GPR55, a Lysophosphatidylinositol Receptor with Cannabinoid Sensitivity?

Tapio Nevalainen, Andrew J. Irving

    Research output: Contribution to journalReview article

    37 Citations (Scopus)

    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 13, 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.

    Original languageEnglish
    Pages (from-to)799-813
    Number of pages15
    JournalCurrent Topics in Medicinal Chemistry
    Volume10
    Issue number8
    Publication statusPublished - Jun 2010

    Keywords

    • GPR55
    • Cannabinoid
    • Lysophosphatidylinositol
    • PROTEIN-COUPLED RECEPTOR
    • CRYSTAL-STRUCTURE
    • PHOSPHOLIPASE-C
    • NUCLEAR RECEPTOR
    • PPAR-ALPHA
    • MASS-SPECTROMETRY
    • CB1 RECEPTOR
    • RAT-BRAIN
    • BONE MASS
    • MESENTERIC VASODILATION

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