Optimization of the first small-molecule relaxin/insulin-like family peptide receptor (RXFP1) agonists: Activation results in an antifibrotic gene expression profile

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 stud...

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Detalhes bibliográficos
Publicado no:Eur J Med Chem
Main Authors: Wilson, Kenneth J., Xiao, Jingbo, Chen, Catherine Z., Huang, Zaohua, Agoulnik, Irina U., Ferrer, Marc, Southall, Noel, Hu, Xin, Zheng, Wei, Xu, Xin, Wang, Amy, Myhr, Courtney, Barnaeva, Elena, George, Emmett R., Agoulnik, Alexander I., Marugan, Juan J.
Formato: Artigo
Idioma:Inglês
Publicado em: 2018
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6102074/
https://ncbi.nlm.nih.gov/pubmed/30006176
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.ejmech.2018.06.008
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