5-Aryl-1,3,4-oxadiazol-2-ylthioalkanoic Acids: A Highly Potent New Class of Inhibitors of Rho/Myocardin-Related Transcription Factor (MRTF)/Serum Reponse Factor (SRF)-Mediated Gene Transcription as Potential Antifibrotic Agents for Scleroderma

Through a phenotypic high throughput screen (HTS) using a serum response element luciferase (SRE.L) promoter, we identified a novel 5-aryl-1,3,4-oxadiazol-2-ylthiopropionic acid lead inhibitor of Rho/MRTF/SRF-mediated gene transcription with good potency (IC(50) = 180 nM). We were able to rapidly im...

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Detalhes bibliográficos
Publicado no:J Med Chem
Main Authors: Kahl, Dylan J., Hutchings, Kim M., Lisabeth, Erika Mathes, Haak, Andrew J., Leipprandt, Jeffrey R., Dexheimer, Thomas, Khanna, Dinesh, Tsou, Pei-Suen, Campbell, Phillip L., Fox, David A., Wen, Bo, Sun, Duxin, Bailie, Marc, Neubig, Richard R., Larsen, Scott D.
Formato: Artigo
Idioma:Inglês
Publicado em: 2019
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6590913/
https://ncbi.nlm.nih.gov/pubmed/30951312
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b01772
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