Back to Search
Start Over
Structural features of subtype-selective EP receptor modulators.
- Source :
-
Drug discovery today [Drug Discov Today] 2017 Jan; Vol. 22 (1), pp. 57-71. Date of Electronic Publication: 2016 Aug 06. - Publication Year :
- 2017
-
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.<br /> (Copyright © 2016 The Authors. Published by Elsevier Ltd.. All rights reserved.)
- Subjects :
- Animals
Dinoprostone chemistry
Drug Design
Humans
Ligands
Molecular Structure
Molecular Targeted Therapy
Protein Binding
Pharmaceutical Preparations chemistry
Receptors, Prostaglandin E, EP1 Subtype agonists
Receptors, Prostaglandin E, EP1 Subtype antagonists & inhibitors
Receptors, Prostaglandin E, EP2 Subtype agonists
Receptors, Prostaglandin E, EP2 Subtype antagonists & inhibitors
Receptors, Prostaglandin E, EP3 Subtype agonists
Receptors, Prostaglandin E, EP3 Subtype antagonists & inhibitors
Receptors, Prostaglandin E, EP4 Subtype agonists
Receptors, Prostaglandin E, EP4 Subtype antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1878-5832
- Volume :
- 22
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Drug discovery today
- Publication Type :
- Academic Journal
- Accession number :
- 27506873
- Full Text :
- https://doi.org/10.1016/j.drudis.2016.08.003