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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)...
Autores principales: | Ciotti, Sonia, Sgarra, Riccardo, Sgorbissa, Andrea, Penzo, Carlotta, Tomasella, Andrea, Casarsa, Federico, Benedetti, Fabio, Berti, Federico, Manfioletti, Guidalberto, Brancolini, Claudio |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Nature Publishing Group UK
2018
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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 |
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