STRUCTURE OF GLUA2 LIGAND-BINDING DOMAIN (S1S2J-L504Y-N775S) IN COMPLEX WITH GLUTAMATE AND TDPAM01 AT 1.6 A RESOLUTION.

6,6'-(Ethane-1,2-diyl)bis(4-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide)

Crystal Structures of Potent Dimeric Positive Allosteric Modulators at the Ligand-Binding Domain of the GluA2 Receptor.

NATIVE GLUA2 IS A MEMBRANE PROTEIN. THE CRYSTALLIZED PROTEIN IS A L540Y-N775S-MUTANT OF THE GLUA2 LIGAND-BINDING DOMAIN. TRANSMEMBRANE REGIONS ARE REPLACED WITH A GLY-THR LINKER (RESIDUES 118-119) AND GLY1-ALA2 IS A CLONING REMNANT. THE SEQUENCE MATCHES DISCONTINUOUSLY WITH REFERENCE DATABASE (413-527, 653-797).

GluR-2,AMPA-selective glutamate receptor 2,GluR-B,GluR-K2,Glutamate receptor ionotropic,AMPA 2,GluA2,GluR-2,AMPA-selective glutamate receptor 2,GluR-B,GluR-K2,Glutamate receptor ionotropic,AMPA 2,GluA2

15% PEG4000, 0.1 M zinc acetate, 0.1 M sodium acetate

Glutamate receptor 2,Glutamate receptor 2

ampa receptor, gluA2, ligand-binding domain, glua2-S1S2J-L504Y-N775S, membrane protein, signaling protein, positive allosteric modulator

(chain A and (resid 1 through 15 or resid 17 or resid 20 through 23 or resid 25 through 42 or resid 44 through 76 or resid 78 through 106 or resid 109 through 115 or resid 117 through 163 or resid 165 through 175 or resid 177 through 183 or resid 185 through 195 or resid 197 or resid 200 through 208 or resid 211 through 216 or resid 218 through 221 or resid 223 through 231 or resid 233 through 239 or resid 241 through 245 or resid 247 through 262))

(chain B and (resid 1 through 15 or resid 17 or resid 20 through 23 or resid 25 through 42 or resid 44 through 76 or resid 78 through 106 or resid 109 through 115 or resid 117 through 163 or resid 165 through 175 or resid 177 through 183 or resid 185 through 195 or resid 197 or resid 200 through 208 or resid 211 through 216 or resid 218 through 221 or resid 223 through 231 or resid 233 through 239 or resid 241 through 245 or resid 247 through 262))

(chain C and (resid 1 through 15 or resid 17 or resid 20 through 23 or resid 25 through 42 or resid 44 through 76 or resid 78 through 106 or resid 109 through 115 or resid 117 through 163 or resid 165 through 175 or resid 177 through 183 or resid 185 through 195 or resid 197 or resid 200 through 208 or resid 211 through 216 or resid 218 through 221 or resid 223 through 231 or resid 233 through 239 or resid 241 through 245 or resid 247 through 262))