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Discovery of small molecule agonists of the Relaxin Family Peptide Receptor 2. | LitMetric

AI Article Synopsis

  • RXFP2 is a G-protein coupled receptor that specifically responds to the peptide INSL3, playing a crucial role in testicular descent and recently linked to bone health.
  • Researchers have developed a series of small molecule RXFP2 agonists that are effective in promoting gubernacular invagination during embryo development and enhancing bone mineralization in human osteoblasts.
  • These RXFP2 agonists are easy to administer orally and have good pharmacokinetic profiles, paving the way for future studies on their potential therapeutic applications in various diseases.

Article Abstract

The relaxin/insulin-like family peptide receptor 2 (RXFP2) belongs to the family of class A G-protein coupled receptors (GPCRs) and it is the only known target for the insulin-like factor 3 peptide (INSL3). The importance of this ligand-receptor pair in the development of the gubernacular ligament during the transabdominal phase of testicular descent is well established. More recently, RXFP2 has been implicated in maintaining healthy bone formation. In this report, we describe the discovery of a small molecule series of RXFP2 agonists. These compounds are highly potent, efficacious, and selective RXFP2 allosteric agonists that induce gubernacular invagination in mouse embryos, increase mineralization activity in human osteoblasts in vitro, and improve bone trabecular parameters in adult mice. The described RXFP2 agonists are orally bioavailable and display favorable pharmacokinetic properties, which allow for future evaluation of the therapeutic benefits of modulating RXFP2 activation in disease models.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9636434PMC
http://dx.doi.org/10.1038/s42003-022-04143-9DOI Listing

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