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A structure-guided molecular chaperone approach for restoring the transcriptional activity of the p53 cancer mutant Y220C

AIM: The p53 cancer mutation Y220C creates a conformationally unstable protein with a unique elongated surface crevice that can be targeted by molecular chaperones. We report the structure-guided optimization of the carbazole-based stabilizer PK083. MATERIALS & METHODS: Biophysical, cellular and...

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Publicado en:Future Med Chem
Main Authors: Bauer, Matthias R, Jones, Rhiannon N, Tareque, Raysa K, Springett, Bradley, Dingler, Felix A, Verduci, Lorena, Patel, Ketan J, Fersht, Alan R, Joerger, Andreas C, Spencer, John
Formato: Artigo
Idioma:Inglês
Publicado: Newlands Press Ltd 2019
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Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC6803818/
https://ncbi.nlm.nih.gov/pubmed/31633398
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.4155/fmc-2019-0181
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