Identification of small molecule RXFP3 ligands

National Center For Advancing Translational Sciences

Investigators

Abstract

Novel small molecule RXFP3 agonists and antagonists will be valuable tools to elucidate the functions of relaxin-3 and its actions at RXFP3 receptors. During this period, the project team successfully developed a 1536-well high-throughput assay to screen for small molecules that agonize or antagonize the RXFP3 receptor. More than 50,000 small molecules were screened for effects on cAMP levels, and several counterscreens have been developed to characterize screening hits and help identify on-target RXFP3 modulators.