Structure-activity relationship of triaryl propionic acid analogues on the human EP3 prostanoid receptor.
Potent and selective ligands for the human EP3 prostanoid receptor are described. Triaryl compounds bearing an ortho-substituted propionic acid moiety were identified as potent EP3 antagonists based on the SAR described herein. The binding affinities of key compound on all eight human prostanoid receptors is reported.
Gallant
Michel
M
Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire-Dorval, Québec, Canada H9R 4P8. michel_gallant@merck.com
Belley
Michel
M
Carrière
Marie-Claude
MC
Chateauneuf
Anne
A
Denis
Danielle
D
Lachance
Nicolas
N
Lamontagne
Sonia
S
Metters
Kathleen M
KM
Sawyer
Nicole
N
Slipetz
Deborah
D
Truchon
Jean François
JF
Labelle
Marc
M
D000818:Animals; D045744:Cell Line, Tumor; D000242:Cyclic AMP / Q000378:metabolism; D006801:Humans; D007202:Indicators and Reagents; D007700:Kinetics; D011487:Protein Conformation; D051381:Rats; D018078:Receptors, Prostaglandin E / Q000187:drug effects*; D058308:Receptors, Prostaglandin E, EP3 Subtype; D013329:Structure-Activity Relationship
D007202:Indicators and Reagents; C545647:PTGER3 protein, human; D018078:Receptors, Prostaglandin E; D058308:Receptors, Prostaglandin E, EP3 Subtype; D000242:Cyclic AMP