Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T46263 | Target Info | |||
| Target Name | Lymphocyte activation antigen 4F2 (SLC3A2) | ||||
| Synonyms | SLC3A2; Lymphocyte activation antigen 4F2 large subunit; CD98; 4F2hc; 4F2 heavy chain antigen; 4F2 cellsurface antigen heavy chain | ||||
| Target Type | Clinical trial Target | ||||
| Gene Name | SLC3A2 | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Cholesterol | Ligand Info | |||||
| Structure Description | LAT1-CD98hc complex bound to MEM-108 Fab | PDB:6JMQ | ||||
| Method | Electron microscopy | Resolution | 3.31 Å | Mutation | No | [1] |
| PDB Sequence |
RTRWALLLLF
189 WLGWLGMLAG199 AVVIIVRAPR209 CRELPAQKWW219 HTGALYRIGD229 LQAFQGHGAG 239 NLAGLKGRLD249 YLSSLKVKGL259 VLGPIHKNQK269 DDVAQTDLLQ279 IDPNFGSKED 289 FDSLLQSAKK299 KSIRVILDLT309 PNYRGENSWF319 STQVDTVATK329 VKDALEFWLQ 339 AGVDGFQVRD349 IENLKDASSF359 LAEWQNITKG369 FSEDRLLIAG379 TNSSDLQQIL 389 SLLESNKDLL399 LTSSYLSDSG409 STGEHTKSLV419 TQYLNATGNR429 WCSWSLSQAR 439 LLTSFLPAQL449 LRLYQLMLFT459 LPGTPVFSYG469 DEIGLDAAAL479 PGQPMEAPVM 489 LWDESSFPDI499 PGAVSANMTV509 KGQSEDPGSL519 LSLFRRLSDQ529 RSKERSLLHG 539 DFHAFSAGPG549 LFSYIRHWDQ559 NERFLVVLNF569 GDVGLSAGLQ579 ASDLPASASL 589 PAKADLLLST599 QPGREEGSPL609 ELERLKLEPH619 EGLLLRFPYA629 A |
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| Ligand Name: Cholesterol hemisuccinate | Ligand Info | |||||
| Structure Description | Overall structure of the LAT1-4F2hc bound with JX-075 | PDB:7DSK | ||||
| Method | Electron microscopy | Resolution | 2.90 Å | Mutation | No | [2] |
| PDB Sequence |
KFTGLSKEEL
170 LKVAGSPGWV180 RTRWALLLLF190 WLGWLGMLAG200 AVVIIVRAPR210 CRELPAQKWW 220 HTGALYRIGD230 LQAFQGHGAG240 NLAGLKGRLD250 YLSSLKVKGL260 VLGPIHKNQK 270 DDVAQTDLLQ280 IDPNFGSKED290 FDSLLQSAKK300 KSIRVILDLT310 PNYRGENSWF 320 STQVDTVATK330 VKDALEFWLQ340 AGVDGFQVRD350 IENLKDASSF360 LAEWQNITKG 370 FSEDRLLIAG380 TNSSDLQQIL390 SLLESNKDLL400 LTSSYLSDSG410 STGEHTKSLV 420 TQYLNATGNR430 WCSWSLSQAR440 LLTSFLPAQL450 LRLYQLMLFT460 LPGTPVFSYG 470 DEIGLDAAAL480 PGQPMEAPVM490 LWDESSFPDI500 PGAVSANMTV510 KGQSEDPGSL 520 LSLFRRLSDQ530 RSKERSLLHG540 DFHAFSAGPG550 LFSYIRHWDQ560 NERFLVVLNF 570 GDVGLSAGLQ580 ASDLPASASL590 PAKADLLLST600 QPGREEGSPL610 ELERLKLEPH 620 EGLLLRFPYA630 A
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Distearoyl phosphatidic acid | Ligand Info | |||||
| Structure Description | The LAT2-4F2hc complex in complex with leucine | PDB:7CMI | ||||
| Method | Electron microscopy | Resolution | 2.90 Å | Mutation | No | [3] |
| PDB Sequence |
TGLSKEELLK
172 VAGSPGWVRT182 RWALLLLFWL192 GWLGMLAGAV202 VIIVRAPRCR212 ELPAQKWWHT 222 GALYRIGDLQ232 AFQGHGAGNL242 AGLKGRLDYL252 SSLKVKGLVL262 GPIHKNQKDD 272 VAQTDLLQID282 PNFGSKEDFD292 SLLQSAKKKS302 IRVILDLTPN312 YRGENSWFST 322 QVDTVATKVK332 DALEFWLQAG342 VDGFQVRDIE352 NLKDASSFLA362 EWQNITKGFS 372 EDRLLIAGTN382 SSDLQQILSL392 LESNKDLLLT402 SSYLSDSGST412 GEHTKSLVTQ 422 YLNATGNRWC432 SWSLSQARLL442 TSFLPAQLLR452 LYQLMLFTLP462 GTPVFSYGDE 472 IGLDAAALPG482 QPMEAPVMLW492 DESSFPDIPG502 AVSANMTVKG512 QSEDPGSLLS 522 LFRRLSDQRS532 KERSLLHGDF542 HAFSAGPGLF552 SYIRHWDQNE562 RFLVVLNFGD 572 VGLSAGLQAS582 DLPASASLPA592 KADLLLSTQP602 GREEGSPLEL612 ERLKLEPHEG 622 LLLRFPYAA
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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 .3PH or .3PH2 or .3PH3 or :33PH;style chemicals stick;color identity;select .A:163 or .A:183 or .A:184 or .A:186 or .A:187 or .A:189 or .A:190 or .A:193 or .A:197; 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: Distearoyl phosphatidic acid | Ligand Info | |||||
| Structure Description | Overall structure of Erastin-bound xCT-4F2hc complex | PDB:7EPZ | ||||
| Method | Electron microscopy | Resolution | 3.40 Å | Mutation | No | [4] |
| PDB Sequence |
GLSKEELLKV
173 AGSPGWVRTR183 WALLLLFWLG193 WLGMLAGAVV203 IIVRAPRCRE213 LPAQKWWHTG 223 ALYRIGDLQA233 FQGHGAGNLA243 GLKGRLDYLS253 SLKVKGLVLG263 PIHKNQKDDV 273 AQTDLLQIDP283 NFGSKEDFDS293 LLQSAKKKSI303 RVILDLTPNY313 RGENSWFSTQ 323 VDTVATKVKD333 ALEFWLQAGV343 DGFQVRDIEN353 LKDASSFLAE363 WQNITKGFSE 373 DRLLIAGTNS383 SDLQQILSLL393 ESNKDLLLTS403 SYLSDSGSTG413 EHTKSLVTQY 423 LNATGNRWCS433 WSLSQARLLT443 SFLPAQLLRL453 YQLMLFTLPG463 TPVFSYGDEI 473 GLDAAALPGQ483 PMEAPVMLWD493 ESSFPDIPGA503 VSANMTVKGQ513 SEDPGSLLSL 523 FRRLSDQRSK533 ERSLLHGDFH543 AFSAGPGLFS553 YIRHWDQNER563 FLVVLNFGDV 573 GLSAGLQASD583 LPASASLPAK593 ADLLLSTQPG603 REEGSPLELE613 RLKLEPHEGL 623 LLRFPYAA
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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 .PX8 or .PX82 or .PX83 or :3PX8;style chemicals stick;color identity;select .A:183 or .A:186 or .A:187 or .A:190 or .A:191; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: Digitonin | Ligand Info | |||||
| Structure Description | Human LAT2-4F2hc complex in the apo-state | PDB:7B00 | ||||
| Method | Electron microscopy | Resolution | 3.98 Å | Mutation | No | [5] |
| PDB Sequence |
TGLSKEELLK
70 VAGSPGWVRT80 RWALLLLFWL90 GWLGMLAGAV100 VIIVRAPRCR110 ELPAQKWWHT 120 GALYRIGDLQ130 AFQGHGAGNL140 AGLKGRLDYL150 SSLKVKGLVL160 GPIHKNQKDD 170 VAQTDLLQID180 PNFGSKEDFD190 SLLQSAKKKS200 IRVILDLTPN210 YRGENSWFST 220 QVDTVATKVK230 DALEFWLQAG240 VDGFQVRDIE250 NLKDASSFLA260 EWQNITKGFS 270 EDRLLIAGTN280 SSDLQQILSL290 LESNKDLLLT300 SSYLSDSGST310 GEHTKSLVTQ 320 YLNATGNRWC330 SWSLSQARLL340 TSFLPAQLLR350 LYQLMLFTLP360 GTPVFSYGDE 370 IGLDAAALPG380 QPMEAPVMLW390 DESSFPDIPG400 AVSANMTVKG410 QSEDPGSLLS 420 LFRRLSDQRS430 KERSLLHGDF440 HAFSAGPGLF450 SYIRHWDQNE460 RFLVVLNFGD 470 VGLSAGLQAS480 DLPASASLPA490 KADLLLSTQP500 GREEGSPLEL510 ERLKLEPHEG 520 LLLRFPYAA
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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 .AJP or .AJP2 or .AJP3 or :3AJP;style chemicals stick;color identity;select .B:491 or .B:507; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Cryo-EM structure of the human L-type amino acid transporter 1 in complex with glycoprotein CD98hc. Nat Struct Mol Biol. 2019 Jun;26(6):510-517. | ||||
| REF 2 | Mechanism of substrate transport and inhibition of the human LAT1-4F2hc amino acid transporter. Cell Discov. 2021 Mar 23;7(1):16. | ||||
| REF 3 | Structural insight into the substrate recognition and transport mechanism of the human LAT2-4F2hc complex. Cell Discov. 2020 Nov 10;6(1):82. | ||||
| REF 4 | The structure of erastin-bound xCT-4F2hc complex?reveals molecular mechanisms underlying erastin-induced ferroptosis. Cell Res. 2022 Jul;32(7):687-690. | ||||
| REF 5 | Structural basis for substrate specificity of heteromeric transporters of neutral amino acids. Proc Natl Acad Sci U S A. 2021 Dec 7;118(49):e2113573118. | ||||
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