3EB3

Voltage-dependent K+ channel beta subunit (W121A) in complex with cortisone

3EB3 の概要

• エントリーDOI: 10.2210/pdb3eb3/pdb
• 関連するPDBエントリー: 1exb 1qrq 3EAU 3EB4
• 分子名称: Voltage-gated potassium channel subunit beta-2, NADPH DIHYDRO-NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE, 17,21-DIHYDROXYPREGNA-1,4-DIENE-3,11,20-TRIONE, ... (4 entities in total)
• 機能のキーワード: kvbeta, cortisone, interface, cytoplasm, ion transport, ionic channel, nadp, phosphoprotein, potassium, potassium transport, transport, voltage-gated channel, transport protein, oxidoreductase
• 由来する生物種: Rattus norvegicus (brown rat,rat,rats)
• 細胞内の位置: Cytoplasm (Potential): P62483
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 37560.91

構造登録者

Pan, Y.,Weng, J.,Kabaleeswaran, V.,Li, H.,Cao, Y.,Bhosle, R.C.,Zhou, M. (登録日: 2008-08-26, 公開日: 2008-09-23, 最終更新日: 2023-08-30)

主引用文献

Pan, Y.,Weng, J.,Kabaleeswaran, V.,Li, H.,Cao, Y.,Bhosle, R.C.,Zhou, M.
Cortisone dissociates the Shaker family K+ channels from their beta subunits.
Nat.Chem.Biol., 4:708-714, 2008

PubMed Abstract: The Shaker family voltage-dependent potassium channels (Kv1) are expressed in a wide variety of cells and are essential for cellular excitability. In humans, loss-of-function mutations of Kv1 channels lead to hyperexcitability and are directly linked to episodic ataxia and atrial fibrillation. All Kv1 channels assemble with beta subunits (Kv betas), and certain Kv betas, for example Kv beta 1, have an N-terminal segment that closes the channel by the N-type inactivation mechanism. In principle, dissociation of Kv beta 1, although never reported, should eliminate inactivation and thus potentiate Kv1 current. We found that cortisone increases rat Kv1 channel activity by binding to Kv beta 1. A crystal structure of the Kv beta-cortisone complex was solved to 1.82-A resolution and revealed novel cortisone binding sites. Further studies demonstrated that cortisone promotes dissociation of Kv beta. The new mode of channel modulation may be explored by native or synthetic ligands to fine-tune cellular excitability.

PubMed: 18806782
DOI: 10.1038/nchembio.114

実験手法

X-RAY DIFFRACTION (2 Å)