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An integrated chemical biology approach provides insight into Cdk2 functional redundancy and inhibitor sensitivity.

Chemistry & biology - 24 Aug 2012

Echalier Aude, Cot Emilie, Camasses Alain, Hodimont Elsie, Hoh François, Jay Philippe, Sheinerman Felix, Krasinska Liliana, Fisher Daniel

Abstract excerpt

Cdk2 promotes DNA replication and is a promising cancer therapeutic target, but its functions appear redundant with Cdk1, an essential Cdk affected by most Cdk2 inhibitors. Here, we present an integrated multidisciplinary approach to address Cdk redundancy. Mathematical modeling of enzymology data predicted conditions allowing selective chemical Cdk2 inhibition. Together with experiments in Xenopus egg extracts,...

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Identifiers

PMID: 22921070
DOI: 10.1016/j.chembiol.2012.06.015

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