1OMW

Crystal Structure of the complex between G Protein-Coupled Receptor Kinase 2 and Heterotrimeric G Protein beta 1 and gamma 2 subunits

1OMW の概要

• エントリーDOI: 10.2210/pdb1omw/pdb
• 分子名称: G-protein coupled receptor kinase 2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) beta subunit 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) gamma-2 subunit, ... (4 entities in total)
• 機能のキーワード: wd-40 repeat, transferase
• 由来する生物種: Bos taurus (cattle); 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: 125573.51

構造登録者

Lodowski, D.T.,Pitcher, J.A.,Capel, W.D.,Lefkowitz, R.J.,Tesmer, J.J.G. (登録日: 2003-02-26, 公開日: 2003-06-03, 最終更新日: 2023-08-16)

主引用文献

Lodowski, D.T.,Pitcher, J.A.,Capel, W.D.,Lefkowitz, R.J.,Tesmer, J.J.G.
Keeping G proteins at Bay: A Complex Between G Protein-Coupled Receptor Kinase 2 and G-Beta-Gamma
Science, 300:1256-1262, 2003

PubMed Abstract: The phosphorylation of heptahelical receptors by heterotrimeric guanine nucleotide-binding protein (G protein)-coupled receptor kinases (GRKs) is a universal regulatory mechanism that leads to desensitization of G protein signaling and to the activation of alternative signaling pathways. We determined the crystallographic structure of bovine GRK2 in complex with G protein beta1gamma2 subunits. Our results show how the three domains of GRK2-the RGS (regulator of G protein signaling) homology, protein kinase, and pleckstrin homology domains-integrate their respective activities and recruit the enzyme to the cell membrane in an orientation that not only facilitates receptor phosphorylation, but also allows for the simultaneous inhibition of signaling by Galpha and Gbetagamma subunits.

PubMed: 12764189
DOI: 10.1126/science.1082348

実験手法

X-RAY DIFFRACTION (2.5 Å)