ArticleBritish journal of pharmacology2000
Pharmacological characterization of [(3)H]-prostaglandin E(2) binding to the cloned human EP(4) prostanoid receptor.
Article in British journal of pharmacology, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed.
- Engineering with EP2/EP4 knockout and IL-15 transpresentation renders stem cell-derived NK cells self-persistent and resistant to PGE2 inhibition.Frontiers in immunology · 2026Article
- SPMs exert anti-inflammatory and pro-resolving effects through positive allosteric modulation of the prostaglandin EP4 receptor.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- Targeting histone deacetylase-3 blocked epithelial-mesenchymal plasticity and metastatic dissemination in gastric cancer.Cell biology and toxicology · 2023Article
- Mapping the Molecular Architecture Required for Lipid-Binding Pockets Using a Subset of Established and Orphan G-Protein Coupled Receptors.Journal of chemical information and modeling · 2021Article
- Discovery to Launch of Anti-allergy (Emadine; Patanol/Pataday/Pazeo) and Anti-glaucoma (Travatan; Simbrinza) Ocular Drugs, and Generation of Novel Pharmacological Tools Such as AL-8810.ACS pharmacology & translational science · 2020Article
- Improved homology modeling of the human & rat EPBMC molecular and cell biology · 2019Article
- Chemical Equilibrium at the Tick-Host Feeding Interface:A Critical Examination of Biological Relevance in Hematophagous Behavior.Frontiers in physiology · 2019Review
- The EP1/EP3 receptor agonist 17-pt-PGEVascular pharmacology · 2016Article
- Prostaglandin E2 prevents hyperosmolar-induced human mast cell activation through prostanoid receptors EP2 and EP4.PloS one · 2014Article
- The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.British journal of pharmacology · 2013Article
- Frondoside A inhibits breast cancer metastasis and antagonizes prostaglandin E receptors EP4 and EP2.Breast cancer research and treatment · 2012Article
- Expression of E-series prostaglandin (EP) receptors and urodynamic effects of an EP4 receptor antagonist on cyclophosphamide-induced overactive bladder in rats.BJU international · 2010Article
- Inhibition of cyclooxygenase-2 down-regulates aromatase activity and decreases proliferation of Leydig tumor cells.The Journal of biological chemistry · 2009Article
- Prostaglandin E(2) couples through EP(4) prostanoid receptors to induce IL-8 production in human colonic epithelial cell lines.British journal of pharmacology · 2009Article
- EP4 mediates PGE2 dependent cell survival through the PI3 kinase/AKT pathway.Prostaglandins & other lipid mediators · 2007Article
- Prostaglandin E2 receptor distribution and function in the gastrointestinal tract.British journal of pharmacology · 2006Review
- EP4 prostanoid receptor-mediated vasodilatation of human middle cerebral arteries.British journal of pharmacology · 2004Article
- Regulation of human penile smooth muscle tone by prostanoid receptors.British journal of pharmacology · 2002Article
- Travoprost.Drugs & aging · 2002Review
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2 authors.
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Abstract
Prostaglandin (PG) E(2) (PGE(2)) is a potent prostanoid derived from arachidonic which can interact with EP(1), EP(2), EP(3) and EP(4) prostanoid receptor subtypes. Recombinant human EP(4) receptors expressed in human embryonic kidney (HEK-293) cells were evaluated for their binding characteristics using [(3)H]-PGE(2) and a broad panel of natural and synthetic prostanoids in order to define their pharmacological properties. [(3)H]-PGE(2) binding was optimal in 2-[N-Morpholino]ethanesulphonic acid (MES) buffer (pH 6.0) yielding 98+/-0.7% specific binding. The receptor displayed high affinity (K(d)=0.72+/-0.12 nM; n=3) for [(3)H]-PGE(2) and interacted with a saturable number of binding sites (B(max)=6.21+/-0.84 pmol mg(-1) protein). In competition studies, PGE(2) (K(i)=0.75+/-0.03 nM; n=12) and PGE(1) (K(i)=1.45+/-0.24 nM; n=3) displayed high affinities, as did two derivatives of PGE(1), namely 11-deoxy-PGE(1) (K(i)=1.36+/-0.34 nM) and 13,14-dihydro-PGE(1) (K(i)=3.07+/-0.29 nM). Interestingly, synthetic DP receptor-specific agonists such as BW245C (K(i)=64.7+/-1.0 nM; n=3) and ZK118182 (K(i)=425+/-42 nM; n=4), and the purported EP(3) receptor-specific ligand enprostil (K(i)=43.1+/-4.4 nM), also displayed high affinity for the EP(4) receptor. Two known EP(4) receptor antagonists were weak inhibitors of [(3)H]-PGE(2) binding akin to their known functional potencies, thus: AH23848 (K(i)=2690+/-232 nM); AH22921 (K(i)=31,800+/-4090 nM). These studies have provided a detailed pharmacological characterization of the recombinant human EP(4) receptor expressed in HEK-293 cells.
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