Lysophosphatidic Acid Binds to and Activates GPR92, a G Protein-Coupled Receptor Highly Expressed in Gastrointestinal Lymphocytes
Author
Summary, in English
Here, the ligand binding, activation, and tissue distribution of the orphan G protein-coupled receptor (GPCR) GPR92 were studied. GPR92 binds and is activated by compounds based on the lysophosphatidic acid (LPA) backbone. The binding of LPA to GPR92 was of high affinity (K(D) = 6.4 +/- 0.9 nM) and led to an increase in both phosphoinositide hydrolysis and cAMP production. GPR92 is atypical in that it has a low sequence homology with the classic LPA(1-3) receptors (21-22%). Expression of GPR92 is mainly found in heart, placenta, spleen, brain, lung, and gut. Notably, GPR92 is highly expressed in the lymphocyte compartment of the gastrointestinal tract. It is the most abundant GPCR activated by LPA found in the small intestinal intraepithelial CD8+ cytotoxic T cells.
Department/s
Publishing year
2006
Language
English
Pages
619-628
Publication/Series
Journal of Pharmacology and Experimental Therapeutics
Volume
318
Issue
2
Links
Document type
Journal article
Publisher
American Society for Pharmacology and Experimental Therapeutics
Topic
- Immunology in the medical area
Status
Published
Research group
- Mucosal Immunology
- Drug Target Discovery
ISBN/ISSN/Other
- ISSN: 1521-0103