Target Binding Site Detail
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T48330 | Target Info | |||
| Target Name | Large neutral amino acids transporter 1 (SLC7A5) | ||||
| Synonyms | y+ system cationic amino acid transporter; Solute carrier family 7 member 5; MPE16; Large neutral amino acids transporter small subunit 1; LAT1; L-type amino acid transporter LAT1; L-type amino acid transporter 1; Integral membrane protein E16; HLAT1; CD98LC; CD98 light chain; 4F2LC; 4F2 light chain; 4F2 LC | ||||
| Target Type | Literature-reported Target | ||||
| Gene Name | SLC7A5 | ||||
| Biochemical Class | Amino acid-polyamine-organocation | ||||
| UniProt ID | |||||
| Ligand General Information | Top | ||||
|---|---|---|---|---|---|
| Ligand Name | Distearoyl phosphatidic acid | Ligand Info | |||
| Canonical SMILES | CCCCCCCCCCCCCCCCCC(=O)OCC(COP(=O)(O)O)OC(=O)CCCCCCCCCCCCCCCCC | ||||
| InChI | 1S/C39H77O8P/c1-3-5-7-9-11-13-15-17-19-21-23-25-27-29-31-33-38(40)45-35-37(36-46-48(42,43)44)47-39(41)34-32-30-28-26-24-22-20-18-16-14-12-10-8-6-4-2/h37H,3-36H2,1-2H3,(H2,42,43,44)/t37-/m1/s1 | ||||
| InChIKey | YFWHNAWEOZTIPI-DIPNUNPCSA-N | ||||
| PubChem Compound ID | 447938 | ||||
| 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 |
VTLQRNITLL
53 NGVAIIVGTI63 IGSGIFVTPT73 GVLKEAGSPG83 LALVVWAACG93 VFSIVGALCY 103 AELGTTISKS113 GGDYAYMLEV123 YGSLPAFLKL133 WIELLIIRPS143 SQYIVALVFA 153 TYLLKPLFPT163 CPVPEEAAKL173 VACLCVLLLT183 AVNCYSVKAA193 TRVQDAFAAA 203 KLLALALIIL213 LGFVQIGKGD223 VSNLDPNFSF233 EGTKLDVGNI243 VLALYSGLFA 253 YGGWNYLNFV263 TEEMINPYRN273 LPLAIIISLP283 IVTLVYVLTN293 LAYFTTLSTE 303 QMLSSEAVAV313 DFGNYHLGVM323 SWIIPVFVGL333 SCFGSVNGSL343 FTSSRLFFVG 353 SREGHLPSIL363 SMIHPQLLTP373 VPSLVFTCVM383 TLLYAFSKDI393 FSVINFFSFF 403 NWLCVALAII413 GMIWLRHRKP423 ELERPIKVNL433 ALPVFFILAC443 LFLIAVSFWK 453 TPVECGIGFT463 IILSGLPVYF473 FGVWWKNKPK483 WLLQGIFSTT493 VLCQKLMQVV 503 PQET
|
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|
|
PHE130
3.796
TRP134
4.481
LEU137
4.921
GLY357
4.604
HIS358
2.898
LEU359
3.744
PRO360
3.583
SER361
3.090
ILE362
3.837
LEU363
4.346
PRO375
4.299
VAL378
3.772
|
|||||
| 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 |
VTLQRNITLL
53 NGVAIIVGTI63 IGSGIFVTPT73 GVLKEAGSPG83 LALVVWAACG93 VFSIVGALCY 103 AELGTTISKS113 GGDYAYMLEV123 YGSLPAFLKL133 WIELLIIRPS143 SQYIVALVFA 153 TYLLKPLFPT163 CPVPEEAAKL173 VACLCVLLLT183 AVNCYSVKAA193 TRVQDAFAAA 203 KLLALALIIL213 LGFVQIGKGD223 VSNLDPNFSF233 EGTKLDVGNI243 VLALYSGLFA 253 YGGWNYLNFV263 TEEMINPYRN273 LPLAIIISLP283 IVTLVYVLTN293 LAYFTTLSTE 303 QMLSSEAVAV313 DFGNYHLGVM323 SWIIPVFVGL333 SCFGSVNGSL343 FTSSRLFFVG 353 SREGHLPSIL363 SMIHPQLLTP373 VPSLVFTCVM383 TLLYAFSKDI393 FSVINFFSFF 403 NWLCVALAII413 GMIWLRHRKP423 ELERPIKVNL433 ALPVFFILAC443 LFLIAVSFWK 453 TPVECGIGFT463 IILSGLPVYF473 FGVWWKNKPK483 WLLQGIFSTT493 VLCQKLMQVV 503 PQET
|
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|
|
PHE130
4.672
TRP134
4.299
LEU137
4.948
GLY357
4.868
HIS358
3.443
LEU359
3.876
PRO360
3.679
SER361
3.448
ILE362
4.014
LEU363
4.276
PRO375
4.169
VAL378
3.828
|
|||||
| 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 |
VTLQRNITLL
53 NGVAIIVGTI63 IGSGIFVTPT73 GVLKEAGSPG83 LALVVWAACG93 VFSIVGALCY 103 AELGTTISKS113 GGDYAYMLEV123 YGSLPAFLKL133 WIELLIIRPS143 SQYIVALVFA 153 TYLLKPLFPT163 CPVPEEAAKL173 VACLCVLLLT183 AVNCYSVKAA193 TRVQDAFAAA 203 KLLALALIIL213 LGFVQIGKGD223 VSNLDPNFSF233 EGTKLDVGNI243 VLALYSGLFA 253 YGGWNYLNFV263 TEEMINPYRN273 LPLAIIISLP283 IVTLVYVLTN293 LAYFTTLSTE 303 QMLSSEAVAV313 DFGNYHLGVM323 SWIIPVFVGL333 SCFGSVNGSL343 FTSSRLFFVG 353 SREGHLPSIL363 SMIHPQLLTP373 VPSLVFTCVM383 TLLYAFSKDI393 FSVINFFSFF 403 NWLCVALAII413 GMIWLRHRKP423 ELERPIKVNL433 ALPVFFILAC443 LFLIAVSFWK 453 TPVECGIGFT463 IILSGLPVYF473 FGVWWKNKPK483 WLLQGIFSTT493 VLCQKLMQVV 503 PQET
|
|||||
|
|
PHE130
3.960
TRP134
3.800
GLY357
4.336
HIS358
2.872
LEU359
3.713
PRO360
3.648
SER361
2.909
ILE362
3.757
LEU363
3.949
PRO375
3.596
VAL378
3.766
|
|||||
| PDB ID: 6IRS human LAT1-4F2hc complex incubated with JPH203 | ||||||
| Method | Electron microscopy | Resolution | 3.30 Å | Mutation | Yes | [2] |
| PDB Sequence |
TLLNGVAIIV
60 GTIIGSGIFV70 TPTGVLKEAG80 SPGLALVVWA90 ACGVFSIVGA100 LCYAELGTTI 110 SKSGGDYAYM120 LEVYGSLPAF130 LKLWIELLII140 RPSSQYIVAL150 VFATYLLKPL 160 FPTCPVPEEA170 AKLVACLCVL180 LLTAVNCYSV190 KAATRVQDAF200 AAAKLLALAL 210 IILLGFVQIG220 KGDVSNLDPN230 FSFEGTKLDV240 GNIVLALYSG250 LFAYGGWNYL 260 NFVTEEMINP270 YRNLPLAIII280 SLPIVTLVYV290 LTNLAYFTTL300 STEQMLSSEA 310 VAVDFGNYHL320 GVMSWIIPVF330 VGLSCFGSVN340 GSLFTSSRLF350 FVGSREGHLP 360 SILSMIHPQL370 LTPVPSLVFT380 CVMTLLYAFS390 KDIFSVINFF400 SFFNWLCVAL 410 AIIGMIWLRH420 RKPELERPIK430 VNLALPVFFI440 LACLFLIAVS450 FWKTPVECGI 460 GFTIILSGLP470 VYFFGVWWKN480 KPKWLLQGIF490 STTVLCQKLM500 QVVPQET |
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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 .B:130 or .B:134 or .B:180 or .B:183 or .B:184 or .B:187 or .B:188 or .B:357 or .B:358 or .B:359 or .B:360 or .B:361 or .B:362 or .B:363 or .B:367 or .B:374 or .B:375 or .B:378 or .B:379 or .B:381 or .B:382 or .B:471 or .B:474 or .B:475 or .B:489 or .B:496 or .B:499 or .B:500 or .B:501; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
PHE130
3.584
TRP134
3.418
LEU180
3.508
THR183
3.953
ALA184
3.821
CYS187
3.288
TYR188
3.444
GLY357
4.395
HIS358
3.844
LEU359
2.930
PRO360
2.512
SER361
2.842
ILE362
4.133
LEU363
4.679
HIS367
2.500
|
|||||
| 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 |
VTLQRNITLL
53 NGVAIIVGTI63 IGSGIFVTPT73 GVLKEAGSPG83 LALVVWAACG93 VFSIVGALCY 103 AELGTTISKS113 GGDYAYMLEV123 YGSLPAFLKL133 WIELLIIRPS143 SQYIVALVFA 153 TYLLKPLFPT163 CPVPEEAAKL173 VACLCVLLLT183 AVNCYSVKAA193 TRVQDAFAAA 203 KLLALALIIL213 LGFVQIGKGD223 VSNLDPNFSF233 EGTKLDVGNI243 VLALYSGLFA 253 YGGWNYLNFV263 TEEMINPYRN273 LPLAIIISLP283 IVTLVYVLTN293 LAYFTTLSTE 303 QMLSSEAVAV313 DFGNYHLGVM323 SWIIPVFVGL333 SCFGSVNGSL343 FTSSRLFFVG 353 SREGHLPSIL363 SMIHPQLLTP373 VPSLVFTCVM383 TLLYAFSKDI393 FSVINFFSFF 403 NWLCVALAII413 GMIWLRHRKP423 ELERPIKVNL433 ALPVFFILAC443 LFLIAVSFWK 453 TPVECGIGFT463 IILSGLPVYF473 FGVWWKNKPK483 WLLQGIFSTT493 VLCQKLMQVV 503 PQET
|
|||||
|
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 .B:130 or .B:134 or .B:137 or .B:357 or .B:358 or .B:359 or .B:360 or .B:361 or .B:362 or .B:363 or .B:375 or .B:378 or .B:379 or .B:382 or .B:471 or .B:474 or .B:475 or .B:476 or .B:481 or .B:489 or .B:492 or .B:495 or .B:496 or .B:500; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
PHE130
4.515
TRP134
3.922
LEU137
4.446
GLY357
4.069
HIS358
3.217
LEU359
3.563
PRO360
3.634
SER361
2.950
ILE362
4.128
LEU363
3.792
PRO375
3.443
VAL378
3.781
|
|||||
| PDB ID: 6IRT human LAT1-4F2hc complex bound with BCH | ||||||
| Method | Electron microscopy | Resolution | 3.50 Å | Mutation | Yes | [2] |
| PDB Sequence |
TLLNGVAIIV
60 GTIIGSGIFV70 TPTGVLKEAG80 SPGLALVVWA90 ACGVFSIVGA100 LCYAELGTTI 110 SKSGGDYAYM120 LEVYGSLPAF130 LKLWIELLII140 RPSSQYIVAL150 VFATYLLKPL 160 FPTCPVPEEA170 AKLVACLCVL180 LLTAVNCYSV190 KAATRVQDAF200 AAAKLLALAL 210 IILLGFVQIG220 KGDVSNLDPN230 FSFEGTKLDV240 GNIVLALYSG250 LFAYGGWNYL 260 NFVTEEMINP270 YRNLPLAIII280 SLPIVTLVYV290 LTNLAYFTTL300 STEQMLSSEA 310 VAVDFGNYHL320 GVMSWIIPVF330 VGLSCFGSVN340 GSLFTSSRLF350 FVGSREGHLP 360 SILSMIHPQL370 LTPVPSLVFT380 CVMTLLYAFS390 KDIFSVINFF400 SFFNWLCVAL 410 AIIGMIWLRH420 RKPELERPIK430 VNLALPVFFI440 LACLFLIAVS450 FWKTPVECGI 460 GFTIILSGLP470 VYFFGVWWKN480 KPKWLLQGIF490 STTVLCQKLM500 QVVPQET |
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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 .B:130 or .B:134 or .B:180 or .B:183 or .B:184 or .B:187 or .B:188 or .B:357 or .B:358 or .B:359 or .B:360 or .B:361 or .B:362 or .B:363 or .B:367 or .B:374 or .B:375 or .B:378 or .B:379 or .B:381 or .B:382 or .B:385 or .B:471 or .B:474 or .B:475 or .B:476 or .B:489 or .B:492 or .B:496 or .B:499 or .B:500 or .B:501; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
PHE130
4.036
TRP134
4.528
LEU180
3.144
THR183
3.802
ALA184
4.111
CYS187
3.664
TYR188
2.821
GLY357
3.710
HIS358
3.653
LEU359
3.053
PRO360
3.422
SER361
3.003
ILE362
4.585
LEU363
3.992
HIS367
3.551
VAL374
4.267
|
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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. | ||||
| REF 2 | Structure of the human LAT1-4F2hc heteromeric amino acid transporter complex. Nature. 2019 Apr;568(7750):127-130. | ||||
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