Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T31721 | Target Info | |||
| Target Name | Excitatory amino acid transporter 3 (SLC1A1) | ||||
| Synonyms | Solute carrier family 1 member 1; Sodium-dependent glutamate/aspartate transporter 3; Neuronal and epithelial glutamate transporter; Excitatory amino-acid carrier 1; EAAT3; EAAC1 | ||||
| Target Type | Literature-reported Target | ||||
| Gene Name | SLC1A1 | ||||
| Biochemical Class | Dicarboxylate/amino acid:cation symporter | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: L-aspartic acid | Ligand Info | |||||
| Structure Description | hEAAT3-OFS-Asp | PDB:6X2Z | ||||
| Method | Electron microscopy | Resolution | 3.03 Å | Mutation | Yes | [1] |
| PDB Sequence |
KNNWVLLSTV
25 AAVVLGITTG35 VLVREHSNLS45 TLEKFYFAFP55 GEILMRMLKL65 IILPLIISSM 75 ITGVAALDSN85 VSGKIGLRAV95 VYYFCTTLIA105 VILGIVLVVS115 IKPGVTQKVG 125 STVDAMLDLI146 RNMFPENLVQ156 ACFQQYKTKR166 EEEYKIVGMY206 SDGINVLGLI 216 VFCLVFGLVI226 GKMGEKGQIL236 VDFFNALSDA246 TMKIVQIIMC256 YMPLGILFLI 266 AGKIIEVEDW276 EIFRKLGLYM286 ATVLTGLAIH296 SIVILPLIYF306 IVVRKNPFRF 316 AMGMAQALLT326 ALMISSSSAT336 LPVTFRCAEE346 NNQVDKRITR356 FVLPVGATIN 366 MDGTALYEAV376 AAVFIAQLND386 LDLGIGQIIT396 ISITATSASI406 GAAGVPQAGL 416 VTMVIVLSAV426 GLPAEDVTLI436 IAVDWLLDRF446 RTMVNVLGDA456 FGTGIVEKLS 466 KKELEQMDV
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: (-)-3-Hydroxy-4,5,6,6a-tetrahydro-3aH-pyrrolo[3,4-d]isoxazole-6-carboxylic acid | Ligand Info | |||||
| Structure Description | Structure of human excitatory amino acid transporter 3 (EAAT3) in complex with HIP-B | PDB:7NSG | ||||
| Method | Electron microscopy | Resolution | 3.34 Å | Mutation | Yes | [2] |
| PDB Sequence |
EWKRFLKNNW
19 VLLSTVAAVV29 LGITTGVLVR39 EHRNLSTLEK49 FYFAFPGEIL59 MRMLKLIILP 69 LIISSMITGV79 AALDSNVSGK89 IGVRAVVYYF99 CTTLIAVILG109 IVLVVSIKPG 119 VTQVSTVDAM142 LDLIRNMFPE152 NLVQACFQQY162 KTKREEVKPK196 TKEYKIVGMY 206 SDGINVLGLI216 VFCLVFGLVI226 GKMGEKGQIL236 VDFFNALSDA246 TMKIVQIIMC 256 YMPLGILFLI266 AGKIIEVEDW276 EIFRKLGLYM286 ATVLTGLAIH296 SIVILPLIYF 306 IVVRKNPFRF316 AMGMAQALLT326 ALMISSSSAT336 LPVTFRCAEE346 NNQVDKRITR 356 FVLPVGATIN366 MDGTALYEAV376 AAVFIAQLND386 LDLGIGQIIT396 ISITATSASI 406 GAAGVPQAGL416 VTMVIVLSAV426 GLPAEDVTLI436 IAVDWLLDRF446 RTMVNVLGDA 456 FGTGIVEKLS466 KKELEQMDVS476
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| Ligand Name: (3aS,6S,6aS)-3-Oxohexahydro-2H-pyrrolo[3,4-d][1,2]oxazole-6-carboxylic acid | Ligand Info | |||||
| Structure Description | Structure of human excitatory amino acid transporter 3 (EAAT3) in complex with HIP-B | PDB:7NSG | ||||
| Method | Electron microscopy | Resolution | 3.34 Å | Mutation | Yes | [2] |
| PDB Sequence |
EWKRFLKNNW
19 VLLSTVAAVV29 LGITTGVLVR39 EHRNLSTLEK49 FYFAFPGEIL59 MRMLKLIILP 69 LIISSMITGV79 AALDSNVSGK89 IGVRAVVYYF99 CTTLIAVILG109 IVLVVSIKPG 119 VTQVSTVDAM142 LDLIRNMFPE152 NLVQACFQQY162 KTKREEVKPK196 TKEYKIVGMY 206 SDGINVLGLI216 VFCLVFGLVI226 GKMGEKGQIL236 VDFFNALSDA246 TMKIVQIIMC 256 YMPLGILFLI266 AGKIIEVEDW276 EIFRKLGLYM286 ATVLTGLAIH296 SIVILPLIYF 306 IVVRKNPFRF316 AMGMAQALLT326 ALMISSSSAT336 LPVTFRCAEE346 NNQVDKRITR 356 FVLPVGATIN366 MDGTALYEAV376 AAVFIAQLND386 LDLGIGQIIT396 ISITATSASI 406 GAAGVPQAGL416 VTMVIVLSAV426 GLPAEDVTLI436 IAVDWLLDRF446 RTMVNVLGDA 456 FGTGIVEKLS466 KKELEQMDVS476
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .UR5 or .UR52 or .UR53 or :3UR5;style chemicals stick;color identity;select .A:331 or .A:332 or .A:333 or .A:367 or .A:370 or .A:411 or .A:412 or .A:415 or .A:444 or .A:447 or .A:448 or .A:451; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: Cholesterol hemisuccinate | Ligand Info | |||||
| Structure Description | Structure of human excitatory amino acid transporter 3 (EAAT3) in complex with TFB-TBOA | PDB:6S3Q | ||||
| Method | Electron microscopy | Resolution | 3.34 Å | Mutation | Yes | [3] |
| PDB Sequence |
EWKRFLKNNW
19 VLLSTVAAVV29 LGITTGVLVR39 EHRNLSTLEK49 FYFAFPGEIL59 MRMLKLIILP 69 LIISSMITGV79 AALDSNVSGK89 IGVRAVVYYF99 CTTLIAVILG109 IVLVVSIKPG 119 VTQVSTVDAM142 LDLIRNMFPE152 NLVQACFQQY162 KTKREEVKPK196 TKEYKIVGMY 206 SDGINVLGLI216 VFCLVFGLVI226 GKMGEKGQIL236 VDFFNALSDA246 TMKIVQIIMC 256 YMPLGILFLI266 AGKIIEVEDW276 EIFRKLGLYM286 ATVLTGLAIH296 SIVILPLIYF 306 IVVRKNPFRF316 AMGMAQALLT326 ALMISSSSAT336 LPVTFRCAEE346 NNQVDKRITR 356 FVLPVGATIN366 MDGTALYEAV376 AAVFIAQLND386 LDLGIGQIIT396 ISITATSASI 406 GAAGVPQAGL416 VTMVIVLSAV426 GLPAEDVTLI436 IAVDWLLDRF446 RTMVNVLGDA 456 FGTGIVEKLS466 KKELEQMDVS476
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .Y01 or .Y012 or .Y013 or :3Y01;style chemicals stick;color identity;select .A:89 or .A:92 or .A:93 or .A:96 or .A:97 or .A:100 or .A:104 or .A:300 or .A:303 or .A:304 or .A:307 or .A:308 or .A:465; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Tfb-tboa | Ligand Info | |||||
| Structure Description | Structure of human excitatory amino acid transporter 3 (EAAT3) in complex with TFB-TBOA | PDB:6S3Q | ||||
| Method | Electron microscopy | Resolution | 3.34 Å | Mutation | Yes | [3] |
| PDB Sequence |
EWKRFLKNNW
19 VLLSTVAAVV29 LGITTGVLVR39 EHRNLSTLEK49 FYFAFPGEIL59 MRMLKLIILP 69 LIISSMITGV79 AALDSNVSGK89 IGVRAVVYYF99 CTTLIAVILG109 IVLVVSIKPG 119 VTQVSTVDAM142 LDLIRNMFPE152 NLVQACFQQY162 KTKREEVKPK196 TKEYKIVGMY 206 SDGINVLGLI216 VFCLVFGLVI226 GKMGEKGQIL236 VDFFNALSDA246 TMKIVQIIMC 256 YMPLGILFLI266 AGKIIEVEDW276 EIFRKLGLYM286 ATVLTGLAIH296 SIVILPLIYF 306 IVVRKNPFRF316 AMGMAQALLT326 ALMISSSSAT336 LPVTFRCAEE346 NNQVDKRITR 356 FVLPVGATIN366 MDGTALYEAV376 AAVFIAQLND386 LDLGIGQIIT396 ISITATSASI 406 GAAGVPQAGL416 VTMVIVLSAV426 GLPAEDVTLI436 IAVDWLLDRF446 RTMVNVLGDA 456 FGTGIVEKLS466 KKELEQMDVS476
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .7O9 or .7O92 or .7O93 or :37O9;style chemicals stick;color identity;select .A:70 or .A:71 or .A:74 or .A:75 or .A:248 or .A:331 or .A:332 or .A:333 or .A:334 or .A:367 or .A:370 or .A:404 or .A:407 or .A:408 or .A:409 or .A:410 or .A:411 or .A:412 or .A:414 or .A:415 or .A:418 or .A:421 or .A:444 or .A:447 or .A:448 or .A:451; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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LEU70
3.660
ILE71
3.579
SER74
3.434
MET75
4.166
MET248
3.842
SER331
3.642
SER332
3.418
SER333
2.620
SER334
4.583
MET367
3.932
THR370
2.729
ALA404
3.234
GLY407
3.206
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Cryo-EM structures of excitatory amino acid transporter 3 visualize coupled substrate, sodium, and proton binding and transport. Sci Adv. 2021 Mar 3;7(10):eabf5814. | ||||
| REF 2 | Structure of human excitatory amino acid transporter 3 (EAAT3) in complex with HIP-B | ||||
| REF 3 | Structure of human excitatory amino acid transporter 3 (EAAT3) | ||||
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