FEBS Letters · 1995 · 155 citations · 26 references
Life SciencesBiochemistryPharmacologyCell SignalingMolecular PharmacologySignal TransductionCell-surface ReceptorsG Protein-coupled Receptor SignalingHormone ReceptorsMembrane ReceptorsReceptor PharmacologyReceptor PhysiologyCamp SignalingCdna CloningChinese Hamster Ovary Cell ExpressionChinese Hamster Ovary CellsG Protein-coupled Hormone ReceptorsProstaglandin PharmacologyProstaglandin SignalingTransmembrane Domains
A functional cDNA clone for the mouse prostaglandin (PG) E receptor EP2 subtype was isolated from a mouse cDNA library. The mouse EP2 receptor consists of 362 amino acid residues with seven putative transmembrane domains. [3H]PGE2 bound specifically to the membrane of Chinese hamster ovary cells stably expressing the cloned receptor. This binding was displaced by unlabeled prostanoids in the order of PGE2 = PGE1 >> iloprost, a stable PGI2 agonist > PGF2 alpha > PGD2. Binding was also inhibited by butaprost (an EP2 agonist) and to a lesser extent by M&B 28767 (an EP3 agonist), but not by sulprostone (an EP1 and EP3 agonist) or SC-19220 (an EP1 antagonist). PGE2 and butaprost increased the cAMP level in the Chinese hamster ovary cells in a concentration-dependent manner. Northern blot analysis revealed that EP2 mRNA is expressed most abundantly in the uterus, followed by the spleen, lung, thymus, ileum, liver, and stomach.
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