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Lysophosphatidic Acid Binds to and Activates GPR92, a G Protein-Coupled Receptor Highly Expressed in Gastrointestinal Lymphocytes

Kotarsky, Knut LU ; Boketoft, Ake ; Bristulf, Jesper ; Nilsson, Niclas LU ; Norberg, Ake ; Hansson, Stefan LU orcid ; Sillard, Rannar ; Owman, Christer LU ; Leeb-Lundberg, Fredrik LU and Olde, Björn LU (2006) In Journal of Pharmacology and Experimental Therapeutics 318(2). p.619-628
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 (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... (More)
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. (Less)
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organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Journal of Pharmacology and Experimental Therapeutics
volume
318
issue
2
pages
619 - 628
publisher
American Society for Pharmacology and Experimental Therapeutics
external identifiers
  • pmid:16651401
  • wos:000239023100020
  • scopus:33745957774
ISSN
1521-0103
DOI
10.1124/jpet.105.098848
language
English
LU publication?
yes
id
ee7c2d99-9007-41a9-b3b5-16add4b46fe7 (old id 157093)
alternative location
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=16651401&dopt=Abstract
date added to LUP
2016-04-01 15:44:25
date last changed
2021-10-10 04:45:04
@article{ee7c2d99-9007-41a9-b3b5-16add4b46fe7,
  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 (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.},
  author       = {Kotarsky, Knut and Boketoft, Ake and Bristulf, Jesper and Nilsson, Niclas and Norberg, Ake and Hansson, Stefan and Sillard, Rannar and Owman, Christer and Leeb-Lundberg, Fredrik and Olde, Björn},
  issn         = {1521-0103},
  language     = {eng},
  number       = {2},
  pages        = {619--628},
  publisher    = {American Society for Pharmacology and Experimental Therapeutics},
  series       = {Journal of Pharmacology and Experimental Therapeutics},
  title        = {Lysophosphatidic Acid Binds to and Activates GPR92, a G Protein-Coupled Receptor Highly Expressed in Gastrointestinal Lymphocytes},
  url          = {http://dx.doi.org/10.1124/jpet.105.098848},
  doi          = {10.1124/jpet.105.098848},
  volume       = {318},
  year         = {2006},
}