6XSR

Crystal structure of GluA2 AMPA receptor in complex with trans-4-butylcyclohexane carboxylic acid (4-BCCA) inhibitor

6XSR の概要

• エントリーDOI: 10.2210/pdb6xsr/pdb
• 分子名称: Glutamate receptor 2, 2-acetamido-2-deoxy-beta-D-glucopyranose, trans-4-butylcyclohexane-1-carboxylic acid (3 entities in total)
• 機能のキーワード: ampa receptor, ion channels, synapse, bcca, transport protein
• 由来する生物種: Rattus norvegicus (Rat)
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 363862.82

構造登録者

Yelshanskaya, M.V.,Singh, A.K.,Sobolevsky, A.I. (登録日: 2020-07-16, 公開日: 2020-12-30, 最終更新日: 2024-10-30)

主引用文献

Yelshanskaya, M.V.,Singh, A.K.,Narangoda, C.,Williams, R.S.B.,Kurnikova, M.G.,Sobolevsky, A.I.
Structural basis of AMPA receptor inhibition by trans-4-butylcyclohexane carboxylic acid.
Br.J.Pharmacol., 179:3628-3644, 2022

PubMed Abstract: AMPA receptors, which shape excitatory postsynaptic currents and are directly involved in overactivation of synaptic function during seizures, represent a well-accepted target for anti-epileptic drugs. Trans-4-butylcyclohexane carboxylic acid (4-BCCA) has emerged as a new promising anti-epileptic drug in several in vitro and in vivo seizure models, but the mechanism of its action remained unknown. The purpose of this study is to characterize structure and dynamics of 4-BCCA interaction with AMPA receptors.

PubMed: 32959886
DOI: 10.1111/bph.15254

実験手法

X-RAY DIFFRACTION (4.25 Å)