2. Academic Validation
  3. The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs

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. doi: 10.1016/s1388-1981(99)00164-x.
M Abramovitz 1,  M Adam,  Y Boie,  M Carrière,  D Denis,  C Godbout,  S Lamontagne,  C Rochette,  N Sawyer,  N M Tremblay,  M Belley,  M Gallant,  C Dufresne,  Y Gareau,  R Ruel,  H Juteau,  M Labelle,  N Ouimet,  K M Metters
Affiliations

Affiliation

  • 1 Department of Biochemistry and Molecular Biology, Merck Frosst Centre for Therapeutic Research, Box 1005 Pointe-Claire-, Dorval, Que., Canada.
PMID: 10634944 DOI: 10.1016/s1388-1981(99)00164-x
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.

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