Relaxin family peptide receptors - from orphans to therapeutic targets

Emma Therese van der Westhuizen, Michelle Louise Halls, Chrishan S Samuel, Ross Bathgate, Elaine N Unemori, Steven W Sutton, Roger James Summers

Research output: Contribution to journalArticleResearchpeer-review

53 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)640 - 651
Number of pages12
JournalDrug Discovery Today
Volume13
Issue number15-16
Publication statusPublished - 2008

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