3BKI
Crystal Structure of the GluR2 ligand binding core (S1S2J) in complex with FQX at 1.87 Angstroms
Summary for 3BKI
| Entry DOI | 10.2210/pdb3bki/pdb |
| Related | 3BKG |
| Descriptor | Glutamate receptor 2, [1,2,5]oxadiazolo[3,4-g]quinoxaline-6,7(5H,8H)-dione 1-oxide (3 entities in total) |
| Functional Keywords | ampa receptor, anqx, quinoxaline-2, 3-diones, alternative splicing, cell junction, endoplasmic reticulum, glycoprotein, ion transport, ionic channel, lipoprotein, membrane, palmitate, phosphoprotein, postsynaptic cell membrane, rna editing, synapse, transmembrane, transport, transport protein |
| Biological source | Rattus norvegicus (rat) More |
| Total number of polymer chains | 4 |
| Total formula weight | 117767.30 |
| Authors | Cruz, L.,Estebanez-Perpina, E.,Pfaff, S.,Borngraeber, S.,Bao, N.,Fletterick, R.,England, P. (deposition date: 2007-12-06, release date: 2008-09-16, Last modification date: 2024-10-30) |
| Primary citation | Cruz, L.A.,Estebanez-Perpina, E.,Pfaff, S.,Borngraeber, S.,Bao, N.,Blethrow, J.,Fletterick, R.J.,England, P.M. 6-Azido-7-nitro-1,4-dihydroquinoxaline-2,3-dione (ANQX) forms an irreversible bond to the active site of the GluR2 AMPA receptor. J.Med.Chem., 51:5856-5860, 2008 Cited by PubMed Abstract: AMPA receptors mediate fast excitatory synaptic transmission and are essential for synaptic plasticity. ANQX, a photoreactive AMPA receptor antagonist, is an important biological probe used to irreversibly inactivate AMPA receptors. Here, using X-ray crystallography and mass spectroscopy, we report that ANQX forms two major products in the presence of the GluR2 AMPAR ligand-binding core (S1S2J). Upon photostimulation, ANQX reacts intramolecularly to form FQX or intermolecularly to form a covalent adduct with Glu705. PubMed: 18754610DOI: 10.1021/jm701517b PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (1.87 Å) |
Structure validation
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