scholarly journals Role of the G-Protein-Coupled Receptor GPR12 as High-Affinity Receptor for Sphingosylphosphorylcholine and Its Expression and Function in Brain Development

2003 ◽  
Vol 23 (3) ◽  
pp. 907-914 ◽  
Author(s):  
Atanas Ignatov ◽  
Julia Lintzel ◽  
Irm Hermans-Borgmeyer ◽  
Hans-Jürgen Kreienkamp ◽  
Patrick Joost ◽  
...  
Keyword(s):  
Brain Development ◽  
G Protein ◽  
G Protein Coupled Receptor ◽  
High Affinity ◽  
High Affinity Receptor ◽  
Affinity Receptor ◽  
And Function ◽  
G Protein Coupled

Sphingosine-1-phosphate is a ligand for the G protein-coupled receptor EDG-6

Blood ◽  
2000 ◽  
Vol 95 (8) ◽  
pp. 2624-2629 ◽  
Author(s):  
James R. Van Brocklyn ◽  
Markus H. Gräler ◽  
Günter Bernhardt ◽  
John P. Hobson ◽  
Martin Lipp ◽  
...  
Keyword(s):  
G Protein ◽  
Hek293 Cells ◽  
Hematopoietic Tissue ◽  
G Protein Coupled Receptor ◽  
High Affinity ◽  
Extracellular Signal ◽  
Sphingosine 1 Phosphate ◽  
High Affinity Receptor ◽  
High Concentrations ◽  
G Protein Coupled

Abstract EDG-6 is a recently cloned member of the endothelial differentiation gene (EDG) G protein-coupled receptor family that is expressed in lymphoid and hematopoietic tissue and in the lung. Homology of EDG-6 to the known sphingosine-1-phosphate (SPP) receptors EDG-1, EDG-3, and EDG-5 and lysophosphatidic acid (LPA) receptors EDG-2 and EDG-4 suggested that its ligand may be a lysophospholipid or lysosphingolipid. We examined the binding of [32P]SPP to HEK293 cells, transiently transfected with cDNA encoding EDG-6. Binding of [32P]SPP was saturable, demonstrating high affinity (KD = 63 nmol/L). Binding was also specific for SPP, as only unlabeled SPP and sphinganine-1-phosphate, which lacks the trans double bond at the 4 position, potently displaced radiolabeled SPP. LPA did not compete for binding of SPP at any concentration tested, whereas sphingosylphosphorylcholine competed for binding to EDG-6, but only at very high concentrations. In addition, SPP activated extracellular signal-regulated kinase (Erk) in EDG-6 transfected cells in a pertussis toxin-sensitive manner. These results indicate that EDG-6 is a high affinity receptor for SPP, which couples to a Gi/o protein, resulting in the activation of growth-related signaling pathways.

Sphingosine-1-phosphate is a ligand for the G protein-coupled receptor EDG-6

Blood ◽  
2000 ◽  
Vol 95 (8) ◽  
pp. 2624-2629
Author(s):  
James R. Van Brocklyn ◽  
Markus H. Gräler ◽  
Günter Bernhardt ◽  
John P. Hobson ◽  
Martin Lipp ◽  
...  
Keyword(s):  
G Protein ◽  
Hek293 Cells ◽  
Hematopoietic Tissue ◽  
G Protein Coupled Receptor ◽  
High Affinity ◽  
Extracellular Signal ◽  
Sphingosine 1 Phosphate ◽  
High Affinity Receptor ◽  
High Concentrations ◽  
G Protein Coupled

EDG-6 is a recently cloned member of the endothelial differentiation gene (EDG) G protein-coupled receptor family that is expressed in lymphoid and hematopoietic tissue and in the lung. Homology of EDG-6 to the known sphingosine-1-phosphate (SPP) receptors EDG-1, EDG-3, and EDG-5 and lysophosphatidic acid (LPA) receptors EDG-2 and EDG-4 suggested that its ligand may be a lysophospholipid or lysosphingolipid. We examined the binding of [32P]SPP to HEK293 cells, transiently transfected with cDNA encoding EDG-6. Binding of [32P]SPP was saturable, demonstrating high affinity (KD = 63 nmol/L). Binding was also specific for SPP, as only unlabeled SPP and sphinganine-1-phosphate, which lacks the trans double bond at the 4 position, potently displaced radiolabeled SPP. LPA did not compete for binding of SPP at any concentration tested, whereas sphingosylphosphorylcholine competed for binding to EDG-6, but only at very high concentrations. In addition, SPP activated extracellular signal-regulated kinase (Erk) in EDG-6 transfected cells in a pertussis toxin-sensitive manner. These results indicate that EDG-6 is a high affinity receptor for SPP, which couples to a Gi/o protein, resulting in the activation of growth-related signaling pathways.

Role of the endogenous obestatin/G-protein coupled receptor 39 (GPR39) system in the regulation of proliferation and migration of activated human pancreatic stellate cells

Pancreatology ◽  
2018 ◽  
Vol 18 (4) ◽  
pp. S118
Author(s):  
Lara Estévez-Perez ◽  
Saul Leal-lopez ◽  
Agustin Sanchez-Temprano ◽  
Begoña Otero-Alen ◽  
Carlos Seoane-Mosteiro ◽  
...  
Keyword(s):  
G Protein ◽  
Stellate Cells ◽  
Pancreatic Stellate Cells ◽  
G Protein Coupled Receptor ◽  
Regulation Of Proliferation ◽  
And Migration ◽  
G Protein Coupled ◽  
Proliferation And Migration

scholarly journals Role of Detergents in Conformational Exchange of a G Protein-coupled Receptor

2012 ◽  
Vol 287 (43) ◽  
pp. 36305-36311 ◽  
Author(s):  
Ka Young Chung ◽  
Tae Hun Kim ◽  
Aashish Manglik ◽  
Rohan Alvares ◽  
Brian K. Kobilka ◽  
...  
Keyword(s):  
G Protein ◽  
Conformational Exchange ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

The G protein coupled receptor 55 in the human placenta and the role of its endogenous agonist lysophosphatidylinositol (LPI) on endothelial function

Placenta ◽  
2013 ◽  
Vol 34 (9) ◽  
pp. A18-A19
Author(s):  
Julia Kremshofer ◽  
Gerit Moser ◽  
Monika Siwetz ◽  
Astrid Blaschitz ◽  
Monika Sundl ◽  
...  
Keyword(s):  
Endothelial Function ◽  
G Protein ◽  
Human Placenta ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled
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