Binding Site Information of Target

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Target General Information
Drug Binding Sites of Target
References
Target General Information  Top
Target ID T93788 Target Info
Target Name Glucose-dependent insulinotropic receptor (GPR119)
Synonyms GPR119; G-protein coupled receptor 119
Target Type Successful Target
Gene Name GPR119
Biochemical Class GPCR rhodopsin
UniProt ID
GP119_HUMAN
Drug Binding Sites of Target  Top
Ligand Name: APD668 Ligand Info
Structure Description GPR119-Gs-APD668 complex PDB:7XZ6
Method Electron microscopy Resolution 2.80 Å Mutation No [1]
PDB Sequence
MESSFSFGVI
10
LAVLASLIIA
20
TNTLVAVAVL
30
LLIHKNDGVS
40
LCFTLNLAVA
50

DTLIGVAISG
60
LLTDQLSSPS
70
RPTQKTLCSL
80
RMAFVTSSAA
90
ASVLTVMLIT
100

FDRYLAIKQP
110
FRYLKIMSGF
120
VAGACIAGLW
130
LVSYLIGFLP
140
LGIPMFQQTA
150

YKGQCSFFAV
160
FHPHFVLTLS
170
CVGFFPAMLL
180
FVFFYCDMLK
190
IASMHSQQIR
200

KMEHAGAMAG
210
SDFKALRTVS
228
VLIGSFALSW
238
TPFLITGIVQ
248
VACQECHLYL
258

VLERYLWLLG
268
VGNSLLNPLI
278
YAYWQKEVRL
288
QLYHMALGVK
298
KV
Residue
Distance (Å)
PHE7
2.100
LEU11
2.687
ILE54
4.933
LEU61
2.437
GLN65
3.314
MET82
2.442
VAL85
2.574
THR86
2.706
ALA89
2.069
ALA90
2.138
VAL93
2.490
LEU94
2.245
VAL132
4.066
SER133
4.181
ILE136
2.279
CYS155
4.523
SER156
2.605
Residue
Distance (Å)
PHE157
2.733
PHE158
4.225
VAL166
3.262
LEU169
2.163
SER170
4.952
VAL172
4.310
GLY173
2.370
PHE174
2.223
ALA177
4.221
TRP238
2.714
PHE241
2.229
LEU242
2.522
LEU260
4.846
GLU261
2.061
ARG262
2.742
TRP265
2.317
VAL269
4.799
Ligand Name: (4r,7r,18e)-4,7-Dihydroxy-N,N,N-Trimethyl-10-Oxo-3,5,9-Trioxa-4-Phosphaheptacos-18-En-1-Aminium 4-Oxide Ligand Info
Structure Description GPR119-Gs-LPC complex PDB:7XZ5
Method Electron microscopy Resolution 3.10 Å Mutation No [1]
PDB Sequence
MESSFSFGVI
10
LAVLASLIIA
20
TNTLVAVAVL
30
LLIHKNDGVS
40
LCFTLNLAVA
50

DTLIGVAISG
60
LLTDQLSSPS
70
RPTQKTLCSL
80
RMAFVTSSAA
90
ASVLTVMLIT
100

FDRYLAIKQP
110
FRYLKIMSGF
120
VAGACIAGLW
130
LVSYLIGFLP
140
LGIPMFQQTA
150

YKGQCSFFAV
160
FHPHFVLTLS
170
CVGFFPAMLL
180
FVFFYCDMLK
190
IASMHSQQIR
200

KMEHAGAMAG
210
SDFKALRTVS
228
VLIGSFALSW
238
TPFLITGIVQ
248
VACQECHLYL
258

VLERYLWLLG
268
VGNSLLNPLI
278
YAYWQKEVRL
288
QLYHMALGVK
298
KV
Residue
Distance (Å)
SER4
4.274
PHE7
2.421
LEU11
4.733
ILE58
4.505
LEU61
2.871
ASP64
4.836
GLN65
1.377
MET82
3.182
VAL85
2.373
THR86
2.751
ALA89
2.463
ALA90
2.373
VAL93
2.509
LEU94
2.482
VAL132
4.415
ILE136
2.912
GLN148
4.644
LYS152
4.221
GLN154
3.812
CYS155
3.224
Residue
Distance (Å)
SER156
2.329
PHE157
2.408
PHE158
2.383
ALA159
2.411
VAL160
4.988
PHE165
4.760
VAL166
4.669
LEU169
2.333
VAL172
4.927
GLY173
2.508
PHE174
2.514
ALA177
3.801
TRP238
2.829
PHE241
2.857
LEU242
3.383
TYR257
2.421
LEU258
4.852
GLU261
2.329
ARG262
1.803
TRP265
2.764
References  Top
REF 1 Structural identification of lysophosphatidylcholines as activating ligands for orphan receptor GPR119. Nat Struct Mol Biol. 2022 Sep;29(9):863-870.

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