Mammalian relaxin receptors

Abstract

High affinity relaxin receptors, polypeptide compositions related thereto, as well as nucleotide compositions encoding the same, are provided. These proteins, herein termed LGR7 and LGR8, are orphan leucine-repeat-containing, G protein-coupled receptors. These receptors have a wide and a unique tissue expression pattern. The receptors, particularly soluble fragments thereof, are useful as therapeutic agents capable of inhibiting the action of relaxin and InsL3. The receptors and fragments thereof also find use in the screening and design of relaxin agonists and antagonists. Conditions treatable with relaxin agonists or antagonists include prevention or induction of labor, treatment of endometriosis, treatment of skin conditions such as scleroderma that require collagen or extracellular matrix remodelling. Additionally, relaxin has been implicated in the dilation of blood vessels' smooth muscle cells directly and through release of nitric oxide and atrial natriuretic peptide. Relaxin has also been used in the treatment of severe chronic pain, particularly pain arising from stretching, swelling, or dislocation of tissues.

1 - 5 . (canceled) 
     
     
         6 . A method of inhibiting premature labor, the method comprising administering a patient suffering from premature labor an antagonist of LGR7 receptor activity. 
     
     
         7 - 23 . (canceled) 
     
     
         24 . The method of  claim 6 , wherein the antagonist of LGR7 receptor activity comprises a soluble ligand-binding region of LGR7. 
     
     
         25 . The method of  claim 24 , wherein the antagonist of LGR7 receptor binding activity is a soluble ligand-binding region of LGR7 truncated to delete LGR7 transmembrane domain. 
     
     
         26 . The method of  claim 25 , wherein the antagonist of LGR7 receptor binding activity comprises at least 100 amino acids of human LGR7 protein.