SLAS

Endogenous Human GPR55 Functional Cellular Assay

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Endogenous Human GPR55 Functional Cellular Assay
Authored by: Corning Incorporated Life Sciences


Target: G-protein-coupled receptor (GPR55)

Cell Line: LN-18 (Human glioblastoma, glioma)

GPR55, a G protein-coupled receptor, is a member of the larger cannabinoid receptor family.While CB1 and CB2 receptors are well characterized members of the cannabinoid receptor family, the GPR55 receptor remains less well understood. Emerging data indicate that bioactive lipid lysophosphatidylinositol [1] and certain cannabinoid ligands (reviewed in Ref. 2) activate GPR55. Its signaling is complex and possibly may be agonist- and tissue-dependent.[2] Recent studies have shown GPR55 couples to G12 protein, activates RhoA, increases Ca2+ release, and phosphorylates the extracellular signal-regulated kinase.[1][3]


Panel A. Activities of endogenous GPR55 in LN-18 cells in response to increasing concentrations of lysophosphatidylinositol (LPI) and several cannabinoid ligandsmeasured on Epic® label-free detection system. Panel B. Potencies (EC50) of LPI and cannabinoid ligands at endogenous GPR55 in LN-18 cells.


References

  1. ↑ 1.0 1.1 Oka S et al. (2007). BiochemBiophys Res Commun 362(4):928-934.
  2. ↑ Ross R. ( 2009). Trends Pharmacol Sci 30(3):156-163.
  3. ↑ Lauckner J et al. ( 2008). Proc Natl Acad Sci 105(7):2699-2704.
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