2Y6M

Crystal structure of EphA4 kinase domain

2Y6M の概要

• エントリーDOI: 10.2210/pdb2y6m/pdb
• 関連するPDBエントリー: 1B0X 2XYU 2Y6O
• 分子名称: EPHRIN TYPE-A RECEPTOR 4, GLYCEROL (3 entities in total)
• 機能のキーワード: transferase
• 由来する生物種: MUS MUSCULUS (HOUSE MOUSE)
• 細胞内の位置: Cell membrane; Single-pass type I membrane protein: Q03137
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 33207.35

構造登録者

Farenc, C.J.A.,Celie, P.H.N.,Siegal, G. (登録日: 2011-01-25, 公開日: 2011-11-02, 最終更新日: 2023-12-20)

主引用文献

Farenc, C.J.A.,Celie, P.H.N.,Tensen, C.P.,Siegal, G.
Crystal Structure of the Epha4 Protein Tyrosine Kinase Domain in the Apo- and Dasatinib-Bound State.
FEBS Lett., 585:3593-, 2011

PubMed Abstract: The Eph family of receptor tyrosine kinases regulates diverse cellular processes while the over-expression of a member of this family, EphA4, has been reported in a variety of malignant carcinomas. To gain insight into molecular mechanisms and to facilitate structure-based inhibitor design, we solved the crystal structure of the native EphA4 kinase domain in both the apo and dasatinib bound forms. Analysis of the two structures provides insight into structural features of inhibitor binding and revealed a hydrophobic back-pocket in the ATP- binding site of EphA4 which was previously unidentified. The structures suggest a route towards development of novel and specific inhibitors.

PubMed: 22036717
DOI: 10.1016/J.FEBSLET.2011.10.028

実験手法

X-RAY DIFFRACTION (1.7 Å)