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.
Publication types
-
Research Support, Non-U.S. Gov't
-
Review
MeSH terms
-
Benzazepines / chemistry
-
Benzazepines / metabolism
-
Humans
-
Hydrogen Bonding
-
Ligands
-
Molecular Structure
-
Protein Conformation
-
Pyrrolidines / chemistry
-
Pyrrolidines / metabolism
-
Quinolines / chemistry
-
Quinolines / metabolism
-
Receptors, G-Protein-Coupled / agonists*
-
Receptors, G-Protein-Coupled / antagonists & inhibitors*
-
Receptors, G-Protein-Coupled / metabolism
-
Structure-Activity Relationship*
-
Sulfonamides / chemistry
-
Sulfonamides / metabolism
-
Urea / chemistry
-
Urea / metabolism
-
Urotensins / chemistry*
-
Urotensins / genetics
-
Urotensins / metabolism*
Substances
-
Benzazepines
-
Ligands
-
Pyrrolidines
-
Quinolines
-
Receptors, G-Protein-Coupled
-
Sulfonamides
-
UTS2R protein, human
-
Urotensins
-
Urea
-
urotensin II