Optimization of the first small-molecule relaxin/insulin-like family peptide receptor (RXFP1) agonists: Activation results in an antifibrotic gene expression profile.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.06.008
Abstract: A dose responsive quantitative high throughput screen (qHTS) of >350,000 compounds against a human relaxin/insulin-like family peptide receptor (RXFP1) transfected HEK293 cell line identified 2-acetamido-N-phenylbenzamides 1 and 3 with modest agonist activity. An extensive structure-activity study… read more here.
Keywords: like family; family peptide; insulin like; receptor rxfp1 ... See more keywords
ML290 is a biased allosteric agonist at the relaxin receptor RXFP1
Sign Up to like & getrecommendations! Published in 2017 at "Scientific Reports"
DOI: 10.1038/s41598-017-02916-5
Abstract: Activation of the relaxin receptor RXFP1 has been associated with improved survival in acute heart failure. ML290 is a small molecule RXFP1 agonist with simple structure, long half-life and high stability. Here we demonstrate that… read more here.
Keywords: rxfp1; accumulation; relaxin receptor; receptor rxfp1 ... See more keywords
The relaxin receptor RXFP1 signals through a mechanism of autoinhibition
Sign Up to like & getrecommendations! Published in 2022 at "Nature Chemical Biology"
DOI: 10.1101/2022.01.22.477343
Abstract: The relaxin family peptide receptor 1 (RXFP1) is the receptor for relaxin-2, an important regulator of reproductive and cardiovascular physiology. RXFP1 is a multi-domain G protein-coupled receptor (GPCR) with an ectodomain consisting of a low-density… read more here.
Keywords: relaxin; receptor rxfp1; rxfp1 signals; mechanism ... See more keywords