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Article

Halogen-enriched fragment libraries as leads for drug rescue of mutant p53.

Journal of the American Chemical Society - 18 Apr 2012

Wilcken Rainer, Liu Xiangrui, Zimmermann Markus O, Rutherford Trevor J, Fersht Alan R, Joerger Andreas C, Boeckler Frank M

Abstract excerpt

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 complement classical approaches. From screening of HEFLibs and subsequent structure-guided design, we developed substituted...

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Identifiers

PMID: 22439615
DOI: 10.1021/ja301056a
PMCID: PMC3789257

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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