Background: Sphingosylphosphorylcholine (SPC) and lysophosphatidylcholine (LPC) are bioactive lipid molecules involved in numerous biologicals processes. GPR4 shares sequence homology with OGR1 (51%), the highest of all GPCRÕs. GPR4 has been identified as another high affinity receptor for SPC and low affinity receptor for LPC. SPC and LPC stimulate kinase activation and DNA synthesis stimulated, both of which are pertussis toxin-sensitive, suggesting Gi-heterotrimeric G protein involvement. The GPR4 subfamily of GPCRÕs consists of four receptors that share significant sequence homology; OGR1, TDAG8 and G2A. G2A has been shown to be a potent transforming oncogene. GPR4 also malignantly transforms NIH3T3 cells and TDAG8 malignantly transforms the normal mammary epithelial cell line NMuMG. Overexpression of GPR4 or TDGA8 in HEK293 cells leads to transcriptional activation independent of exogenously added ligand. TDAG8 and GPR4 are also overexpressed in a range of human cancer tissues suggestive of a driving role in maintaining tumor formation.
Positive Control: Human brain lysate (Cat. No. X1633C).
Immunogen: Synthetic peptide derived from the GPR4 protein.
Purification Method: Antigen Immunoaffiinity Purification.
Formulation: Provided as ligand affinity purified antibody in phosphate buffered saline with 0.08% sodium azide.
References: 1. Sin, W.C., et al. 'G protein-coupled receptors GPR4 and TDAG8 are oncogenic and overexpressed in human cancers.' Oncogene 2004
2. Yun, M.R., et al. 'The action mode of lysophosphatidylcholine in human monocytes.' J. Pharmacol. Sci. 2004, 94, 45-50
3. Bektas, M., et al. 'The G protein-coupled receptor GPR4 suppresses ERK activation in a ligand-independent manner.' Biochemistry 2003, 42, 12181-12191
4. Lum, H., et al. 'Inflammatory stress increases receptor for lysophosphatidylcholine in human microvascular endothelial cells.' Am. J. Physiol. Heart Circ. Physiol. 2003, 285, H1786-H1789
5. Xu, Y. 'Sphingosylphosphorylcholine and lysophosphatidylcholine: G protein-coupled receptors and receptor-mediated signal transduction.' Biochim Biophys Acta 2002, 1582, 81-88
6. Zhu, K., et al. 'Sphingosylphosphorylcholine and lysophosphatidylcholine are ligands for the G protein-coupled receptro GPR4.' J. Biol. Chem. 2001, 276, 41325-41335
7. An, S., et al. 'Cloning, sequencing and tissue distribution of two related G protein-coupled receptor candidates expressed prominently in human lung tissue.' FEBS Lett. 1995, 375, 121-124.
UniProt: P46093.
Caution: This product is intended FOR RESEARCH USE ONLY, and FOR TESTS IN VITRO, not for use in diagnostic or therapeutic procedures involving humans or animals.
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