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pharmacoeconomics (6) 15 Miscellaneous (49)

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Abstract #69964 Published in IGR 18-2

Structural features of subtype-selective EP receptor modulators

Markovič T; Jakopin Ž; Dolenc MS; Mlinarič-Raščan I
Drug Discovery Today 2017; 22: 57-71

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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.

University of Ljubljana, Faculty of Pharmacy, Askerceva cesta 7, 1000 Ljubljana, Slovenia.

Full article

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Classification:

3.8 Pharmacology (Part of: 3 Laboratory methods)
11.4 Prostaglandins (Part of: 11 Medical treatment)

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