title: Structure-activity relationship of triaryl propionic acid analogues on the human EP3 prostanoid receptor.
abstract: 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.
authors.affiliation: Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire-Dorval, Québec, Canada H9R 4P8. michel_gallant@merck.com
authors.forename: Michel
authors.initials: M
authors.lastname: Gallant
authors.forename: Michel
authors.initials: M
authors.lastname: Belley
authors.forename: Marie-Claude
authors.initials: MC
authors.lastname: Carrière
authors.forename: Anne
authors.initials: A
authors.lastname: Chateauneuf
authors.forename: Danielle
authors.initials: D
authors.lastname: Denis
authors.forename: Nicolas
authors.initials: N
authors.lastname: Lachance
authors.forename: Sonia
authors.initials: S
authors.lastname: Lamontagne
authors.forename: Kathleen M
authors.initials: KM
authors.lastname: Metters
authors.forename: Nicole
authors.initials: N
authors.lastname: Sawyer
authors.forename: Deborah
authors.initials: D
authors.lastname: Slipetz
authors.forename: Jean François
authors.initials: JF
authors.lastname: Truchon
authors.forename: Marc
authors.initials: M
authors.lastname: Labelle
mesh_terms: 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
chemical_list: D007202:Indicators and Reagents; C545647:PTGER3 protein, human; D018078:Receptors, Prostaglandin E; D058308:Receptors, Prostaglandin E, EP3 Subtype; D000242:Cyclic AMP