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Gewählte Publikation:
SHR Neuro Krebs Kardio Lipid Stoffw Microb
Henstridge, CM; Balenga, NAB; Schroder, R; Kargl, JK; Platzer, W; Martini, L; Arthur, S; Penman, J; Whistler, JL; Kostenis, E; Waldhoer, M; Irving, AJ.
GPR55 ligands promote receptor coupling to multiple signalling pathways.
BRIT J PHARMACOL. 2010; 160(3): 604-614.
Doi: 10.1111/j.1476-5381.2009.00625.x
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- Co-Autor*innen der Med Uni Graz
- Aghaei Bandbon Balenga Nariman
- Kargl Julia
- Platzer Wolfgang
- Waldhoer Maria
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- Abstract:
- Background and purpose: Although GPR55 is potently activated by the endogenous lysophospholipid, L-alpha-lysophosphatidylinositol (LPI), it is also thought to be sensitive to a number of cannabinoid ligands, including the prototypic CB1 receptor antagonists AM251 and SR141716A (Rimonabant (R)). In this study we have used a range of functional assays to compare the pharmacological activity of selected cannabinoid ligands, AM251, AM281 and SR141716A with LPI in a HEK293 cell line engineered to stably express recombinant, human GPR55. Experimental approach: We evaluated Ca2+ signalling, stimulation of extracellular signal regulated kinase (ERK1/2) mitogen activated kinase MAP-kinases, induction of transcriptional regulators that are downstream of GPR55, including nuclear factor of activated T cells (NFAT), nuclear factor-kappa B (NF-kappa B) and cAMP response element binding protein (CREB), as well as receptor endocytosis. In addition, we assessed the suitability of a novel, label-free assay for GPR55 ligands that involves optical measurement of dynamic mass redistribution following receptor activation. Key results: GPR55 linked to a range of downstream signalling events and that the activity of GPR55 ligands was influenced by the functional assay employed, with differences in potency and efficacy observed. Conclusions and implications: Our data help to resolve some of the issues surrounding the pharmacology of cannabinoid ligands at GPR55 and highlight some differences in effector coupling associated with distinct GPR55 ligands.
- Find related publications in this database (using NLM MeSH Indexing)
- Biological Assay - methods
- Cannabinoids - pharmacology
- Cell Line, Transformed -
- Endocytosis - drug effects
- Humans -
- Ligands -
- Lysophospholipids - pharmacology
- Morpholines - pharmacology
- Piperidines - pharmacology
- Pyrazoles - pharmacology
- Receptors, G-Protein-Coupled - drug effects
- Signal Transduction - drug effects
- Find related publications in this database (Keywords)
- GPR55
- GPCR
- cannabinoid
- LPI