Novel Small Molecule Agonists of the Relaxin Receptor as Potential Therapy for Heart Failure and Fibrosis
Lead Inventor: Juan Marugan (NCATS)
Inventors: Alexander Agoulnik (Florida International University), Catherine Chen (NCATS), Marc Ferrer-Alegre (NCATS), Noel Southall (NCATS), Jingbo Xiao (NCATS), Wei Zheng (NCATS)
Ref. No.: E-072-2012/0
Abstract: The present invention is directed to novel small molecule agonists of the mammalian relaxin family receptor 1 (RXFP1), including human RXFP1. Activation of RXFP1 induces: 1) vasodilation due to up-regulation of the endothelin system; 2) extracellular matrix remodeling; 3) moderation of inflammation by reducing levels of inflammatory cytokines; and 4) angiogenesis. Small molecule agonists of RXFP1 may be useful in treating acute heart failure, scleroderma, fibrosis, other conditions associated with the biology of relaxin, and in improving reproductive health and wound healing. These compounds are the first and only small molecule agonists of RXFP1.
Identification and Optimization of Small-Molecule Agonists of the Human Relaxin Hormone Receptor RXFP1 •
Nature Communications • June 14, 2013 • Probe Development Branch, NCATS Chemical Genomics Center
Identification of Small-Molecule Agonists of Human Relaxin Family Receptor 1 (RXFP1) by Using a Homogenous Cell-Based cAMP Assay • Journal of Biomolecular Screening • Dec. 4, 2012 • Probe Development Branch, NCATS Chemical Genomics Center