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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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Detalles Bibliográficos
Autores principales: 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: Online Artículo Texto
Lenguaje:English
Publicado: Newlands Press Ltd 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6803818/
https://www.ncbi.nlm.nih.gov/pubmed/31633398
http://dx.doi.org/10.4155/fmc-2019-0181