Exploiting Transient Protein States for the Design of Small-Molecule Stabilizers of Mutant p53

The destabilizing p53 cancer mutation Y220C creates an extended crevice on the surface of the protein that can be targeted by small-molecule stabilizers. Here, we identify different classes of small molecules that bind to this crevice and determine their binding modes by X-ray crystallography. These...

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Detalles Bibliográficos
Autores principales: Joerger, Andreas C., Bauer, Matthias R., Wilcken, Rainer, Baud, Matthias G.J., Harbrecht, Hannes, Exner, Thomas E., Boeckler, Frank M., Spencer, John, Fersht, Alan R.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Cell Press 2015
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4671956/
https://www.ncbi.nlm.nih.gov/pubmed/26636255
http://dx.doi.org/10.1016/j.str.2015.10.016

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