Receptors for relaxin family peptides

Ann N Y Acad Sci. 2005 May:1041:61-76. doi: 10.1196/annals.1282.010.

Abstract

Recent studies have identified four receptors that are the physiological targets for relaxin family peptides. All are class I (rhodopsin like) G-protein-coupled receptors with LGR7 (RXFP1) and LGR8 (RXFP2) being type C leucine-rich repeat-containing receptors, whereas GPCR135 (RXFP3) and GPCR142 (RXFP4) resemble receptors that respond to small peptides such as somatostatin and angiotensin II. The cognate ligands for the receptors have been identified: relaxin for RXFP1; INSL3 for RXFP2; relaxin 3 for RXFP3 and INSL5 for RXFP4. RXFP1 and RXFP2 receptors produce increases in intracellular cAMP levels upon stimulation, although the response is complex and contains a component sensitive to PI-3-kinase inhibitors. There is also evidence that RXFP1 can activate Erk1/2 and nitric oxide synthase, and relaxin has been reported to enter cells and activate glucocorticoid receptors. In contrast, RXFP3 and RXFP4 couple to Gi by a pertussis toxin-sensitive mechanism to cause inhibition of cAMP production. Now that the receptors for relaxin family peptides and their cognate ligands have been identified, we suggest a nomenclature for both the peptides and the receptors that we hope will be helpful to researchers in this rapidly advancing field.

Publication types

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

MeSH terms

  • Animals
  • Gene Expression
  • Humans
  • Ligands
  • Receptors, G-Protein-Coupled
  • Receptors, Peptide / agonists
  • Receptors, Peptide / antagonists & inhibitors
  • Receptors, Peptide / genetics
  • Receptors, Peptide / metabolism*
  • Relaxin / classification*
  • Relaxin / metabolism*
  • Signal Transduction

Substances

  • Ligands
  • Receptors, G-Protein-Coupled
  • Receptors, Peptide
  • relaxin receptors
  • Relaxin