title: Structural features of subtype-selective EP receptor modulators.
abstract: Prostaglandin E2 is a potent endogenous molecule that binds to four different G-protein-coupled receptors: EP1-4. Each of these receptors is a valuable drug target, with distinct tissue localisation and signalling pathways. We review the structural features of EP modulators required for subtype-selective activity, as well as the structural requirements for improved pharmacokinetic parameters. Novel EP receptor subtype selective agonists and antagonists appear to be valuable drug candidates in the therapy of many pathophysiological states, including ulcerative colitis, glaucoma, bone healing, B cell lymphoma, neurological diseases, among others, which have been studied in vitro, in vivo and in early phase clinical trials.
authors: University of Ljubljana, Faculty of Pharmacy, Askerceva cesta 7, 1000 Ljubljana, Slovenia.
authors: Tijana
authors: T
authors: Markovič
authors: University of Ljubljana, Faculty of Pharmacy, Askerceva cesta 7, 1000 Ljubljana, Slovenia.
authors: Žiga
authors: Ž
authors: Jakopin
authors: University of Ljubljana, Faculty of Pharmacy, Askerceva cesta 7, 1000 Ljubljana, Slovenia.
authors: Marija Sollner
authors: MS
authors: Dolenc
authors: University of Ljubljana, Faculty of Pharmacy, Askerceva cesta 7, 1000 Ljubljana, Slovenia. Electronic address: irena.mlinaric-rascan@ffa.uni-lj.si.
authors: Irena
authors: I
authors: Mlinarič-Raščan
mesh_terms: D000818:Animals; D015232:Dinoprostone / Q000737:chemistry; D015195:Drug Design; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D058990:Molecular Targeted Therapy; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D011485:Protein Binding; D058306:Receptors, Prostaglandin E, EP1 Subtype / Q000819:agonists / Q000037:antagonists & inhibitors; D058307:Receptors, Prostaglandin E, EP2 Subtype / Q000819:agonists / Q000037:antagonists & inhibitors; D058308:Receptors, Prostaglandin E, EP3 Subtype / Q000819:agonists / Q000037:antagonists & inhibitors; D058309:Receptors, Prostaglandin E, EP4 Subtype / Q000819:agonists / Q000037:antagonists & inhibitors
chemical_list: D008024:Ligands; D004364:Pharmaceutical Preparations; D058306:Receptors, Prostaglandin E, EP1 Subtype; D058307:Receptors, Prostaglandin E, EP2 Subtype; D058308:Receptors, Prostaglandin E, EP3 Subtype; D058309:Receptors, Prostaglandin E, EP4 Subtype; D015232:Dinoprostone