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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Pubblicato in:Eur J Med Chem
Autori principali: 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.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2018
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Article
Accesso online: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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