Halogen-Enriched Fragment Libraries as Leads for Drug Rescue of Mutant p53

[Image: see text] The destabilizing p53 cancer mutation Y220C creates a druggable surface crevice. We developed a strategy exploiting halogen bonding for lead discovery to stabilize the mutant with small molecules. We designed halogen-enriched fragment libraries (HEFLibs) as starting points to compl...

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Detalhes bibliográficos
Main Authors: Wilcken, Rainer, Liu, Xiangrui, Zimmermann, Markus O., Rutherford, Trevor J., Fersht, Alan R., Joerger, Andreas C., Boeckler, Frank M.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2012
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3789257/
https://ncbi.nlm.nih.gov/pubmed/22439615
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ja301056a
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