Lysophosphatidic Acid Binds to and Activates GPR92, a G Protein-Coupled Receptor Highly Expressed in Gastrointestinal Lymphocytes
(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)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/157093
- author
- Kotarsky, Knut LU ; Boketoft, Ake ; Bristulf, Jesper ; Nilsson, Niclas LU ; Norberg, Ake ; Hansson, Stefan LU ; Sillard, Rannar ; Owman, Christer LU ; Leeb-Lundberg, Fredrik LU and Olde, Björn LU
- organization
- publishing date
- 2006
- 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
- 2022-03-30 02:46:55
@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}}, }