Cargando…
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...
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 |
Ejemplares similares
-
Aminobenzothiazole derivatives stabilize the thermolabile p53 cancer mutant Y220C and show anticancer activity in p53-Y220C cell lines
por: Baud, Matthias G.J., et al.
Publicado: (2018) -
Targeting Cavity-Creating p53 Cancer Mutations with
Small-Molecule Stabilizers: the Y220X Paradigm
por: Bauer, Matthias R., et al.
Publicado: (2020) -
Harnessing Fluorine–Sulfur Contacts and Multipolar
Interactions for the Design of p53 Mutant Y220C Rescue Drugs
por: Bauer, Matthias R., et al.
Publicado: (2016) -
Discovery of Nanomolar-Affinity
Pharmacological Chaperones
Stabilizing the Oncogenic p53 Mutant Y220C
por: Stephenson Clarke, Joseph R., et al.
Publicado: (2022) -
Small molecule induced reactivation of mutant p53 in cancer cells
por: Liu, Xiangrui, et al.
Publicado: (2013)