4DGL

Crystal Structure of the CK2 Tetrameric Holoenzyme

4DGL の概要

• エントリーDOI: 10.2210/pdb4dgl/pdb
• 関連するPDBエントリー: 1JWH
• 分子名称: Casein kinase II subunit beta, Casein kinase II subunit alpha, ZINC ION, ... (4 entities in total)
• 機能のキーワード: protein kinase, transferase
• 由来する生物種: Homo sapiens (human); 詳細
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 130191.17

構造登録者

Lolli, G.,Battistutta, R. (登録日: 2012-01-26, 公開日: 2012-05-02, 最終更新日: 2024-02-28)

主引用文献

Lolli, G.,Pinna, L.A.,Battistutta, R.
Structural determinants of protein kinase CK2 regulation by autoinhibitory polymerization.
Acs Chem.Biol., 7:1158-1163, 2012

PubMed Abstract: CK2 is a Ser/Thr protein kinase essential for cell viability whose activity is anomalously high in several cancers. CK2 is a validated target for cancer therapy with one small molecule inhibitor in phase I clinical trials. This enzyme is not regulated by mechanisms common to other protein kinases, and how its activity is controlled is still unclear. We present a new crystal structure of the CK2 holoenzyme that supports an autoinhibitory mechanism of regulation whereby the β-subunit plays an essential role in the formation of inactive polymeric assemblies. The derived structural model of (down)regulation by aggregation contributes to the interpretation of biochemical and functional data and paves the way for new strategies in the modulation of CK2 activity and for the design of non-ATP-competitive inhibitors targeting the interaction between the α catalytic and the β regulatory subunits.

PubMed: 22506723
DOI: 10.1021/cb300054n

実験手法

X-RAY DIFFRACTION (3 Å)