Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T92640 | Target Info | |||
| Target Name | Lysophosphatidic acid receptor 1 (LPAR1) | ||||
| Synonyms | Lysophosphatidic acid receptor Edg-2; LPA1; LPA-1; LPA receptor 1; EDG2; EDG 2 receptor | ||||
| Target Type | Clinical trial Target | ||||
| Gene Name | LPAR1 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: (2r)-2-Hydroxy-3-(Phosphonooxy)propyl (9e)-Octadec-9-Enoate | Ligand Info | |||||
| Structure Description | Lysophosphatidic acid receptor 1-Gi complex bound to LPA | PDB:7TD0 | ||||
| Method | Electron microscopy | Resolution | 2.83 Å | Mutation | Yes | [1] |
| PDB Sequence |
QCFYNESIAF
32 FYNRSGKHLA42 TEWNTVSKLV52 MGLGITVCIF62 IMLANLLVMV72 AIYVNRRFHF 82 PIYYLMANLA92 AADFFAGLAY102 FYLMFNTGPN112 TRRLTVSTWL122 LRQGLIDTSL 132 TASVANLLAI142 AIERHITVFR152 MQLHTRMSNR162 RVVVVIVVIW172 TMAIVMGAIP 182 SVGWNCICDI192 ENCSNMAPLY202 SDSYLVFWAI212 FNLVTFVVMV222 VLYAHIFGYV 232 RQRTMRMDTM253 MSLLKTVVIV263 LGAFIICWTP273 GLVLLLLDVC283 CPQCDVLAYE 293 KFFLLLAEFN303 SAMNPIIYSY313 RDKEMSATFR323
|
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|
|
TYR34
2.408
LYS39
2.475
HIS40
4.613
TYR102
4.756
LEU105
2.490
THR109
2.379
GLY110
2.634
THR113
2.182
TRP121
4.720
ARG124
2.503
GLN125
2.059
ILE128
2.557
ASP129
2.796
LEU132
2.217
THR133
4.597
SER196
4.207
MET198
2.331
|
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: [(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate | Ligand Info | |||||
| Structure Description | Human Lysophosphatidic Acid Receptor 1-Gi complex bound to ONO-0740556 | PDB:7YU3 | ||||
| Method | Electron microscopy | Resolution | 3.50 Å | Mutation | No | [2] |
| PDB Sequence |
QCFYNESIAF
32 FYNRSGKHLA42 TEWNTVSKLV52 MGLGITVCIF62 IMLANLLVMV72 AIYVNRRFHF 82 PIYYLMANLA92 AADFFAGLAY102 FYLMFNTGPN112 TRRLTVSTWL122 LRQGLIDTSL 132 TASVANLLAI142 AIERHITVFR152 MQLHTRMSNR162 RVVVVIVVIW172 TMAIVMGAIP 182 SVGWNCICDI192 ENCSNMAPLY202 SDSYLVFWAI212 FNLVTFVVMV222 VLYAHIFGYV 232 RQRTMRMDTM253 MSLLKTVVIV263 LGAFIICWTP273 GLVLLLLDVC283 CPQCDVLAYE 293 KFFLLLAEFN303 SAMNPIIYSY313 RDKEMSATFR323
|
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|
|
TYR34
3.171
LYS39
2.642
LEU105
3.617
ASN108
4.207
THR109
3.366
GLY110
4.196
THR113
3.967
ARG124
2.503
GLN125
3.258
ILE128
4.876
ASP129
3.038
LEU132
4.789
MET198
4.696
ALA199
4.033
|
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Differential activation mechanisms of lipid GPCRs by lysophosphatidic acid and sphingosine 1-phosphate. Nat Commun. 2022 Feb 8;13(1):731. | ||||
| REF 2 | Structure of the active G(i)-coupled human lysophosphatidic acid receptor 1 complexed with a potent agonist. Nat Commun. 2022 Sep 15;13(1):5417. | ||||
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