3KRX

Human GRK2 in complex with Gbetgamma subunits and balanol (co-crystal)

3KRX の概要

• エントリーDOI: 10.2210/pdb3krx/pdb
• 関連するPDBエントリー: 1BX6 1OMW 3CIK 3KRW
• 分子名称: Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... (6 entities in total)
• 機能のキーワード: rgs homology domain, atp-binding, phosphoprotein, serine/threonine-protein kinase, transferase, transducer, wd repeat, cell membrane, lipoprotein, membrane, methylation, prenylation, protein binding
• 由来する生物種: Homo sapiens (human); 詳細
• 細胞内の位置: Cell membrane; Lipid-anchor; Cytoplasmic side (Potential): P63212
• タンパク質・核酸の鎖数: 3
• 化学式量合計: 125959.85

構造登録者

Tesmer, J.J.G.,Tesmer, V.M. (登録日: 2009-11-19, 公開日: 2010-02-16, 最終更新日: 2023-09-06)

主引用文献

Tesmer, J.J.,Tesmer, V.M.,Lodowski, D.T.,Steinhagen, H.,Huber, J.
Structure of human g protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
J.Med.Chem., 53:1867-1870, 2010

PubMed Abstract: G protein-coupled receptor kinase 2 (GRK2) is a pharmaceutical target for the treatment of cardiovascular diseases such as congestive heart failure, myocardial infarction, and hypertension. To better understand how nanomolar inhibition and selectivity for GRK2 might be achieved, we have determined crystal structures of human GRK2 in complex with Gbetagamma in the presence and absence of the AGC kinase inhibitor balanol. The selectivity of balanol among human GRKs is assessed.

PubMed: 20128603
DOI: 10.1021/jm9017515

実験手法

X-RAY DIFFRACTION (3.1 Å)