ea0049ep754 | Cardiovascular Endocrinology and Lipid Metabolism | ECE2017
Agoulnik Alexander
, Agoulnik Irina
, Hu Xin
, Kaftanovskaya Elena
, Huang Zaohua
, Myhr Courtney
, Xiao Jingbo
, Soula Mariluz
, Ho Brian
, Barnaeva Elena
, Southall Noel
, Ferrer Marc
, Marugan Juan
The anti-fibrotic, vasodilatory, and angiogenic therapeutic properties of relaxin peptide have been shown in several animal models of human diseases and in clinical trials. Using high-throughput screening of small molecule library, structure-activity relationship (SAR) studies, ligand-receptor interaction modeling, site-specific mutagenesis, and transgenic animal studies we discovered the first series of small molecule agonists of relaxin GPCR, RXFP1. The lead compound ML290 i...