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

Investigators

Linked publications, trials & patents

Abstract

During this reporting period, the collaborative team has worked to define the SAR of a first-in-class RXFP2 agonist that the team recently published. Lead optimization included characterization of receptor activation (cAMP induction), in vitro ADME, and pharmacokinetic properties. Mutagenesis studies were conducted to explore the binding site of the compounds and virtual screening was employed to identify additional chemotypes that might activate the receptor. A cryoEM structure of the receptor in complex with the small molecule agonist is being pursued. Additional efficacy models related to male fertility are also being explored.