1MQD

X-ray structure of the GluR2 ligand-binding core (S1S2J) in complex with (S)-Des-Me-AMPA at 1.46 A resolution. Crystallization in the presence of lithium sulfate.

1MQD の概要

• エントリーDOI: 10.2210/pdb1mqd/pdb
• 関連するPDBエントリー: 1FTJ 1FTK 1FTL 1FTM 1FTO 1FW0 1GR2 1LB8 1LB9 1LBB 1LBC 1M5B 1M5C 1M5D 1M5E 1M5F 1MM6 1MM7
• 分子名称: Glutamate receptor subunit 2, SULFATE ION, (S)-2-AMINO-3-(3-HYDROXY-ISOXAZOL-4-YL)PROPIONIC ACID, ... (5 entities in total)
• 機能のキーワード: ionotropic glutamate receptor glur2, ligand-binding core, agonist complex., membrane protein
• 由来する生物種: Rattus norvegicus (Norway 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: 4
• 化学式量合計: 117379.05

構造登録者

Kasper, C.,Lunn, M.-L.,Liljefors, T.,Gouaux, E.,Egebjerg, J.,Kastrup, J.S. (登録日: 2002-09-16, 公開日: 2003-07-01, 最終更新日: 2024-10-23)

主引用文献

Kasper, C.,Lunn, M.L.,Liljefors, T.,Gouaux, E.,Egebjerg, J.,Kastrup, J.S.
GluR2 ligand-binding core complexes: Importance of the isoxazolol moiety and 5-substituent for the binding mode of AMPA-type agonists.
FEBS Lett., 531:173-178, 2002

PubMed Abstract: X-ray structures of the GluR2 ligand-binding core in complex with (S)-Des-Me-AMPA and in the presence and absence of zinc ions have been determined. (S)-Des-Me-AMPA, which is devoid of a substituent in the 5-position of the isoxazolol ring, only has limited interactions with the partly hydrophobic pocket of the ligand-binding site, and adopts an AMPA-like binding mode. The structures, in comparison with other agonist complex structures, disclose the relative importance of the isoxazolol ring and of the substituent in the 5-position for the mode of binding. A relationship appears to exist between the extent of interaction of the ligand with the hydrophobic pocket and the affinity of the ligand.

PubMed: 12417307
DOI: 10.1016/S0014-5793(02)03496-8

実験手法

X-RAY DIFFRACTION (1.46 Å)