The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs.
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.
Abramovitz
M
M
Department of Biochemistry and Molecular Biology, Merck Frosst Centre for Therapeutic Research, Box 1005 Pointe-Claire-, Dorval, Que., Canada.
Adam
M
M
Boie
Y
Y
Carrière
M
M
Denis
D
D
Godbout
C
C
Lamontagne
S
S
Rochette
C
C
Sawyer
N
N
Tremblay
N M
NM
Belley
M
M
Gallant
M
M
Dufresne
C
C
Gareau
Y
Y
Ruel
R
R
Juteau
H
H
Labelle
M
M
Ouimet
N
N
Metters
K M
KM
D001667:Binding, Competitive; D002460:Cell Line; D002462:Cell Membrane / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D011453:Prostaglandins / Q000378:metabolism*; D011869:Radioligand Assay; D011982:Receptors, Prostaglandin / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism*; D011994:Recombinant Proteins / Q000378:metabolism
D008024:Ligands; D011453:Prostaglandins; D011982:Receptors, Prostaglandin; D011994:Recombinant Proteins