Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T95438 | Target Info | |||
| Target Name | Excitatory amino acid transporter 2 (SLC1A2) | ||||
| Synonyms | Solute carrier family 1 member 2; Sodium-dependent glutamate/aspartate transporter 2; Glutamate/aspartatetransporter II; Glutamate/aspartate transporter II; GLT1; EAAT2 | ||||
| Target Type | Literature-reported Target | ||||
| Gene Name | SLC1A2 | ||||
| Biochemical Class | Dicarboxylate/amino acid:cation symporter | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: WAY-213613 | Ligand Info | |||||
| Structure Description | Structure of human excitatory amino acid transporter 2 (EAAT2) in complex with WAY-213613 | PDB:7XR6 | ||||
| Method | Electron microscopy | Resolution | 3.40 Å | Mutation | No | [1] |
| PDB Sequence |
RLCDKLGKNL
45 LLTLTVFGVI55 LGAVCGGLLR65 LASPIHPDVV75 MLIAFPGDIL85 MRMLKMLILP 95 LIISSLITGL105 SGLDAKASGR115 LGTRAMVYYM125 STTIIAAVLG135 VILVLAIHPG 145 NPKVSSLDAF168 LDLIRNLFPE178 NLVQACFQQI188 QTVTKVIKKG233 LEFKDGMNVL 243 GLIGFFIAFG253 IAMGKMGDQA263 KLMVDFFNIL273 NEIVMKLVIM283 IMWYSPLGIA 293 CLICGKIIAI303 KDLEVVARQL313 GMYMVTVIIG323 LIIHGGIFLP333 LIYFVVTRKN 343 PFSFFAGIFQ353 AWITALGTAS363 SAGTLPVTFR373 CLEENLGIDK383 RVTRFVLPVG 393 ATINMDGTAL403 YEAVAAIFIA413 QMNGVVLDGG423 QIVTVSLTAT433 LASVGAASIP 443 SAGLVTMLLI453 LTAVGLPTED463 ISLLVAVDWL473 LDRMRTSVNV483 VGDSFGAGIV 493 YHLSKSELDT503 IDSQ
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ALA362
3.815
SER363
3.629
SER364
2.797
ALA365
4.810
MET398
3.929
THR401
3.230
TYR404
3.581
GLU405
4.677
ALA439
3.663
ALA440
3.750
GLY446
3.122
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Cholesterol | Ligand Info | |||||
| Structure Description | Inward-facing structure of human EAAT2 in the WAY213613-bound state | PDB:7VR7 | ||||
| Method | Electron microscopy | Resolution | 3.49 Å | Mutation | No | [2] |
| PDB Sequence |
NLLLTLTVFG
53 VILGAVCGGL63 LRLASPIHPD73 VVMLIAFPGD83 ILMRMLKMLI93 LPLIISSLIT 103 GLSGLDGRLG117 TRAMVYYMST127 TIIAAVLGVI137 LVLAIHPGNP147 SSLDAFLDLI 172 RNLFPENLVQ182 ACFQQIQTVT192 KIKKGLEFKD238 GMNVLGLIGF248 FIAFGIAMGK 258 MGDQAKLMVD268 FFNILNEIVM278 KLVIMIMWYS288 PLGIACLICG298 KIIAIKDLEV 308 VARQLGMYMV318 TVIIGLIIHG328 GIFLPLIYFV338 VTRKNPFSFF348 AGIFQAWITA 358 LGTASSAGTL368 PVTFRCLEEN378 LGIDKRVTRF388 VLPVGATINM398 DGTALYEAVA 408 AIFIAQMNGV418 VLDGGQIVTV428 SLTATLASVG438 AASIPSAGLV448 TMLLILTAVG 458 LPTEDISLLV468 AVDWLLDRMR478 TSVNVVGDSF488 GAGIVYHLSK498 SE |
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Cholesterol hemisuccinate | Ligand Info | |||||
| Structure Description | Structure of human excitatory amino acid transporter 2 (EAAT2) in complex with glutamate | PDB:7XR4 | ||||
| Method | Electron microscopy | Resolution | 3.40 Å | Mutation | No | [1] |
| PDB Sequence |
LCDKLGKNLL
46 LTLTVFGVIL56 GAVCGGLLRL66 ASPIHPDVVM76 LIAFPGDILM86 RMLKMLILPL 96 IISSLITGLS106 GLDAKASGRL116 GTRAMVYYMS126 TTIIAAVLGV136 ILVLAIHPGN 146 PKVSSLDAFL169 DLIRNLFPEN179 LVQACFQQIQ189 TVTKKVVIKK232 GLEFKDGMNV 242 LGLIGFFIAF252 GIAMGKMGDQ262 AKLMVDFFNI272 LNEIVMKLVI282 MIMWYSPLGI 292 ACLICGKIIA302 IKDLEVVARQ312 LGMYMVTVII322 GLIIHGGIFL332 PLIYFVVTRK 342 NPFSFFAGIF352 QAWITALGTA362 SSAGTLPVTF372 RCLEENLGID382 KRVTRFVLPV 392 GATINMDGTA402 LYEAVAAIFI412 AQMNGVVLDG422 GQIVTVSLTA432 TLASVGAASI 442 PSAGLVTMLL452 ILTAVGLPTE462 DISLLVAVDW472 LLDRMRTSVN482 VVGDSFGAGI 492 VYHLSKSELD502 TIDSQ
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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:115 or .A:118 or .A:119 or .A:122 or .A:123 or .A:126 or .A:130 or .A:331 or .A:334 or .A:335 or .A:339 or .A:492 or .A:496; color #00ffc7; 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: Lauryl glucoside | Ligand Info | |||||
| Structure Description | Structure of human excitatory amino acid transporter 2 (EAAT2) in complex with WAY-213613 | PDB:7XR6 | ||||
| Method | Electron microscopy | Resolution | 3.40 Å | Mutation | No | [1] |
| PDB Sequence |
RLCDKLGKNL
45 LLTLTVFGVI55 LGAVCGGLLR65 LASPIHPDVV75 MLIAFPGDIL85 MRMLKMLILP 95 LIISSLITGL105 SGLDAKASGR115 LGTRAMVYYM125 STTIIAAVLG135 VILVLAIHPG 145 NPKVSSLDAF168 LDLIRNLFPE178 NLVQACFQQI188 QTVTKVIKKG233 LEFKDGMNVL 243 GLIGFFIAFG253 IAMGKMGDQA263 KLMVDFFNIL273 NEIVMKLVIM283 IMWYSPLGIA 293 CLICGKIIAI303 KDLEVVARQL313 GMYMVTVIIG323 LIIHGGIFLP333 LIYFVVTRKN 343 PFSFFAGIFQ353 AWITALGTAS363 SAGTLPVTFR373 CLEENLGIDK383 RVTRFVLPVG 393 ATINMDGTAL403 YEAVAAIFIA413 QMNGVVLDGG423 QIVTVSLTAT433 LASVGAASIP 443 SAGLVTMLLI453 LTAVGLPTED463 ISLLVAVDWL473 LDRMRTSVNV483 VGDSFGAGIV 493 YHLSKSELDT503 IDSQ
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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 .XKJ or .XKJ2 or .XKJ3 or :3XKJ;style chemicals stick;color identity;select .A:46 or .A:47 or .A:50 or .A:51 or .A:54 or .A:55 or .A:285 or .A:288 or .A:444 or .A:468 or .A:469 or .A:471 or .A:472 or .A:475 or .A:478; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: (3beta,14beta,17beta,25R)-3-[4-methoxy-3-(methoxymethyl)butoxy]spirost-5-en | Ligand Info | |||||
| Structure Description | Inward-facing structure of human EAAT2 in the WAY213613-bound state | PDB:7VR7 | ||||
| Method | Electron microscopy | Resolution | 3.49 Å | Mutation | No | [2] |
| PDB Sequence |
NLLLTLTVFG
53 VILGAVCGGL63 LRLASPIHPD73 VVMLIAFPGD83 ILMRMLKMLI93 LPLIISSLIT 103 GLSGLDGRLG117 TRAMVYYMST127 TIIAAVLGVI137 LVLAIHPGNP147 SSLDAFLDLI 172 RNLFPENLVQ182 ACFQQIQTVT192 KIKKGLEFKD238 GMNVLGLIGF248 FIAFGIAMGK 258 MGDQAKLMVD268 FFNILNEIVM278 KLVIMIMWYS288 PLGIACLICG298 KIIAIKDLEV 308 VARQLGMYMV318 TVIIGLIIHG328 GIFLPLIYFV338 VTRKNPFSFF348 AGIFQAWITA 358 LGTASSAGTL368 PVTFRCLEEN378 LGIDKRVTRF388 VLPVGATINM398 DGTALYEAVA 408 AIFIAQMNGV418 VLDGGQIVTV428 SLTATLASVG438 AASIPSAGLV448 TMLLILTAVG 458 LPTEDISLLV468 AVDWLLDRMR478 TSVNVVGDSF488 GAGIVYHLSK498 SE |
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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 .9Z9 or .9Z92 or .9Z93 or :39Z9;style chemicals stick;color identity;select .A:93 or .A:96 or .A:97 or .A:100 or .A:101 or .A:104 or .A:105 or .A:108 or .A:109 or .A:121 or .A:246 or .A:388 or .A:392 or .A:396 or .A:434 or .A:435 or .A:437 or .A:438 or .A:441 or .A:442 or .A:448 or .A:449 or .A:452; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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ILE93
4.929
LEU96
3.730
ILE97
3.898
SER100
3.526
LEU101
3.485
GLY104
3.815
LEU105
4.066
LEU108
3.187
ASP109
3.623
MET121
3.868
ILE246
4.252
PHE388
4.164
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structural basis of ligand binding modes of human EAAT2. Nat Commun. 2022 Jun 9;13(1):3329. | ||||
| REF 2 | Structural insights into inhibitory mechanism of human excitatory amino acid transporter EAAT2. Nat Commun. 2022 Aug 11;13(1):4714. | ||||
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