain regions associated with addictive behavior.

GABBR2 Preparation Options

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