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

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

Pharmacology

Research output: Contribution to journal › Article › Research › peer-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 language	English
Pages (from-to)	640 - 651
Number of pages	12
Journal	Drug Discovery Today
Volume	13
Issue number	15-16
Publication status	Published - 2008

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@article{8e91c3f43af84d31879bf589b5e1e75b,

title = "Relaxin family peptide receptors - from orphans to therapeutic targets",

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.",

author = "{van der Westhuizen}, {Emma Therese} and Halls, {Michelle Louise} and Samuel, {Chrishan S} and Ross Bathgate and Unemori, {Elaine N} and Sutton, {Steven W} and Summers, {Roger James}",

year = "2008",

language = "English",

volume = "13",

pages = "640 -- 651",

journal = "Drug Discovery Today",

issn = "1359-6446",

publisher = "Elsevier",

number = "15-16",

}

Relaxin family peptide receptors - from orphans to therapeutic targets. / van der Westhuizen, Emma Therese ; Halls, Michelle Louise ; Samuel, Chrishan S; Bathgate, Ross; Unemori, Elaine N; Sutton, Steven W; Summers, Roger James.

In: Drug Discovery Today, Vol. 13, No. 15-16, 2008, p. 640 - 651.

Research output: Contribution to journal › Article › Research › peer-review

TY - JOUR

T1 - Relaxin family peptide receptors - from orphans to therapeutic targets

AU - van der Westhuizen, Emma Therese

AU - Halls, Michelle Louise

AU - Samuel, Chrishan S

AU - Bathgate, Ross

AU - Unemori, Elaine N

AU - Sutton, Steven W

AU - Summers, Roger James

PY - 2008

Y1 - 2008

N2 - 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.

AB - 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.

UR - http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=18675759

M3 - Article

VL - 13

SP - 640

EP - 651

JO - Drug Discovery Today

JF - Drug Discovery Today

SN - 1359-6446

IS - 15-16

ER -