title: Nonpeptide Urotensin-II receptor agonists and antagonists: review and structure-activity relationships.
abstract: Human Urotensin-II (hU-II) is a cyclic 11-amino acid peptide that plays a role in cardiovascular homeostasis. Its receptor is a member of the class A of G-protein-coupled receptors, called GPR14. In recent years, several nonpeptide ligands have been reported in the literature. Most were identified by high-throughput screening and optimized by medicinal chemistry methods. Other nonpeptide ligands were discovered starting from the 3D structure of hU-II or other ligands. They were identified by a virtual screening approach based on a 3D pharmacophore or by structural similarity with others cyclic peptides. In this review, nonpeptide agonists and antagonists are presented in relation to structure-activity relationships.
authors.affiliation: Université de Caen, U.F.R. des Sciences Pharmaceutiques, Centre d'Etudes et de Recherche sur le Médicament de Normandie, 5 rue Vaubénard, 14032 Caen Cedex, France.
authors.forename: Elodie
authors.initials: E
authors.lastname: Lescot
authors.forename: Ronan
authors.initials: R
authors.lastname: Bureau
authors.forename: Sylvain
authors.initials: S
authors.lastname: Rault
mesh_terms: D001552:Benzazepines / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D006860:Hydrogen Bonding; D008024:Ligands; D015394:Molecular Structure; D011487:Protein Conformation; D011759:Pyrrolidines / Q000737:chemistry / Q000378:metabolism; D011804:Quinolines / Q000737:chemistry / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry / Q000378:metabolism; D014508:Urea / Q000737:chemistry / Q000378:metabolism; D014579:Urotensins / Q000737:chemistry* / Q000235:genetics / Q000378:metabolism*
chemical_list: D001552:Benzazepines; D008024:Ligands; D011759:Pyrrolidines; D011804:Quinolines; D043562:Receptors, G-Protein-Coupled; D013449:Sulfonamides; C121697:UTS2R protein, human; D014579:Urotensins; D014508:Urea; C029677:urotensin II