Sphingosylphosphorylcholine is a ligand for ovarian cancer G-protein-coupled receptor 1

Yan Xu, Kui Zhu, Guiying Hong, Weihua Wu, Linnea M. Baudhuin, Yi Jin Xiao, Derek S. Damron

Research output: Contribution to journalArticlepeer-review

169 Scopus citations

Abstract

Sphingosylphosphorylcholine (SPC) is a bioactive lipid that acts as an intracellular and extracellular signalling molecule in numerous biological processes. Many of the cellular actions of SPC are believed to be mediated by the activation of unidentified G-protein-coupled receptors. Here we sinew that SPC is a high-affinity ligand for an orphan receptor, ovarian cancer G-protein-coupled receptor 1 (OGR1). In OGR1-transfected cells, SPC binds to OGR1 with high affinity (K(d) = 33.3 nM) and high specificity and transiently increases intracellular calcium. The specific binding of SPC to OGR1 also activates p42/44 mitogen-activated protein kinases (MAP kinases) and inhibits cell proliferation. In addition, SPC causes internalization of OGR1 in a structurally specific manner.

Original languageEnglish (US)
Pages (from-to)261-267
Number of pages7
JournalNature Cell Biology
Volume2
Issue number5
DOIs
StatePublished - 2000

ASJC Scopus subject areas

  • Cell Biology

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