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The binding landscape of a partially-selective isopeptidase inhibitor with potent pro-death activity, based on the bis(arylidene)cyclohexanone scaffold

Diaryldienone derivatives with accessible β-carbons show strong anti-neoplastic properties, related to their ability to make covalent adducts with free thiols by Michael addition, and low toxicity in vivo. Accumulation of poly-ubiquitylated proteins, activation of the unfolded protein response (UPR)...

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Detalles Bibliográficos
Autores principales: Ciotti, Sonia, Sgarra, Riccardo, Sgorbissa, Andrea, Penzo, Carlotta, Tomasella, Andrea, Casarsa, Federico, Benedetti, Fabio, Berti, Federico, Manfioletti, Guidalberto, Brancolini, Claudio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5833369/
https://www.ncbi.nlm.nih.gov/pubmed/29416018
http://dx.doi.org/10.1038/s41419-017-0259-1