1mqd

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PDB ID 1mqd

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, resolution 1.46Å
Ligands: , ,
Related: 1FTJ, 1FTK, 1FTL, 1FTM, 1FTO, 1FW0, 1GR2, 1LBB, 1LBC, 1LB8, 1LB9, 1M5B, 1M5C, 1M5D, 1M5E, 1M5F, 1MM6, 1MM7


Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



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.


Overview

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.

About this Structure

1MQD is a Single protein structure of sequence from Rattus norvegicus. Full crystallographic information is available from OCA.

Reference

GluR2 ligand-binding core complexes: importance of the isoxazolol moiety and 5-substituent for the binding mode of AMPA-type agonists., Kasper C, Lunn ML, Liljefors T, Gouaux E, Egebjerg J, Kastrup JS, FEBS Lett. 2002 Nov 6;531(2):173-8. PMID:12417307

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