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 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.
van der Westhuizen
Emma T
ET
Department of Pharmacology, Monash University, Clayton, 3800 Vic, Australia.
Halls
Michelle L
ML
Samuel
Chrishan S
CS
Bathgate
Ross A D
RA
Unemori
Elaine N
EN
Sutton
Steven W
SW
Summers
Roger J
RJ
D000818:Animals; D014151:Anti-Anxiety Agents / Q000627:therapeutic use; D019440:Anti-Obesity Agents / Q000627:therapeutic use; D006333:Heart Failure / Q000188:drug therapy / Q000378:metabolism; D006801:Humans; D008024:Ligands; D009965:Orphan Drug Production; D043562:Receptors, G-Protein-Coupled / Q000037:antagonists & inhibitors / Q000235:genetics / Q000502:physiology*; D018000:Receptors, Peptide / Q000037:antagonists & inhibitors / Q000235:genetics / Q000502:physiology*; D011994:Recombinant Proteins / Q000627:therapeutic use; D012065:Relaxin / Q000378:metabolism* / Q000627:therapeutic use; D015398:Signal Transduction
D014151:Anti-Anxiety Agents; D019440:Anti-Obesity Agents; D008024:Ligands; D043562:Receptors, G-Protein-Coupled; D018000:Receptors, Peptide; D011994:Recombinant Proteins; C033395:relaxin receptors; D012065:Relaxin