Abstract
Increasing experimental studies indicate the existence of novel molecular targets for cannabinoid ligands and recently it has been suggested that the orphan G-protein coupled receptor, GPR55 can be activated by a range of endogenous, plant and synthetic cannabinoids. However, to date, the most potent ligand identified for GPR55 is the endogenous phospholipid, lysophosphatidylinositol (LPI). GPR55 is thought to link predominantly to G-protein α13, where it promotes Rho-dependent signalling. Additional events downstream of GPR55 include activation of ERK-MAP kinase and Ca2+ release from stores, as well as the induction of a number of transcription factors. Although GPR55 has only a low sequence identity with the CB1 or CB2 cannabinoid receptors, it clearly interacts with certain cannabinoid ligands. However, the nature and scope of these effects are presently unclear and they may be influenced by the assay and cellular background used for their study. This article reviews the current status of GPR55 pharmacology and its putative endogenous ligand, LPI.
Keywords: GPR55, Cannabinoid, Lysophosphatidylinositol
Current Topics in Medicinal Chemistry
Title: GPR55, a Lysophosphatidylinositol Receptor with Cannabinoid Sensitivity?
Volume: 10 Issue: 8
Author(s): Tapio Nevalainen and Andrew J. Irving
Affiliation:
Keywords: GPR55, Cannabinoid, Lysophosphatidylinositol
Abstract: Increasing experimental studies indicate the existence of novel molecular targets for cannabinoid ligands and recently it has been suggested that the orphan G-protein coupled receptor, GPR55 can be activated by a range of endogenous, plant and synthetic cannabinoids. However, to date, the most potent ligand identified for GPR55 is the endogenous phospholipid, lysophosphatidylinositol (LPI). GPR55 is thought to link predominantly to G-protein α13, where it promotes Rho-dependent signalling. Additional events downstream of GPR55 include activation of ERK-MAP kinase and Ca2+ release from stores, as well as the induction of a number of transcription factors. Although GPR55 has only a low sequence identity with the CB1 or CB2 cannabinoid receptors, it clearly interacts with certain cannabinoid ligands. However, the nature and scope of these effects are presently unclear and they may be influenced by the assay and cellular background used for their study. This article reviews the current status of GPR55 pharmacology and its putative endogenous ligand, LPI.
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Cite this article as:
Nevalainen Tapio and J. Irving Andrew, GPR55, a Lysophosphatidylinositol Receptor with Cannabinoid Sensitivity?, Current Topics in Medicinal Chemistry 2010; 10 (8) . https://dx.doi.org/10.2174/156802610791164229
DOI https://dx.doi.org/10.2174/156802610791164229 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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