Overview
- Peptide (C)RDRYNHTF(S)FEKFPME, corresponding to amino acid residues 162-177 of rat GPR4 (Accession Q4KLH9). 2nd extracellular loop.
Western blot analysis of rat dorsal root ganglion lysate:1. Anti-GPR4 (extracellular) Antibody (#AGR-041), (1:200).
2. Anti-GPR4 (extracellular) Antibody, preincubated with GPR4 (extracellular) Blocking Peptide (#BLP-GR041).
Western blot analysis of rat (lanes 1 and 3) and mouse (lanes 2 and 4) kidney membranes:1,2. Anti-GPR4 (extracellular) Antibody (#AGR-041), (1:200).
3,4. Anti-GPR4 (extracellular) Antibody, preincubated with GPR4 (extracellular) Blocking Peptide (#BLP-GR041).
Expression of GPR4 in rat dorsal raphe nucleus (DRN).Immunohistochemical staining of perfusion-fixed frozen rat brain sections with Anti-GPR4 (extracellular) Antibody (#AGR-041), (1:400), followed by goat anti-rabbit-Alexa-488. A. GPR4 immunoreactivity (green) appears in cells of both medial and lateral DRN (arrows). B. Pre-incubation of the antibody with GPR4 (extracellular) Blocking Peptide (#BLP-GR041), suppressed staining. Cell nuclei are stained with DAPI (blue). LDRN = lateral DRN, MDRN = medial DRN.
Cell surface detection of GPR4 in live intact human THP-1 monocytic leukemia cells:___ Cells.
___ Cells + goat-anti-rabbit-FITC.
___ Cells + Anti-GPR4 (extracellular) Antibody (#AGR-041), (2.5 µg) + goat-anti-rabbit-FITC.
- Damaghi, M. et al. (2013) Front. Physiol. 4, 370.
- Miyano, K. et al. (2014) J. Pharmacol. Sci. 126, 302.
- Justus, C.R. et al. (2013) Front. Physiol. 4, 354.
- Im, D.S. (2005) Acta Pharmacol. Sin. 26, 1435.
G-protein coupled receptor 4 (GPR4) belongs to a protein family comprised of 3 related G-protein coupled receptors (GPCRs): GPR4, OGR1/GPR68 and TDAG8/GPR65. Like all GPCRs, GPR4's structure is composed of seven-transmembrane-spanning domains linked by an N-terminal extracellular domain and a C-terminal intracellular domain2.
GPR4 responds to pH changes and is activated by a physiological increase in extracellular H+ through several signaling pathways including- the G12/13-protein/Rho, the Gq/PLC, and the Gs-protein/cAMP pathway1,2. It is fully activated at pH levels of 6.8 and lower and is inactive at pH levels of 7.5 and higher3,4.
Recent studies show that the pH-sensing GPCRs also have the ability to regulate cancer cell metastasis and proliferation, immune cell function, inflammation, blood vessel formation, endothelial barrier function thus making them an important therapeutic target for different diseases. Overexpression of GPR4 in human cancer cells shows involvement in driving or maintaining tumor formation.
GPR4 is expressed in several tissues including lung, vascular endothelial cells, kidney, heart, liver, skeletal muscle, ovary, and placenta.
Anti-GPR4 (extracellular) Antibody (#AGR-041) is a highly specific antibody directed against an epitope of the rat protein. The antibody can be used in western blot, immunohistochemistry and live cell flow cytometry applications. It has been designed to recognize GPR4 from mouse, rat and human samples.
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