Overview
- Peptide (C)HRV(S)FEHYPIQAWQR, corresponding to amino acid residues 169-183 of mouse GPR68 (Accession Q8BFQ3). 2nd extracellular loop.
- Rat and mouse kidney lysates and rat heart membranes (1:200-1:1000).
- Western blot analysis of rat kidney lysates (lanes 1 and 3) and mouse kidney membranes (lanes 2 and 4):1,2. Anti-GPR68 (OGR1) (extracellular) Antibody (#AGR-042), (1:200).
3,4. Anti-GPR68 (OGR1) (extracellular) Antibody, preincubated with GPR68/OGR1 (extracellular) Blocking Peptide (#BLP-GR042). - Western blot analysis of rat heart membranes:1. Anti-GPR68 (OGR1) (extracellular) Antibody (#AGR-042), (1:200).
2. Anti-GPR68 (OGR1) (extracellular) Antibody, preincubated with GPR68/OGR1 (extracellular) Blocking Peptide (#BLP-GR042).
- Human THP-1 monocytic leukemia cells.
All GPCRs, including GPR68, are single peptides possessing seven transmembrane domains with an extracellular N-terminus and an intracellular C-terminus1. GPR68 is expressed in several tissues including the spleen, testis, small bowel, brain, heart, lung and kidneys. It shares strong homology (49-54%) with the human receptor GPR42.
GPR68 is proton sensitive in the pH range of 6.8-7.8 and acts as a proton activated receptor. GPR68 stimulates inositol triphosphate (IP3) formation thereby releasing intracellular calcium and activating the mitogen activated protein kinase/extracellular signal-regulated (ERK) kinase cascade. In addition, GPR68 receptor regulates NHE3 and H+-ATPase, in response to extracellular pH changes in cultured HEK 293 renal cells. This activation requires a cluster of histidine residues in the extracellular domains of the receptor and protein-kinase C (PKC) activation4.