3CGZ

Crystal Structure of Salmonella Sensor Kinase PhoQ catalytic domain

3CGZ の概要

• エントリーDOI: 10.2210/pdb3cgz/pdb
• 関連するPDBエントリー: 3CGY
• 分子名称: Virulence sensor histidine kinase phoQ (2 entities in total)
• 機能のキーワード: alpha-beta sandwich, bergerat fold, atp-binding, growth regulation, inner membrane, kinase, magnesium, membrane, metal-binding, nucleotide-binding, phosphoprotein, transferase, transmembrane, two-component regulatory system, virulence
• 由来する生物種: Salmonella typhimurium
• 細胞内の位置: Cell inner membrane; Multi-pass membrane protein (By similarity): P14147
• タンパク質・核酸の鎖数: 3
• 化学式量合計: 52087.71

構造登録者

Guarnieri, M.T.,Zhang, L.,Shen, J.,Zhao, R. (登録日: 2008-03-06, 公開日: 2008-05-13, 最終更新日: 2023-08-30)

主引用文献

Guarnieri, M.T.,Zhang, L.,Shen, J.,Zhao, R.
The Hsp90 inhibitor radicicol interacts with the ATP-binding pocket of bacterial sensor kinase PhoQ.
J.Mol.Biol., 379:82-93, 2008

PubMed Abstract: Sensor kinases in the bacterial two-component system share a unique ATP-binding Bergerat fold with the GHL (gyrase, Hsp90, and MutL) family of proteins. We demonstrated that selected GHL inhibitors bind to the catalytic domain of sensor kinase PhoQ (PhoQcat) using NMR chemical shift perturbation experiments. Using crystallographic approaches, we show that radicicol (an Hsp90 inhibitor) binds and interacts specifically with residues in the ATP-binding pocket of PhoQ. The interaction between radicicol and PhoQcat demonstrates significant similarities as well as differences compared to AMPPNP (a non-hydrolyzable ATP analog) bound to PhoQcat and radicicol bound to Hsp90. Our results suggest that GHL inhibitors may be useful lead compounds for developing sensor kinase inhibitors.

PubMed: 18440021
DOI: 10.1016/j.jmb.2008.03.036

実験手法

X-RAY DIFFRACTION (1.9 Å)