Novel Small Molecule Agonists of the Relaxin Receptor as Potential Therapy for Heart Failure and Fibrosis
Posted Nov 15 2012 7:00pm
Description of Invention: 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 (AHF), 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.
Acute heart failure
Human and animal reproductive health
First and only small molecule agonists of RXFP1
Potent and highly selective
Bioavailable with excellent exposure
Easy to synthesize and scale-up
In vitro data available
In vivo data available (animal)
Inventors: Juan J Marugan (NCATS) Wei Zheng (NCATS) Marc Ferrer-Alegre (NCATS) Catherine Chen (NCATS) Alexander Agoulnik (Florida International University) Noel T Southall (NCATS) Jingbo Xiao (NCATS)
Chen ZC, et al. Identification of small-molecule agonists of human relaxin family receptor 1 (RXFP1) by utilizing a homogeneous cell-based cAMP assay. J. Biomol. Screen. 2012, accepted.
Collaborative Research Opportunity: The National Center for Advancing Translational Sciences is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize small molecule agonists of RXFP1. For collaboration opportunities, please contact Krishna (Balki) Balakrishnan, Ph.D. at 301-217-2336 or firstname.lastname@example.org .