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Journal of Pharmacology And Experimental Therapeutics Fast Forward
First published on May 1, 2006; DOI: 10.1124/jpet.105.098848

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Received for publication November 28, 2005.
Revised April 27, 2006.
Accepted for publication April 27, 2006.

LYSOPHOSPHATIDIC ACID BINDS TO AND ACTIVATES GPR92, A G PROTEIN-COUPLED RECEPTOR HIGHLY EXPRESSED IN GASTRO-INTESTINAL LYMPHOCYTES

Knut Kotarsky 1, Ake Boketoft 2, Jesper Bristulf 2, Niclas E. Nilsson 1, Ake Norberg 3, Stefan Hansson 4, Rannar Sillard 3, Christer Owman 1, Fredrik L.M. Leeb-Lundberg 1, Bjorn Olde 1*

1 Experimental Medical Science; Lund University, Sweden 2 Heptahelix AB, Malmo 3 Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden 4 Division of Obstetrics and Gynecology, department of Clinical Sciences, Lund University

* Address correspondence to: E-mail: bjorn.olde{at}med.lu.se

Abstract

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 (KD = 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 classical LPA1-3 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.


Key words: G protein-coupled receptor, binding studies, lysophosphatidic acid, orphan receptor, receptor signaling, tissue distribution




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