4U22

GluA2flip sLBD complexed with FW and (R,R)-2b crystal form D

4U22 の概要

• エントリーDOI: 10.2210/pdb4u22/pdb
• 分子名称: Glutamate receptor 2, 2-AMINO-3-(5-FLUORO-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YL)-PROPIONIC ACID, N,N'-[biphenyl-4,4'-diyldi(2R)propane-2,1-diyl]dipropane-2-sulfonamide, ... (4 entities in total)
• 機能のキーワード: ampa receptor, transport protein, membrane protein
• 由来する生物種: Rattus norvegicus (Rat); 詳細
• 細胞内の位置: Cell membrane; Multi-pass membrane protein: P19491
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 29891.51

構造登録者

Chen, L.,Gouaux, E. (登録日: 2014-07-16, 公開日: 2014-08-20, 最終更新日: 2024-11-13)

主引用文献

Durr, K.L.,Chen, L.,Stein, R.A.,De Zorzi, R.,Folea, I.M.,Walz, T.,Mchaourab, H.S.,Gouaux, E.
Structure and Dynamics of AMPA Receptor GluA2 in Resting, Pre-Open, and Desensitized States.
Cell, 158:778-792, 2014

PubMed Abstract: Ionotropic glutamate receptors (iGluRs) mediate the majority of fast excitatory signaling in the nervous system. Despite the profound importance of iGluRs to neurotransmission, little is known about the structures and dynamics of intact receptors in distinct functional states. Here, we elucidate the structures of the intact GluA2 AMPA receptor in an apo resting/closed state, in an activated/pre-open state bound with partial agonists and a positive allosteric modulator, and in a desensitized/closed state in complex with fluorowilliardiine. To probe the conformational properties of these states, we carried out double electron-electron resonance experiments on cysteine mutants and cryoelectron microscopy studies. We show how agonist binding modulates the conformation of the ligand-binding domain "layer" of the intact receptors and how, upon desensitization, the receptor undergoes large conformational rearrangements of the amino-terminal and ligand-binding domains. We define mechanistic principles by which to understand antagonism, activation, and desensitization in AMPA iGluRs.

PubMed: 25109876
DOI: 10.1016/j.cell.2014.07.023

実験手法

X-RAY DIFFRACTION (1.4409 Å)