A Selective Antagonist Reveals a Potential Role of G Protein–Coupled Receptor 55 in Platelet and Endothelial Cell Function

@article{Kargl2013ASA,
  title={A Selective Antagonist Reveals a Potential Role of G Protein–Coupled Receptor 55 in Platelet and Endothelial Cell Function},
  author={Julia Kargl and Andrew J. Brown and Liisa Andersen and Georg Dorn and Rudolf Schicho and Maria Waldhoer and Akos Heinemann},
  journal={The Journal of Pharmacology and Experimental Therapeutics},
  year={2013},
  volume={346},
  pages={54 - 66}
}
The G protein–coupled receptor 55 (GPR55) is a lysophosphatidylinositol (LPI) receptor that is also responsive to certain cannabinoids. Although GPR55 has been implicated in several (patho)physiologic functions, its role remains enigmatic owing mainly to the lack of selective GPR55 antagonists. Here we show that the compound CID16020046 ((4-[4-(3-hydroxyphenyl)-3-(4-methylphenyl)-6-oxo-1H,4H,5H,6H-pyrrolo[3,4-c]pyrazol-5-yl] benzoic acid) is a selective GPR55 antagonist. In yeast cells… 

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TLDR
The characterization of GPR55 in the yeast Saccharomyces cerevisiae and in human embryonic kidney (HEK293) cells is presented, suggesting that the relatively low level of sequence identity between these orthologs translates to important functional differences in the ligand-binding site.
Pharmacology of GPR55 in Yeast and Identification of GSK494581A as a Mixed-Activity Glycine Transporter Subtype 1 Inhibitor and GPR55 Agonist
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The characterization of GPR55 in the yeast Saccharomyces cerevisiae and in human embryonic kidney (HEK293) cells is presented, suggesting that the relatively low level of sequence identity between these orthologs translates to important functional differences in the ligand-binding site.
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