Validating aurora b as an anticancer drug target

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Treatment options for a variety of deadly cancers remain limited and the productivity of existing drug development pipelines, despite years of biomedical research, has been steadily declining.

This is partly because current drug discovery efforts are mainly focusing on previously validated 'druggable' protein families such as kinases [].

While the wealth of information in these datasets presents an opportunity to leverage these for finding novel drug targets, it remains a challenge to systematically integrate all these highly heterogeneous sources of information to identify novel anti-cancer drug targets.

Three mutations map to residues in the ATP-binding pocket that are distinct from the “gatekeeper” residue.

The mutants retain wild-type catalytic activity and were resistant to all of the Aurora inhibitors tested.

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