Binding Site Information of Target
| 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 | |||||
| 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 |
ITLLNGVAII
59 VGTIIGSGIF69 VTPTGVLKEA79 GSPGLALVVW89 AACGVFSIVG99 ALCYAELGTT 109 ISKSGGDYAY119 MLEVYGSLPA129 FLKLWIELLI139 IRPSSQYIVA149 LVFATYLLKP 159 LFPTCPVPEE169 AAKLVACLCV179 LLLTAVNCYS189 VKAATRVQDA199 FAAAKLLALA 209 LIILLGFVQI219 FSFEGTKLDV240 GNIVLALYSG250 LFAYGGWNYL260 NFVTEEMINP 270 YRNLPLAIII280 SLPIVTLVYV290 LTNLAYFTTL300 STEQMLSSEA310 VAVDFGNYHL 320 GVMSWIIPVF330 VGLSCFGSVN340 GSLFTSSRLF350 FVLLTPVPSL377 VFTCVMTLLY 387 AFSKDIFSVI397 NFFSFFNWLC407 VALAIIGMIW417 LRHRKPELER427 PIKVNLALPV 437 FFILACLFLI447 AVSFWKTPVE457 CGIGFTIILS467 GLPVYFFGVW477 WKN |
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LEU138
4.239
ILE139
4.025
PHE152
4.885
LEU156
3.717
PRO159
3.566
LEU160
4.969
GLU169
3.348
LYS172
3.874
LEU173
3.762
LEU180
4.356
THR183
4.193
ALA184
4.133
CYS187
3.721
TYR188
4.061
TRP325
4.643
PRO328
4.751
VAL329
3.702
LEU333
3.732
PHE336
3.655
VAL378
3.752
CYS381
4.177
VAL382
3.848
|
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| Ligand Name: 3,5-diiodo-L-tyrosine | Ligand Info | |||||
| Structure Description | Overall structure of the LAT1-4F2hc bound with 3,5-diiodo-L-tyrosine | PDB:7DSQ | ||||
| Method | Electron microscopy | Resolution | 3.40 Å | Mutation | No | [2] |
| 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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| Ligand Name: (2S)-2-amino-7-(naphthalen-1-ylmethoxy)-3,4-dihydro-1H-naphthalene-2-carboxylic acid | 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 |
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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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .HNX or .HNX2 or .HNX3 or :3HNX;style chemicals stick;color identity;select .B:62 or .B:63 or .B:64 or .B:65 or .B:66 or .B:67 or .B:68 or .B:139 or .B:140 or .B:143 or .B:144 or .B:147 or .B:148 or .B:252 or .B:253 or .B:254 or .B:255 or .B:256 or .B:259 or .B:289 or .B:338 or .B:396 or .B:397 or .B:400 or .B:401 or .B:404; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
THR62
3.290
ILE63
2.705
ILE64
4.905
GLY65
3.790
SER66
3.000
GLY67
2.694
ILE68
4.709
ILE139
4.068
ILE140
3.499
SER143
3.107
SER144
3.505
ILE147
4.918
VAL148
3.674
|
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| Ligand Name: (2S)-2-amino-7-[(2-phenylphenyl)methoxy]-3,4-dihydro-1H-naphthalene-2-carboxylic acid | Ligand Info | |||||
| Structure Description | Overall structure of the LAT1-4F2hc bound with JX-078 | PDB:7DSL | ||||
| Method | Electron microscopy | Resolution | 2.90 Å | Mutation | No | [2] |
| 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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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .HO0 or .HO02 or .HO03 or :3HO0;style chemicals stick;color identity;select .B:62 or .B:63 or .B:64 or .B:65 or .B:66 or .B:67 or .B:68 or .B:139 or .B:140 or .B:143 or .B:144 or .B:148 or .B:251 or .B:252 or .B:253 or .B:254 or .B:255 or .B:256 or .B:259 or .B:289 or .B:338 or .B:396 or .B:397 or .B:400 or .B:401 or .B:404 or .B:405; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
THR62
3.297
ILE63
2.884
ILE64
4.958
GLY65
3.747
SER66
3.021
GLY67
2.571
ILE68
4.720
ILE139
4.686
ILE140
3.541
SER143
4.370
SER144
4.104
VAL148
3.507
LEU251
3.712
PHE252
3.183
|
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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 |
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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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 .B:181 or .B:185 or .B:188 or .B:189 or .B:191 or .B:192 or .B:195 or .B:196 or .B:199 or .B:200 or .B:336 or .B:367 or .B:369 or .B:370 or .B:374 or .B:378 or .B:496 or .B:499 or .B:500 or .B:501; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU181
4.802
VAL185
4.323
TYR188
3.975
SER189
4.384
LYS191
2.670
ALA192
3.620
ARG195
4.151
VAL196
3.674
ALA199
4.559
PHE200
3.690
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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 the LAT1-4F2hc bound with JX-075 | PDB:7DSK | ||||
| Method | Electron microscopy | Resolution | 2.90 Å | Mutation | No | [2] |
| 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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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:470 or .B:471 or .B:474 or .B:475 or .B:476 or .B:481 or .B:489 or .B:496 or .B:500; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
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
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: (2~{S})-2-azanyl-7-[[2-(1,3-benzoxazol-2-yl)phenyl]methoxy]-3,4-dihydro-1~{H}-naphthalene-2-carboxylic acid | Ligand Info | |||||
| Structure Description | Overall structure of the LAT1-4F2hc bound with JX-119 | PDB:7DSN | ||||
| Method | Electron microscopy | Resolution | 3.10 Å | Mutation | No | [2] |
| 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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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .HO9 or .HO92 or .HO93 or :3HO9;style chemicals stick;color identity;select .B:62 or .B:63 or .B:64 or .B:65 or .B:66 or .B:67 or .B:68 or .B:140 or .B:143 or .B:144 or .B:147 or .B:148 or .B:252 or .B:253 or .B:254 or .B:255 or .B:256 or .B:259 or .B:338 or .B:393 or .B:394 or .B:396 or .B:397 or .B:400 or .B:401 or .B:404; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
THR62
2.701
ILE63
3.243
ILE64
4.737
GLY65
3.007
SER66
2.641
GLY67
2.654
ILE68
4.820
ILE140
3.191
SER143
4.740
SER144
3.946
ILE147
2.265
VAL148
4.322
PHE252
2.800
|
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| Ligand Name: (1S,2S,4R)-2-aminobicyclo[2.2.1]heptane-2-carboxylic acid | Ligand Info | |||||
| Structure Description | human LAT1-4F2hc complex bound with BCH | PDB:6IRT | ||||
| Method | Electron microscopy | Resolution | 3.50 Å | Mutation | Yes | [3] |
| 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 .AUU or .AUU2 or .AUU3 or :3AUU;style chemicals stick;color identity;select .B:62 or .B:64 or .B:65 or .B:66 or .B:67 or .B:144 or .B:148 or .B:252 or .B:253 or .B:254 or .B:255 or .B:256 or .B:259 or .B:338; color #f3c393; 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 | Structure of the human LAT1-4F2hc heteromeric amino acid transporter complex. Nature. 2019 Apr;568(7750):127-130. | ||||
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