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Diarylthiophenes as inhibitors of the pore-forming protein perforin

Evolution from a furan-containing high-throughput screen (HTS) hit (1) resulted in isobenzofuran-1(3H)-one (2) as a potent inhibitor of the function of both isolated perforin protein and perforin delivered in situ by intact KHYG-1 NK cells. In the current study, structure–activity relationship (SAR)...

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Detalles Bibliográficos
Autores principales: Miller, Christian K., Huttunen, Kristiina M., Denny, William A., Jaiswal, Jagdish K., Ciccone, Annette, Browne, Kylie A., Trapani, Joseph A., Spicer, Julie A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Science Ltd 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4706532/
https://www.ncbi.nlm.nih.gov/pubmed/26711151
http://dx.doi.org/10.1016/j.bmcl.2015.12.003