Overview
- Peptide (C)EPRKPQKSGIMKQQR, corresponding to amino acid residues 960 - 974 of mouse GPR158 (Accession Q8C419). Intracellular, C-terminus.
GPR158 Blocking Peptide (#BLP-GR078)
Western blot analysis of mouse brain lysate (lanes 1 and 3) and rat brain lysate (lanes 2 and 4):1-2. Anti-GPR158 Antibody (#AGR-078), (1:200).
3-4. Anti-GPR158 Antibody, preincubated with GPR158 Blocking Peptide (BLP-GR078).
Western blot analysis of human PC-3 prostate adenocarcinoma cell line lysate (lanes 1 and 4), human U-87 MG glioblastoma cell line lysate (lanes 2 and 5) and human OVCAR-3 ovarian carcinoma cell line lysate (lanes 3 and 6):1-3. Anti-GPR158 Antibody (#AGR-078), (1:200).
4-6. Anti-GPR158 Antibody, preincubated with GPR158 Blocking Peptide (BLP-GR078).
G protein-coupled receptor 158 (GPR158) is a protein that belongs to the G protein-coupled receptor (GPCR) superfamily. GPR158 was identified as an orphan receptor and a member of Class C GPCRs. 1
Class C GPCRs are obligatory dimers and are characterized by a large N- terminus extracellular ligand-binding domain linked to the seven-transmembrane (7TM) domain, and a large intracellular C-terminus domain. Members of Class C GPCRs include metabotropic glutamate receptors (mGluRs) and GABA(B) receptors, among others.1,2
GPR158 is highly expressed in the central nervous system (CNS), particularly in the hippocampus, cortex, midbrain, and cerebellum. Indeed, GPR158 has been linked to affective disorders, such as memory loss, cognitive diseases and depression. 2
Recently, osteocalcin (OCN) has been proposed as a putative ligand for GPR158. OCN is is a protein primarily produced by osteoblasts and appears to mediate its memory and cognitive regulation properties, through GPR158.3,4
Lately however, GPR158 was identified as the long sought metabotropic receptor mediating the slow neuromodulatory effects of glycine (Gly) and in analogy to the well-known metabotropic glutamate receptors (mGluRs), it has been named as mGlyR.5,6
The recognition that GPR158 function is central for cognition and affective states, may pave the way for the development of novel antidepressant drugs targeting GPR158.
Finally, GPR158 expression has been found to be elevated in several types of cancer including glioma, prostate and ovarian cancinomas.2
