Published in
Elsevier, Drug Discovery Today, 15-16(13), p. 640-651, 2008
DOI: 10.1016/j.drudis.2008.04.002
Links
Tools
Relaxin family peptide receptors - from orphans to therapeutic targets
,
Elaine N. Unemori,
{Elaine N} Unemori,
Steven W. Sutton,
{Steven W} Sutton,
Roger J. Summers ,
{Roger James Summers
Full text: Download
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.