1muo

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1muo, resolution 2.9Å

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CRYSTAL STRUCTURE OF AURORA-2, AN ONCOGENIC SERINE-THREONINE KINASE

Contents

Overview

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.

Disease

Known diseases associated with this structure: Colon cancer, susceptibility to OMIM:[603072]

About this Structure

1MUO is a Single protein structure of sequence from Homo sapiens with ADN as ligand. Full crystallographic information is available from OCA.

Reference

Crystal structure of aurora-2, an oncogenic serine/threonine kinase., Cheetham GM, Knegtel RM, Coll JT, Renwick SB, Swenson L, Weber P, Lippke JA, Austen DA, J Biol Chem. 2002 Nov 8;277(45):42419-22. Epub 2002 Sep 16. PMID:12237287

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