Crystal structure of 1-((2-fluoro-4-(3-(trifluoromethyl)-4,5,6,7- tetrahydro-1H-indazol-1-yl)phenyl)methyl)-2-pyrrolidinone in complex with the ligand binding domain of the Rat GluA2 receptor and glutamate at 2.2A resolution.

Integration of Lead Optimization with Crystallography for a Membrane-Bound Ion Channel Target: Discovery of a New Class of Ampa Receptor Positive Allosteric Modulators.

LIGAND BINDING DOMAIN, RESIDUES 413-527,653-796

GLUR-2, AMPA-SELECTIVE GLUTAMATE RECEPTOR 2, GLUR-B, GLUR-K2, GLUTAMATE RECEPTOR IONOTROPIC\,AMPA 2, GLUA2

GANKTVVVTTILESPYVMMKKNHEMLEGNERYEGYCVDLAAEIAKHCGFKYKLTIVGDGKYGARDADTKIWNGMVGELVY
GKADIAIAPLTITLVREEVIDFSKPFMSLGISIMIKKGTPIESAEDLSKQTEIAYGTLDSGSTKEFFRRSKIAVFDKMWT
YMRSAEPSVFVRTTAEGVARVRKSKGKYAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSSLGNAVNLAVLK
LSEQGLLDKLKNKWWYDKGECGS

X-RAY STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J) INCOMPLEX WITH BR-HIBO AT 1.65 A RESOLUTION

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND-BINDING CORE ( S1S2J)MUTANT L650T IN COMPLEX WITH QUISQUALATE

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J)IN COMPLEX WITH BROMO-WILLARDIINE AT 1.8 ANGSTROMSRESOLUTION

CRYSTAL STRUCTURE OF THE NON-DESENSITIZING GLUR2 LIGANDBINDING CORE MUTANT (S1S2J-L483Y) IN COMPLEX WITH AMPA AT2.3 RESOLUTION

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND-BINDING CORE ( S1S2J)L650T MUTANT IN COMPLEX WITH AMPA (AMMONIUM SULFATECRYSTAL FORM)

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J)IN COMPLEX WITH QUISQUALATE IN A ZINC CRYSTAL FORM AT 1.65ANGSTROMS RESOLUTION

X-RAY STRUCTURE OF THE GLUR2 LIGAND-BINDING CORE ( S1S2J) INCOMPLEX WITH (S)-ATPA AT 1.9 A RESOLUTION . CRYSTALLIZATIONWITHOUT ZINC IONS.

X-RAY STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J-Y702F) IN COMPLEX WITH BR-HIBO AT 1.73 A RESOLUTION

X-RAY STRUCTURE OF THE Y702F MUTANT OF THE GLUR2 LIGAND-BINDING CORE (S1S2J) IN COMPLEX WITH (S)-CPW399 AT 2.1 ARESOLUTION.

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J)L650T MUTANT IN COMPLEX WITH AMPA

X-RAY STRUCTURE OF THE GLUR2 LIGAND-BINDING CORE ( S1S2J) INCOMPLEX WITH (S)-DES-ME-AMPA AT 1.46 A RESOLUTION.CRYSTALLIZATION IN THE PRESENCE OF LITHIUM SULFATE.

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J)IN COMPLEX WITH BROMO-WILLARDIINE (CONTROL FOR THE CRYSTALTITRATION EXPERIMENTS)

CRYSTAL STRUCTURE OF GLUTAMATE RECEPTOR LIGAND-BINDING COREIN COMPLEX WITH IODO-WILLARDIINE IN THE ZN CRYSTAL FORM

MEASUREMENT OF CONFORMATIONAL CHANGES ACCOMPANYINGDESENSITIZATION IN AN IONOTROPIC GLUTAMATE RECEPTOR:STRUCTURE OF G725C MUTANT

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND-BINDING CORE ( S1S2J)WITH THE L483Y AND L650T MUTATIONS AND IN COMPLEX WITH AMPA

MEASUREMENT OF CONFORMATIONAL CHANGES ACCOMPANYINGDESENSITIZATION IN AN IONOTROPIC GLUTAMATE RECEPTOR:STRUCTURE OF S729C MUTANT

X-RAY STRUCTURE OF THE GLUR2 LIGAND-BINDING CORE ( S1S2J) INCOMPLEX WITH THE ANTAGONIST (S)-ATPO AT 2.1 A RESOLUTION.

CRYSTAL STRUCTURE OF 1-((4-(3-(TRIFLUOROMETHYL)-6,7- DIHYDROPYRANO(4,3-C(PYRAZOL-1(4H)-YL)PHENYL)METHYL )-2-PYRROLIDINONE IN COMPLEX WITH THE LIGAND BINDING DOMAIN OF THE RAT GLUA2 RECEPTOR AND GLUTAMATE AT 1 .6A RESOLUTION.

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J)IN COMPLEX WITH FLUORO-WILLARDIINE AT 1.35 ANGSTROMSRESOLUTION

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2I)IN COMPLEX WITH KAINATE AT 1.6 A RESOLUTION

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J-Y450W) MUTANT IN COMPLEX WITH THE PARTIAL AGONIST KAINICACID AT 2.1 A RESOLUTION

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J)IN THE APO STATE AT 2.0 A RESOLUTION

CRYSTAL STRUCTURE OF GLUTAMATE RECEPTOR LIGAND-BINDING COREIN COMPLEX WITH BROMO-WILLARDIINE IN THE ZN CRYSTAL FORM

GLUR2 LIGAND BINDING CORE (S1S2J) MUTANT L650T IN COMPLEXWITH KAINATE

CRYSTAL TITRATION EXPERIMENTS (AMPA CO-CRYSTALS SOAKED IN10 MM BRW)

X-RAY STRUCTURE OF THE GLUR2 LIGAND-BINDING CORE ( S1S2J) INCOMPLEX WITH (S)-CPW399 AT 1.85 A RESOLUTION.

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J)IN COMPLEX WITH GLUTAMATE AT 1.9 RESOLUTION

X-RAY STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J) INCOMPLEX WITH ACPA AT 1.46 A RESOLUTION

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING DOMAIN MUTANT(S1S2J-N754D) IN COMPLEX WITH KAINATE AT 2.1 A RESOLUTION

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J)IN COMPLEX WITH KAINATE AT 2.0 A RESOLUTION

CRYSTAL TITRATION EXPERIMENTS (AMPA CO-CRYSTALS SOAKED IN 1UM BRW)

CRYSTAL TITRATION EXPERIMENTS (AMPA CO-CRYSTALS SOAKED IN10 UM BRW)

CRYSTAL STRUCTURE OF N,N-DIMETHYL-4-(3-( TRIFLUOROMETHYL)-4,5,6,7-TETRAHYDRO-1H-INDAZOL-1-YL )BENZAMIDE IN COMPLEX WITH THE LIGAND BINDING DOMAIN OF THE RAT GLUA2 RECEPTOR AND GLUTAMATE AT 2.2A RESOLUTION.

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J)IN COMPLEX WITH IODO-WILLARDIINE AT 2.15 ANGSTROMSRESOLUTION

X-RAY STRUCTURE OF THE GLUR2 LIGAND-BINDING CORE ( S1S2J) INCOMPLEX WITH (S)-THIO-ATPA AT 2.2 A RESOLUTION.

X-RAY STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J) INCOMPLEX WITH 2-ME-TET-AMPA AT 1.85 A RESOLUTION.

CRYSTAL TITRATION EXPERIMENTS (AMPA CO-CRYSTALS SOAKED IN 1MM BRW)

X-RAY STRUCTURE OF THE GLUR2 LIGAND-BINDING CORE ( S1S2J) INCOMPLEX WITH (S)-DES-ME-AMPA AT 1.97 A RESOLUTION,CRYSTALLIZATION IN THE PRESENCE OF ZINC ACETATE

CRYSTAL STRUCTURE OF 1-(4-(1-PYRROLIDINYLCARBONYL)PHENYL )-3-(TRIFLUOROMETHYL)-4,5,6,7-TETRAHYDRO-1H-INDAZOLE IN COMPLEX WITH THE LIGAND BINDING DOMAIN OF THE RAT GLUA2 RECEPTOR AND GLUTAMATE AT 2.2A RESOLUTION.

CRYSTAL TITRATION EXPERIMENTS (AMPA CO-CRYSTALS SOAKED IN100 NM BRW)

CRYSTAL STRUCTURE OF 1-(4-(2-OXO-2-(1-PYRROLIDINYL) ETHYL)PHENYL)-3-(TRIFLUOROMETHYL)-4,5,6,7-TETRAHYDRO- 1H-INDAZOLE IN COMPLEX WITH THE LIGAND BINDING DOMAIN OF THE RAT GLUA2 RECEPTOR AND GLUTAMATE AT 1.5A RESOLUTION.

X-RAY STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J-Y702F) IN COMPLEX WITH ACPA AT 1.95 A RESOLUTION

X-RAY STRUCTURE OF THE Y702F MUTANT OF THE GLUR2 LIGAND-BINDING CORE (S1S2J) IN COMPLEX WITH KAINATE AT 1.85 ARESOLUTION

CRYSTAL TITRATION EXPERIMENTS (AMPA CO-CRYSTALS SOAKED IN10 NM BRW)

THE STRUCTURE OF A MIXED GLUR2 LIGAND-BINDING CORE DIMER IN COMPLEX WITH (S)-GLUTAMATE AND THE ANTAGONIST (S)-NS1209

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J)IN COMPLEX WITH QUISQUALATE IN A NON ZINC CRYSTAL FORM AT2.15 ANGSTROMS RESOLUTION

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J)IN COMPLEX WITH QUISQUALATE AND CX614.

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J)IN COMPLEX WITH THE ANTAGONIST DNQX AT 1.8 A RESOLUTION

CRYSTAL TITRATION EXPERIMENTS (AMPA CO-CRYSTALS SOAKED IN100 UM BRW)

CRYSTAL STRUCTURE OF THE GLUR2-FLIP LIGAND BINDING DOMAIN

EXPLORING THE GLUR2 LIGAND-BINDING CORE IN COMPLEX WITH THEBICYCLIC AMPA ANALOGUE (S)-4-AHCP

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J)IN COMPLEX WITH AMPA AT 1.7 RESOLUTION

CRYSTAL STRUCTURE OF THE NON-DESENSITIZING GLUR2 LIGANDBINDING CORE MUTANT (S1S2J-L483Y) IN COMPLEX WITHANTAGONIST DNQX AT 2.3 A RESOLUTION

CRYSTAL STRUCTURE OF GLUR2 LIGAND BINDING CORE (S1S2J- N775S)IN COMPLEX WITH CYCLOTHIAZIDE (CTZ) AS WELL AS GLUTAMATEAT 1.8 A RESOLUTION

X-RAY STRUCTURE OF THE GLUR2 LIGAND-BINDING CORE ( S1S2J) INCOMPLEX WITH (S)-ATPA AT 1.85 A RESOLUTION .CRYSTALLIZATION WITH ZINC IONS.

CRYSTAL TITRATION EXPERIMENT (AMPA COMPLEX CONTROL)

STRUCTURE OF A GLUTAMATE RECEPTOR LIGAND BINDING CORE ( GLUR2) COMPLEXED WITH KAINATE

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J)IN COMPLEX WITH FLUORO-WILLARDIINE AND ANIRACETAM

CRYSTAL STRUCTURE OF THE GLUR2 LIGAND BINDING CORE ( S1S2J)IN COMPLEX WITH WILLARDIINE AT 1.65 ANGSTROMS RESOLUTION

ENGINEERED RESIDUE IN CHAIN A, ASN 775 TO SER ENGINEERED RESIDUE IN CHAIN B, ASN 775 TO SER ENGINEERED RESIDUE IN CHAIN C, ASN 775 TO SER

HYDROGENS HAVE BEEN ADDED IN THE RIDING POSITIONS.

TRANSPORT PROTEIN, AMPA RECEPTOR LIGAND-BINDING CORE, ION CHANNEL