doi: 10.1016/j.febslet.2006.08.015.
Epub 2006 Aug 17.
Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35
Affiliations
- PMID: 16934253
- DOI: 10.1016/j.febslet.2006.08.015
Item in Clipboard
Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35
FEBS Lett.
.
Free article
Abstract
We found that zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, acted as an agonist for a G protein-coupled receptor, GPR35. In our intracellular calcium mobilization assay, zaprinast activated rat GPR35 strongly (geometric mean EC(50) value of 16nM), whereas it activated human GPR35 moderately (geometric mean EC(50) value of 840nM). We also demonstrated that GPR35 acted as a Galpha(i/o)- and Galpha(16)-coupled receptor for zaprinast when heterologously expressed in human embryonic kidney 293 (HEK 293) cells. These findings will facilitate the research on GPR35 and the drug discovery of the GPR35 modulators.
Similar articles
-
G-protein coupled receptor 35 (GPR35) activation and inflammatory pain: Studies on the antinociceptive effects of kynurenic acid and zaprinast.Neuropharmacology. 2011 Jun;60(7-8):1227-31. doi: 10.1016/j.neuropharm.2010.11.014. Epub 2010 Nov 24. Neuropharmacology. 2011. PMID: 21110987
-
5-Nitro-2-(3-phenylpropylamino)benzoic acid is a GPR35 agonist.Pharmacology. 2008;82(4):245-9. doi: 10.1159/000157625. Epub 2008 Sep 26. Pharmacology. 2008. PMID: 18818509
-
G-protein-coupled receptor 35 is a target of the asthma drugs cromolyn disodium and nedocromil sodium.Pharmacology. 2010;86(1):1-5. doi: 10.1159/000314164. Epub 2010 Jun 19. Pharmacology. 2010. PMID: 20559017
-
Relaxin-3, INSL5, and their receptors.Results Probl Cell Differ. 2008;46:213-37. doi: 10.1007/400_2007_055. Results Probl Cell Differ. 2008. PMID: 18236022 Review.
-
Orthologue selectivity and ligand bias: translating the pharmacology of GPR35.Trends Pharmacol Sci. 2011 May;32(5):317-25. doi: 10.1016/j.tips.2011.02.002. Epub 2011 Mar 9. Trends Pharmacol Sci. 2011. PMID: 21392828 Review.
Cited by
-
Antagonists of GPR35 display high species ortholog selectivity and varying modes of action.J Pharmacol Exp Ther. 2012 Dec;343(3):683-95. doi: 10.1124/jpet.112.198945. Epub 2012 Sep 11. J Pharmacol Exp Ther. 2012. PMID: 22967846 Free PMC article.
-
Therapeutic Opportunities and Challenges in Targeting the Orphan G Protein-Coupled Receptor GPR35.ACS Pharmacol Transl Sci. 2020 Jul 29;3(5):801-812. doi: 10.1021/acsptsci.0c00079. eCollection 2020 Oct 9. ACS Pharmacol Transl Sci. 2020. PMID: 33073184 Free PMC article. Review.
-
Receptor selectivity between the G proteins Gα12 and Gα13 is defined by a single leucine-to-isoleucine variation.FASEB J. 2019 Apr;33(4):5005-5017. doi: 10.1096/fj.201801956R. Epub 2019 Jan 2. FASEB J. 2019. PMID: 30601679 Free PMC article.
-
A High-Throughput Chemical Screen in DJ-1β Mutant Flies Identifies Zaprinast as a Potential Parkinson's Disease Treatment.Neurotherapeutics. 2021 Oct;18(4):2565-2578. doi: 10.1007/s13311-021-01134-2. Epub 2021 Oct 25. Neurotherapeutics. 2021. PMID: 34697772 Free PMC article.
-
Comprehensive RNA-Seq expression analysis of sensory ganglia with a focus on ion channels and GPCRs in Trigeminal ganglia.PLoS One. 2013 Nov 8;8(11):e79523. doi: 10.1371/journal.pone.0079523. eCollection 2013. PLoS One. 2013. PMID: 24260241 Free PMC article.
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Other Literature Sources
Molecular Biology Databases
Miscellaneous
