Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T38529 | Target Info | |||
| Target Name | Prostaglandin E2 receptor EP2 (PTGER2) | ||||
| Synonyms | Prostanoid EP2 receptor; Prostaglandin E2 receptor EP2 subtype; PGE2 receptor EP2 subtype; PGE receptor, EP2 subtype; PGE receptor EP2 subtype; EP2 receptor | ||||
| Target Type | Successful Target | ||||
| Gene Name | PTGER2 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Dinoprostone | Ligand Info | |||||
| Structure Description | Cryo-EM structure of the PGE2-bound EP2-Gs complex | PDB:7CX2 | ||||
| Method | Electron microscopy | Resolution | 2.80 Å | Mutation | Yes | [1] |
| PDB Sequence |
ESPAISSVMF
32 SAGVLGNLIA42 LALLARSLFH68 VLVTELVFTD78 LLGTCLISPV88 VLASYARNQT 98 LVALAPESRA108 CTYFAFAMTF118 FSLATMLMLF128 AMALERYLSI138 GHPYFYQRRV 148 SRSGGLAVLP158 VIYAVSLLFC168 SLPLLDYGQY178 VQYCPGTWCF188 IRHGRTAYLQ 198 LYATLLLLLI208 VSVLACNFSV218 ILNLIRMHRR228 SRAEETDHLI264 LLAIMTITFA 274 VCSLPFTIFA284 YMNETSSRKE294 KWDLQALRFL304 SINSIIDPWV314 FAILRPPVLR 324 LMRSVL
|
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|
|
GLU23
4.394
SER28
2.624
MET31
3.604
PHE32
4.353
GLY81
4.424
THR82
3.445
ILE85
3.822
SER86
2.665
VAL89
3.246
TYR93
3.181
PHE112
4.831
MET116
3.217
PHE119
4.567
|
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| Ligand Name: Taprenepag | Ligand Info | |||||
| Structure Description | Cryo-EM structure of the Taprenepag-bound EP2-Gs complex | PDB:7CX3 | ||||
| Method | Electron microscopy | Resolution | 2.80 Å | Mutation | Yes | [1] |
| PDB Sequence |
ESPAISSVMF
32 SAGVLGNLIA42 LALLARSLFH68 VLVTELVFTD78 LLGTCLISPV88 VLASYARNQT 98 LVALAPESRA108 CTYFAFAMTF118 FSLATMLMLF128 AMALERYLSI138 GHPYFYQRRV 148 SRSGGLAVLP158 VIYAVSLLFC168 SLPLLDYGQY178 VQYCPGTWCF188 IRHGRTAYLQ 198 LYATLLLLLI208 VSVLACNFSV218 ILNLIRMHRR228 SAEETDHLIL265 LAIMTITFAV 275 CSLPFTIFAY285 MNETSSRKEK295 WDLQALRFLS305 INSIIDPWVF315 AILRPPVLRL 325 MRSVL
|
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|
|
SER28
2.967
MET31
3.389
PHE32
3.863
GLY35
4.999
THR77
4.297
ASP78
3.712
GLY81
3.702
THR82
2.796
ILE85
3.479
SER86
2.649
VAL89
3.227
TYR93
3.368
PHE112
4.776
MET116
3.455
|
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| Ligand Name: CP-533536 | Ligand Info | |||||
| Structure Description | Cryo-EM structure of the Evatanepag-bound EP2-Gs complex | PDB:7CX4 | ||||
| Method | Electron microscopy | Resolution | 2.90 Å | Mutation | Yes | [1] |
| PDB Sequence |
GESPAISSVM
31 FSAGVLGNLI41 ALALLARSLF67 HVLVTELVFT77 DLLGTCLISP87 VVLASYARNQ 97 TLVALAPESR107 ACTYFAFAMT117 FFSLATMLML127 FAMALERYLS137 IGHPYFYQRR 147 VSRSGGLAVL157 PVIYAVSLLF167 CSLPLLDYGQ177 YVQYCPGTWC187 FIRHGRTAYL 197 QLYATLLLLL207 IVSVLACNFS217 VILNLIRMHR227 RSAEETDHLI264 LLAIMTITFA 274 VCSLPFTIFA284 YMNETSSRKE294 KWDLQALRFL304 SINSIIDPWV314 FAILRPPVLR 324 LMRSVL
|
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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 .GM9 or .GM92 or .GM93 or :3GM9;style chemicals stick;color identity;select .R:28 or .R:31 or .R:32 or .R:35 or .R:78 or .R:81 or .R:82 or .R:85 or .R:86 or .R:89 or .R:93 or .R:116 or .R:119 or .R:120 or .R:123 or .R:185 or .R:186 or .R:298 or .R:301 or .R:302 or .R:304 or .R:305 or .R:306 or .R:308 or .R:309; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
SER28
2.572
MET31
3.416
PHE32
4.697
GLY35
4.645
ASP78
4.308
GLY81
4.793
THR82
2.878
ILE85
3.595
SER86
2.735
VAL89
3.276
TYR93
2.405
MET116
3.321
PHE119
3.171
|
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Ligand recognition, unconventional activation, and G protein coupling of the prostaglandin E(2) receptor EP2 subtype. Sci Adv. 2021 Apr 2;7(14):eabf1268. | ||||
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