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...

ea0063gp223 | Adrenal and Neuroendocrine - Clinical (1) | ECE2019

Small molecule allosteric agonist of relaxin receptor ML290 demonstrates antifibrotic properties in liver fibrosis

Kaftanovskaya Elena , Ng Hooi Hooi , Soula Mariluz , Rivas Bryan , Myhr Courtney , Ho Brian , Cervantes Briana , Bishop Colin , Shupe Thomas , Wilson Kenneth , Barnaeva Elena , Ferrer Marc , Southall Noel , Marugan Juan , Agoulnik Irina , Agoulnik Alexander

The beneficial effects of relaxin peptide treatment have been demonstrated in animal models of liver fibrosis. However, the low stability of peptide in vivo prevents using it in chronic treatments. We have identified a series of small molecule allosteric agonists of the human relaxin receptor, RXFP1. The therapeutic effects of lead compound ML290 was tested in various models of liver fibrosis. To analyze the anti-fibrotic effects of ML290 on gene expression, we used p...