Searchable abstracts of presentations at key conferences in endocrinology

ea0049ep754 | Cardiovascular Endocrinology and Lipid Metabolism | ECE2017

Therapeutic potentials of small molecular weight allosteric agonist of relaxin receptor

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...