1MQB

Crystal Structure of Ephrin A2 (ephA2) Receptor Protein Kinase

1MQB の概要

• エントリーDOI: 10.2210/pdb1mqb/pdb
• 関連するPDBエントリー: 1MP8 1MQ4
• 分子名称: Ephrin type-A receptor 2, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER (3 entities in total)
• 機能のキーワード: tyrosine protein kinase, transferase
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cell membrane; Single-pass type I membrane protein: P29317
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 76579.21

構造登録者

Nowakowski, J.,Cronin, C.N.,McRee, D.E.,Knuth, M.W.,Nelson, C.,Pavletich, N.,Rogers, J.,Sang, B.C.,Scheibe, D.N.,Swanson, R.V.,Thompson, D.A. (登録日: 2002-09-16, 公開日: 2003-09-16, 最終更新日: 2024-02-14)

主引用文献

Nowakowski, J.,Cronin, C.N.,McRee, D.E.,Knuth, M.W.,Nelson, C.,Pavletich, N.,Rogers, J.,Sang, B.C.,Scheibe, D.N.,Swanson, R.V.,Thompson, D.A.
Structures of the Cancer Related Aurora-A, FAK and EphA2 Protein Kinases from Nanovolume Crystallography
Structure, 10:1659-1667, 2003

PubMed Abstract: Protein kinases are important drug targets in human cancers, inflammation, and metabolic diseases. This report presents the structures of kinase domains for three cancer-associated protein kinases: ephrin receptor A2 (EphA2), focal adhesion kinase (FAK), and Aurora-A. The expression profiles of EphA2, FAK, and Aurora-A in carcinomas suggest that inhibitors of these kinases may have inherent potential as therapeutic agents. The structures were determined from crystals grown in nanovolume droplets, which produced high-resolution diffraction data at 1.7, 1.9, and 2.3 A for FAK, Aurora-A, and EphA2, respectively. The FAK and Aurora-A structures are the first determined within two unique subfamilies of human kinases, and all three structures provide new insights into kinase regulation and the design of selective inhibitors.

PubMed: 12467573
DOI: 10.1016/S0969-2126(02)00907-3

実験手法

X-RAY DIFFRACTION (2.3 Å)