6JUH

structure of CavAb in complex with efonidipine

6JUH の概要

• エントリーDOI: 10.2210/pdb6juh/pdb
• 分子名称: Ion transport protein, 1,2-DIMYRISTOYL-RAC-GLYCERO-3-PHOSPHOCHOLINE, 1,2-DIMYRISTOYL-SN-GLYCERO-3-PHOSPHOCHOLINE, ... (6 entities in total)
• 機能のキーワード: voltage-gated calcium channel block, membrane protein
• 由来する生物種: Arcobacter butzleri RM4018
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 131190.94

構造登録者

Tang, L.,Xu, F. (登録日: 2019-04-13, 公開日: 2019-11-06, 最終更新日: 2023-11-22)

主引用文献

Xu, F.,Xiong, W.,Huang, Y.,Shen, J.,Zhou, D.,Tang, L.
Structural basis for efonidipine block of a voltage-gated Ca2+channel.
Biochem.Biophys.Res.Commun., 513:631-634, 2019

PubMed Abstract: Efonidipine is a dual L-/T- type calcium channel blocker with a slow onset of action and a long lasting effect that exibihits antihypertensive and nephroprotective effects. differs from most other DHPs which can induce reflex tachycardia. Efonidipine reduces blood pressure without decreasing cardiac output and exerts organ-protective effects on the heart and kidney. In order to investigate how efonidipine block voltage-gated Ca channel, we determined the crystal structure of CaAb in complex with efonidipine at atomic resolution using x-ray crystallography. Our results reveal that efonidipine targets the central cavity of a model voltage-gated calcium channel underneath its selectivity filter and occlude the channel in an inactivated state. Binding of efonidipine does not break down the fourfold symmetry of the quaternary structure and its pore structure. Our work provides the structural basis for efonidipine block of a voltage-gated Ca channel at the molecular level.

PubMed: 30981510
DOI: 10.1016/j.bbrc.2019.03.176

実験手法

X-RAY DIFFRACTION (3 Å)