Sphingosine 1-phosphate is a ligand of the human gpr3, gpr6 and gpr12 family of constitutively active G protein-coupled receptors

Uhlenbrock, Kirsten; Gassenhuber, Johann; Kostenis, Evi

doi:10.1016/s0898-6568(02)00041-4

Cited by 188 publications

(232 citation statements)

References 53 publications

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“…GPR3 is an orphan receptor that exhibits a high degree of constitutive activity when overexpressed in numerous tissue culture cell lines, resulting in a high level of cAMP production (Eggerickx et al 1995, Uhlenbrock et al 2002. This indicates that it is coupled to G s .…”

Section: Maintenance Of Meiotic Arrestmentioning

confidence: 99%

“…It is currently not known whether constitutive activity of GPR3 in the oocyte is sufficient to produce the amount of cAMP required to maintain meiotic arrest, or whether the follicle cells surrounding the oocyte produce a ligand that increases the activity of GPR3. Structurally, GPR3 is closely related to the lysophosphatidic acid receptors, sphingosine-1-phosphate (edg) receptors, cannabinoid receptors, and melanocortin receptors (Uhlenbrock et al 2002, Ignatov et al 2003, Kostenis 2004a, 2004b. With the exception of the melanocortin receptors, these receptor families are activated by lipids.…”

Section: Maintenance Of Meiotic Arrestmentioning

confidence: 99%

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Stops and starts in mammalian oocytes: recent advances in understanding the regulation of meiotic arrest and oocyte maturation

Mehlmann¹

2005

Reproduction

437

307

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Mammalian oocytes grow and undergo meiosis within ovarian follicles. Oocytes are arrested at the first meiotic prophase, held in meiotic arrest by the surrounding follicle cells until a surge of LH from the pituitary stimulates the immature oocyte to resume meiosis. Meiotic arrest depends on a high level of cAMP within the oocyte. This cAMP is generated by the oocyte, through the stimulation of the G s G-protein by the G-protein-coupled receptor, GPR3. Stimulation of meiotic maturation by LH occurs via its action on the surrounding somatic cells rather than on the oocyte itself. LH induces the expression of epidermal growth factor-like proteins in the mural granulosa cells that act on the cumulus cells to trigger oocyte maturation. The signaling pathway between the cumulus cells and the oocyte, however, remains unknown. This review focuses on recent studies highlighting the importance of the oocyte in producing cAMP to maintain arrest, and discusses possible targets at the level of the oocyte on which LH could act to stimulate meiotic resumption.

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Section: Maintenance Of Meiotic Arrestmentioning

confidence: 99%

Section: Maintenance Of Meiotic Arrestmentioning

confidence: 99%

Stops and starts in mammalian oocytes: recent advances in understanding the regulation of meiotic arrest and oocyte maturation

Mehlmann¹

2005

Reproduction

437

307

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“…Other potential receptors for S1P such as GPR3, GPR6, and GPR12 (Uhlenbrock et al, 2002;Ignatov et al, 2003) were not examined in these cells. We observed that G␣ i2 , G␣ o , G␣ 13 , G␣ s , and G␣ q/11 mediate NK cell chemotaxis induced by S1P (Kveberg et al, 2002).…”

Section: B Sphingosine 1-phosphate Induces Human Natural Killer Cellmentioning

confidence: 99%

Insights into Seven and Single Transmembrane-Spanning Domain Receptors and Their Signaling Pathways in Human Natural Killer Cells

Maghazachi

2005

Pharmacol Rev

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“…Five well established high affinity S1P receptors (S1P [1][2][3][4][5] receptors) are also part of the EDG receptor family. Now five new receptors, GPR3, GPR6, GPR12, GPR63, and P2Y 10 , have been claimed to be novel S1P receptors (7)(8)(9)(10). Similarly, GPR55 was discovered to be a new cannabinoid receptor adding to the two classical cannabinoid receptors CB 1 and CB 2 (11)(12)(13)(14).…”

mentioning

confidence: 99%

Lipid G Protein-coupled Receptor Ligand Identification Using β-Arrestin PathHunter™ Assay

Yin¹,

Chu²,

et al. 2009

Journal of Biological Chemistry

298

329

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A growing number of orphan G-protein-coupled receptors (GPCRs) have been reported to be activated by lipid ligands, such as lysophosphatidic acid, sphingosine 1-phosphate (S1P), and cannabinoids, for which there are already well established receptors. These new ligand claims are controversial due to either lack of independent confirmations or conflicting reports. We used the ␤-arrestin PathHunter TM assay system, a newly developed, generic GPCR assay format that measures ␤-arrestin binding to GPCRs, to evaluate lipid receptor and ligand pairing. This assay eliminates interference from endogenous receptors on the parental cells because it measures a signal that is specifically generated by the tagged receptor and is immediately downstream of receptor activation. We screened a large number of newly "deorphaned" receptors (GPR23, GPR92, GPR55, G2A, GPR18, GPR3, GPR6, GPR12, and GPR63) and control receptors against a collection of ϳ400 lipid molecules to try to identify the receptor ligand in an unbiased fashion. GPR92 was confirmed to be a lysophosphatidic acid receptor with weaker responses to farnesyl pyrophosphate and geranylgeranyl diphosphate. The putative cannabinoid receptor GPR55 responded strongly to AM251, rimonabant, and lysophosphatidylinositol but only very weakly to endocannabinoids. G2A receptor was confirmed to be an oxidized free fatty acid receptor. In addition, we discovered that 3,3-diindolylmethane, a dietary molecule from cruciferous vegetables, which has known anti-cancer properties, to be a CB 2 receptor partial agonist, with binding affinity around 1 M. The anti-inflammatory effect of 3,3-diindolylmethane in RAW264.7 cells was shown to be partially mediated by CB 2 .

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Sphingosine 1-phosphate is a ligand of the human gpr3, gpr6 and gpr12 family of constitutively active G protein-coupled receptors

Cited by 188 publications

References 53 publications

Stops and starts in mammalian oocytes: recent advances in understanding the regulation of meiotic arrest and oocyte maturation

Stops and starts in mammalian oocytes: recent advances in understanding the regulation of meiotic arrest and oocyte maturation

Insights into Seven and Single Transmembrane-Spanning Domain Receptors and Their Signaling Pathways in Human Natural Killer Cells

Lipid G Protein-coupled Receptor Ligand Identification Using β-Arrestin PathHunter™ Assay

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