Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T18876 | Target Info | |||
| Target Name | Prostaglandin E2 receptor EP4 (PTGER4) | ||||
| Synonyms | Prostanoid EP4 receptor; Prostaglandin E2 receptor EP4 subtype; PTGER2; PGE2 receptor EP4 subtype; PGE receptor EP4 subtype | ||||
| Target Type | Clinical trial Target | ||||
| Gene Name | PTGER4 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Dinoprostone | Ligand Info | |||||
| Structure Description | Cryo-EM Structure of the Prostaglandin E Receptor EP4 Coupled to G Protein | PDB:7D7M | ||||
| Method | Electron microscopy | Resolution | 3.30 Å | Mutation | Yes | [1] |
| PDB Sequence |
SPVTIPAVMF
28 IFGVVGNLVA38 IVVLCKSRKE48 QKETTFYTLV58 CGLAVTDLLG68 TLLVSPVTIA 78 TYMKGQWPGG88 QPLCEYSTFI98 LLFFSLSGLS108 IICAMSVERY118 LAINHAYFYS 128 HYVDKRLAGL138 TLFAVYASNV148 LFCALPNMGL158 GSSRLQYPDT168 WCFIDWTTQV 178 TAHAAYSYMY188 AGFSSFLILA198 TVLCNVLVCG208 ALLRMHRQFF260 RRIAGAEIQM 270 VILLIATSLV280 VLICSIPLVV290 RVFVNQLYQP300 SLEREVSKNP310 DLQAIRIASV 320 NPILDPWIYI330 LLRKTVLSKA340 IEKIK
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PRO20
4.906
PRO24
3.447
MET27
3.120
PHE28
4.084
GLY68
3.771
THR69
3.080
VAL72
3.412
SER73
3.294
THR76
3.293
TYR80
3.133
LEU99
3.708
PHE102
4.799
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| Ligand Name: 4-[4-cyano-2-[[(2R)-2-(4-fluoranylnaphthalen-1-yl)propanoyl]amino]phenyl]butanoic acid | Ligand Info | |||||
| Structure Description | Crystal structure of the human prostaglandin E receptor EP4 in complex with Fab and ONO-AE3-208 | PDB:5YWY | ||||
| Method | X-ray diffraction | Resolution | 3.20 Å | Mutation | Yes | [2] |
| PDB Sequence |
NSPVTIPAVM
27 FIFGVVGNLV37 AIVVLCKSRK47 EQKETTFYTL57 VCGLLVTDLL67 GTLLVSPVTI 77 ATYMKGQWPG87 GQPLCEYSTF97 ILLFFSLSRL107 SIICAMSVER117 YLAINHAYFY 127 SHYVDKRLAG137 LTLFAVYASN147 VLFCALPNMG157 LGSSRLQYPD167 TWCFIDWTTQ 177 VTAHAAYSYM187 YAGFSSFLIL197 ATVLCNVLVC207 GALLRMHAGA266 EIQMVILLIA 276 TSLVVLICSI286 PLVVRVFVNQ296 LYQPSLEREV306 SKNPDLQAIR316 IASVNPILDP 326 WIYILLRKTV336 LSKAIEKIKC346
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| Ligand Name: 4-[2-[[(2R)-2-(4-bromanylnaphthalen-1-yl)propanoyl]amino]-4-cyano-phenyl]butanoic acid | Ligand Info | |||||
| Structure Description | Crystal structure of the human prostaglandin E receptor EP4 in complex with Fab and an antagonist Br-derivative | PDB:5YHL | ||||
| Method | X-ray diffraction | Resolution | 4.20 Å | Mutation | Yes | [2] |
| PDB Sequence |
NSPVTIPAVM
27 FIFGVVGNLV37 AIVVLCKSRK47 EQKETTFYTL57 VCGLLVTDLL67 GTLLVSPVTI 77 ATYMKGQWPG87 GQPLCEYSTF97 ILLFFSLSRL107 SIICAMSVER117 YLAINHAYFY 127 SHYVDKRLAG137 LTLFAVYASN147 VLFCALPNMG157 LGSSRLQYPD167 TWCFIDWTTQ 177 VTAHAAYSYM187 YAGFSSFLIL197 ATVLCNVLVC207 GALLRMHAGA266 EIQMVILLIA 276 TSLVVLICSI286 PLVVRVFVNQ296 LYQPSLEREV306 SKNPDLQAIR316 IASVNPILDP 326 WIYILLRKTV336 LSKAIEKIKC346
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Click to Show 3D Structure of This Binding Site
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Cryo-EM Structure of the Prostaglandin E Receptor EP4 Coupled to G Protein. Structure. 2021 Mar 4;29(3):252-260.e6. | ||||
| REF 2 | Ligand binding to human prostaglandin E receptor EP(4) at the lipid-bilayer interface. Nat Chem Biol. 2019 Jan;15(1):18-26. | ||||
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