4U4G
Structure of GluA2* in complex with competitive antagonist ZK 200775
Summary for 4U4G
| Entry DOI | 10.2210/pdb4u4g/pdb |
| Related | 4U4F |
| Descriptor | Glutamate receptor 2, beta-D-mannopyranose-(1-3)-beta-D-mannopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid (3 entities in total) |
| Functional Keywords | ionotropic glutamate receptor, ampa receptor, competitive antagonist, tetramer, complex, transport protein |
| Biological source | Rattus norvegicus (Rat) |
| Total number of polymer chains | 4 |
| Total formula weight | 373585.02 |
| Authors | Yelshanskaya, M.V.,Li, M.,Sobolevsky, A.I. (deposition date: 2014-07-23, release date: 2014-10-22, Last modification date: 2024-11-06) |
| Primary citation | Yelshanskaya, M.V.,Li, M.,Sobolevsky, A.I. Structure of an agonist-bound ionotropic glutamate receptor. Science, 345:1070-1074, 2014 Cited by PubMed Abstract: Ionotropic glutamate receptors (iGluRs) mediate most excitatory neurotransmission in the central nervous system and function by opening their ion channel in response to binding of agonist glutamate. Here, we report a structure of a homotetrameric rat GluA2 receptor in complex with partial agonist (S)-5-nitrowillardiine. Comparison of this structure with the closed-state structure in complex with competitive antagonist ZK 200775 suggests conformational changes that occur during iGluR gating. Guided by the structures, we engineered disulfide cross-links to probe domain interactions that are important for iGluR gating events. The combination of structural information, kinetic modeling, and biochemical and electrophysiological experiments provides insight into the mechanism of iGluR gating. PubMed: 25103407DOI: 10.1126/science.1256508 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (4.49 Å) |
Structure validation
Download full validation report
