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Article

Harnessing Fluorine-Sulfur Contacts and Multipolar Interactions for the Design of p53 Mutant Y220C Rescue Drugs.

ACS chemical biology - 19 Aug 2016

Bauer Matthias R, Jones Rhiannon N, Baud Matthias G J, Wilcken Rainer, Boeckler Frank M, Fersht Alan R, Joerger Andreas C, Spencer John

Abstract excerpt

Many oncogenic mutants of the tumor suppressor p53 are conformationally unstable, including the frequently occurring Y220C mutant. We have previously developed several small-molecule stabilizers of this mutant. One of these molecules, PhiKan083, 1-(9-ethyl-9H-carbazole-3-yl)-N-methylmethanamine, binds to a mutation-induced surface crevice with a KD = 150 μM, thereby increasing the melting temperature of the...

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Identifiers

PMID: 27267810
DOI: 10.1021/acschembio.6b00315
PMCID: PMC4994063

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