biostudies-literatureHossain MAMonash Biomedicine Discovery Institute, Monash UniversityNational Health and Medical Research Council842-853https://www.ebi.ac.uk/biostudies/studies/S-EPMC10186362biostudies-literatureUnknown6(5)H2 relaxin is a peptide hormone that exerts its biological actions through the G protein-coupled receptor, RXFP1. The numerous important biological functions of H2 relaxin, including potent renal, vasodilatory, cardioprotective, and anti-fibrotic actions, have resulted in considerable interest in its use as a therapeutic for various cardiovascular diseases and other fibrotic indications. Interestingly though, H2 relaxin and RXFP1 have been shown to be overexpressed in prostate cancer, allowing for the downregulation or blocking of relaxin/RXFP1 to decrease prostate tumor growth. These findings suggest the application of an RXFP1 antagonist for the treatment of prostate cancer. However, these therapeutically relevant actions are still poorly understood and have been hindered by the lack of ACS pharmacology & translational scienceDevelopment of Novel High-Affinity Antagonists for the Relaxin Family Peptide Receptor 1.PMC10186362GNT2001178GNT1135837GNT2001027Handley TSelemidis SHossain MASamuel CSPraveen PHarrison IPBathgate RADNoorzi NAWu HfalseDevelopment of Novel High-Affinity Antagonists for the Relaxin Family Peptide Receptor 1.H2 relaxin is a peptide hormone that exerts its biological actions through the G protein-coupled receptor, RXFP1. The numerous important biological functions of H2 relaxin, including potent renal, vasodilatory, cardioprotective, and anti-fibrotic actions, have resulted in considerable interest in its use as a therapeutic for various cardiovascular diseases and other fibrotic indications. Interestingly though, H2 relaxin and RXFP1 have been shown to be overexpressed in prostate cancer, allowing for the downregulation or blocking of relaxin/RXFP1 to decrease prostate tumor growth. These findings suggest the application of an RXFP1 antagonist for the treatment of prostate cancer. However, these therapeutically relevant actions are still poorly understood and have been hindered by the lack of 2023-01-01T00:00:00Z2023 May2026-06-02T07:01:51.535Z2026-04-15T03:15:34.975ZS-EPMC101863623720081710.1021/acsptsci.3c00053