Relaxin family peptide receptors--from orphans to therapeutic targets

Drug Discov Today. 2008 Aug;13(15-16):640-51. doi: 10.1016/j.drudis.2008.04.002. Epub 2008 Jun 6.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Anti-Anxiety Agents / therapeutic use
  • Anti-Obesity Agents / therapeutic use
  • Heart Failure / drug therapy
  • Heart Failure / metabolism
  • Humans
  • Ligands
  • Orphan Drug Production*
  • 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

Substances

  • Anti-Anxiety Agents
  • Anti-Obesity Agents
  • Ligands
  • Receptors, G-Protein-Coupled
  • Receptors, Peptide
  • Recombinant Proteins
  • relaxin receptors
  • Relaxin