Relaxin family peptide receptors – from orphans to therapeutic targets

The relaxin family peptides have distinct expression profiles and physiological functions. Several of them are the cognate ligands for 4 G-protein-coupled relaxin family peptide receptors (RXFPs; formerly LGR7, LGR8, GPCR135, GPCR142). The relaxin/RXFP1 system has roles in reproductive physiology bu...

Full description

Saved in:
Bibliographic Details
Published in:Drug discovery today 2008-08, Vol.13 (15), p.640-651
Main Authors: van der Westhuizen, Emma T., Halls, Michelle L., Samuel, Chrishan S., Bathgate, Ross A.D., Unemori, Elaine N., Sutton, Steven W., Summers, Roger J.
Format: Article
Language:English
Subjects:
Animals
Anti-Anxiety Agents - therapeutic use
Anti-Obesity Agents - therapeutic use
Biological and medical sciences
Heart Failure - drug therapy
Heart Failure - metabolism
Hormones. Endocrine system
Humans
Ligands
Medical sciences
Orphan Drug Production
Pharmacology. Drug treatments
Receptors, G-Protein-Coupled - antagonists & inhibitors
Receptors, G-Protein-Coupled - genetics
Receptors, G-Protein-Coupled - physiology
Receptors, Peptide - antagonists & inhibitors
Receptors, Peptide - genetics
Receptors, Peptide - physiology
Recombinant Proteins - therapeutic use
Relaxin - metabolism
Relaxin - therapeutic use
Signal Transduction
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The relaxin family peptides have distinct expression profiles and physiological functions. Several of them are the cognate ligands for 4 G-protein-coupled relaxin family peptide receptors (RXFPs; formerly LGR7, LGR8, GPCR135, GPCR142). The relaxin/RXFP1 system has roles in reproductive physiology but is also involved in fibrosis, wound healing and responses to infarction. Relaxin has a potential use in congestive heart failure where fibrosis plays an important role in organ failure. The INSL3/RXFP2 system has biological roles in reproductive biology that may have limited therapeutic potential. However, the recently characterized relaxin-3/RXFP3 system is important in stress/anxiety and body composition. RXFP3 receptor antagonists are potentially novel anti-anxiety and anti-obesity drugs. Relaxin family peptide receptors are a recently de-orphanized group of G-protein coupled receptors with great potential as therapeutic targets for the treatment of anxiety, obesity and diseases involving fibrosis.
ISSN:1359-6446
1878-5832
DOI:10.1016/j.drudis.2008.04.002