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Arylquins Target Vimentin to Trigger Par-4 Secretion for Tumor Cell Apoptosis

The tumor suppressor protein Par-4, which is secreted by normal cells, selectively induces apoptosis in cancer cells. We identified a 3-arylquinoline derivative, designated Arylquin 1, as a potent Par-4 secretagogue in cell cultures and mice. Mechanistically, Arylquin 1 binds to vimentin, displaces...

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Detalles Bibliográficos
Autores principales: Burikhanov, Ravshan, Sviripa, Vitaliy M., Hebbar, Nikhil, Zhang, Wen, Layton, W. John, Hamza, Adel, Zhan, Chang-Guo, Watt, David S., Liu, Chunming, Rangnekar, Vivek M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4201913/
https://www.ncbi.nlm.nih.gov/pubmed/25218743
http://dx.doi.org/10.1038/nchembio.1631
Descripción
Sumario:The tumor suppressor protein Par-4, which is secreted by normal cells, selectively induces apoptosis in cancer cells. We identified a 3-arylquinoline derivative, designated Arylquin 1, as a potent Par-4 secretagogue in cell cultures and mice. Mechanistically, Arylquin 1 binds to vimentin, displaces Par-4 from vimentin for secretion and triggers the efficient paracrine apoptosis of diverse cancer cells. Thus, targeting vimentin with Par-4 secretagogues efficiently induces paracrine apoptosis of tumor cells.