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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Udgivet i:Structure
Main Authors: 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.
Format: Artigo
Sprog:Inglês
Udgivet: Cell Press 2015
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Article
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4671956/
https://ncbi.nlm.nih.gov/pubmed/26636255
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.str.2015.10.016
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