1MUO

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

1MUO の概要

• エントリーDOI: 10.2210/pdb1muo/pdb
• 分子名称: Aurora-related kinase 1, ADENOSINE (2 entities in total)
• 機能のキーワード: transferase
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cytoplasm, cytoskeleton, centrosome: O14965
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 34699.48

構造登録者

Cheetham, G.M.T.,Knegtel, R.M.A.,Coll, J.T.,Renwick, S.B.,Swenson, L.,Weber, P.,Lippke, J.A.,Austen, D.A. (登録日: 2002-09-24, 公開日: 2003-04-15, 最終更新日: 2024-02-14)

主引用文献

Cheetham, G.M.T.,Knegtel, R.M.A.,Coll, J.T.,Renwick, S.B.,Swenson, L.,Weber, P.,Lippke, J.A.,Austen, D.A.
Crystal Structure of Aurora-2, an Oncogenic Serine/Threonine Kinase
J.Biol.Chem., 277:42419-42422, 2002

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.

PubMed: 12237287
DOI: 10.1074/jbc.C200426200

実験手法

X-RAY DIFFRACTION (2.9 Å)