Crystal structure of aurora-2, an oncogenic serine/threonine kinase.
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Cheetham GM, Knegtel RM, Coll JT, Renwick SB, Swenson L, Weber P, Lippke JA, Austen DA
Crystal structure of aurora-2, an oncogenic serine/threonine kinase.
J Biol Chem. 2002 Nov 8;277(45):42419-22. Epub 2002 Sep 16.
- PubMed ID
- 12237287 [ View in PubMed]
- Abstract
Aurora-2 is a key member of a closely related subgroup of serine/threonine kinases that plays important roles in the completion of essential mitotic events. Aurora-2 is oncogenic and amplified in various human cancers and could be an important therapeutic target for inhibitory molecules that would disrupt the cell cycle and block proliferation. We report the first crystal structure of Aurora-2 kinase in complex with adenosine. Analysis of residues in the active site suggests differences with structurally and biologically related protein kinases. The activation loop, which contains residues specific to the Aurora family of kinases, has a unique conformation. These results provide valuable insight into the design of selective and highly potent ATP-competitive inhibitors of the Aurora kinases.