Therapeutic effects of a small molecule agonist of the relaxin receptor ML290 in liver fibrosis.

ABSTRACT: Fibrosis is an underlying cause of cirrhosis and hepatic failure resulting in end stage liver disease with limited pharmacological options. The beneficial effects of relaxin peptide treatment were demonstrated in clinically relevant animal models of liver fibrosis. However, the use of relaxin is problematic because of a short half-life. The aim of this study was to test the therapeutic effects of recently identified small molecule agonists of the human relaxin receptor, relaxin family peptide receptor 1 (RXFP1). The lead compound of this series, ML290, was selected based on its effects on the expression of fibrosis-related genes in primary human stellate cells. RNA sequencing analysis of TGF-β1-activated LX-2 cells showed that ML290 treatment primarily affected extracellular matrix remodel

SUBMITTER: Kaftanovskaya EM 

PROVIDER: S-EPMC6988856 | biostudies-literature | 2019 Nov

REPOSITORIES: biostudies-literature