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Beamlines | MX Case Study

Inhibitors of Aurora-A Protein Kinase for the Treatment of Cancer

Aurora-A is an essential enzyme which is required for human cells to multiply. Aurora-A has higher activity than normal in many human cancers and is a target for the development of anti-cancer drugs, some of which are in clinical trials. X-ray crystallography is used to characterise how these small molecules interact with Aurora-A, and these data provide information on how they work and allow the production of a new generation of more potent inhibitors.

Aurora
Electron density at 2.8 Å resolution around the site where one of the inhibitors binds. Knowledge of the geometry and neighbouring atoms will inform drug development.

Magda Kosmopoulou and Richard Bayliss, Institute of Cancer Research, London