Identification of novel agonist of the Relaxin family peptide receptor 2 (RXFP2) as potential new therapeutics for testicular maldescent

National Center For Advancing Translational Sciences

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Abstract

During this period, the collaborative team has worked to validate and characterize hits previously identified in the primary screen, focusing on a several chemotypes for medicinal chemistry optimization. Significant improvements in potency and efficacy were attained. Additional molecules were designed, synthesized, and tested for RXFP2 agonism using cAMP and luciferase reporter assays. The team is continuing to pursue in vitro assays using progenitor bone cells that will facilitate functional characterization of RXFP2 agonism. Pharmacokinetics and metabolism studies of an optimized compound have been completed and the efficay of lead molecule is being assessed in mouse models of osteoporosis.