The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs.
Article Details
- CitationCopy to clipboard
Abramovitz M, Adam M, Boie Y, Carriere M, Denis D, Godbout C, Lamontagne S, Rochette C, Sawyer N, Tremblay NM, Belley M, Gallant M, Dufresne C, Gareau Y, Ruel R, Juteau H, Labelle M, Ouimet N, Metters KM
The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs.
Biochim Biophys Acta. 2000 Jan 17;1483(2):285-93.
- PubMed ID
- 10634944 [ View in PubMed]
- Abstract
Stable cell lines that individually express the eight known human prostanoid receptors (EP(1), EP(2), EP(3), EP(4), DP, FP, IP and TP) have been established using human embryonic kidney (HEK) 293(EBNA) cells. These recombinant cell lines have been employed in radioligand binding assays to determine the equilibrium inhibitor constants of known prostanoid receptor ligands at these eight receptors. This has allowed, for the first time, an assessment of the affinity and selectivity of several novel compounds at the individual human prostanoid receptors. This information should facilitate interpretation of pharmacological studies that employ these ligands as tools to study human tissues and cell lines and should, therefore, result in a greater understanding of prostanoid receptor biology.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Dinoprostone Prostaglandin E2 receptor EP2 subtype Ki (nM) 4.9 N/A N/A Details Dinoprostone Solute carrier organic anion transporter family member 2A1 Ki (nM) >10000 N/A N/A Details Latanoprost Prostaglandin F2-alpha receptor Ki (nM) 555 N/A N/A Details Latanoprost Prostaglandin F2-alpha receptor Ki (nM) 2.8 N/A N/A Details Misoprostol Prostaglandin E2 receptor EP2 subtype Ki (nM) 34 N/A N/A Details