Target Binding Site Detail
| 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 | |||||
| Ligand General Information | Top | ||||
|---|---|---|---|---|---|
| Ligand Name | Cholesterol hemisuccinate | Ligand Info | |||
| Canonical SMILES | CC(C)CCCC(C)C1CCC2C1(CCC3C2CC=C4C3(CCC(C4)OC(=O)CCC(=O)O)C)C | ||||
| InChI | 1S/C31H50O4/c1-20(2)7-6-8-21(3)25-11-12-26-24-10-9-22-19-23(35-29(34)14-13-28(32)33)15-17-30(22,4)27(24)16-18-31(25,26)5/h9,20-21,23-27H,6-8,10-19H2,1-5H3,(H,32,33)/t21-,23+,24+,25-,26+,27+,30+,31-/m1/s1 | ||||
| InChIKey | WLNARFZDISHUGS-MIXBDBMTSA-N | ||||
| PubChem Compound ID | 65082 | ||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| PDB ID: 7DSK Overall structure of the LAT1-4F2hc bound with JX-075 | ||||||
| Method | Electron microscopy | Resolution | 2.90 Å | Mutation | No | [1] |
| 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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| PDB ID: 7DSL Overall structure of the LAT1-4F2hc bound with JX-078 | ||||||
| Method | Electron microscopy | Resolution | 2.90 Å | Mutation | No | [1] |
| 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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| PDB ID: 7DSN Overall structure of the LAT1-4F2hc bound with JX-119 | ||||||
| Method | Electron microscopy | Resolution | 3.10 Å | Mutation | No | [1] |
| 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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| PDB ID: 7DSQ Overall structure of the LAT1-4F2hc bound with 3,5-diiodo-L-tyrosine | ||||||
| Method | Electron microscopy | Resolution | 3.40 Å | Mutation | No | [1] |
| PDB Sequence |
FTGLSKEELL
171 KVAGSPGWVR181 TRWALLLLFW191 LGWLGMLAGA201 VVIIVRAPRC211 RELPAQKWWH 221 TGALYRIGDL231 QAFQGHGAGN241 LAGLKGRLDY251 LSSLKVKGLV261 LGPIHKNQKD 271 DVAQTDLLQI281 DPNFGSKEDF291 DSLLQSAKKK301 SIRVILDLTP311 NYRGENSWFS 321 TQVDTVATKV331 KDALEFWLQA341 GVDGFQVRDI351 ENLKDASSFL361 AEWQNITKGF 371 SEDRLLIAGT381 NSSDLQQILS391 LLESNKDLLL401 TSSYLSDSGS411 TGEHTKSLVT 421 QYLNATGNRW431 CSWSLSQARL441 LTSFLPAQLL451 RLYQLMLFTL461 PGTPVFSYGD 471 EIGLDAAALP481 GQPMEAPVML491 WDESSFPDIP501 GAVSANMTVK511 GQSEDPGSLL 521 SLFRRLSDQR531 SKERSLLHGD541 FHAFSAGPGL551 FSYIRHWDQN561 ERFLVVLNFG 571 DVGLSAGLQA581 SDLPASASLP591 AKADLLLSTQ601 PGREEGSPLE611 LERLKLEPHE 621 GLLLRFPYAA631
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Click to Show 3D Structure of This Binding Site
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Mechanism of substrate transport and inhibition of the human LAT1-4F2hc amino acid transporter. Cell Discov. 2021 Mar 23;7(1):16. | ||||
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