Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T41750 | Target Info | |||
| Target Name | Gastric inhibitory polypeptide receptor (GIPR) | ||||
| Synonyms | Glucosedependent insulinotropic polypeptide receptor; GIPR | ||||
| Target Type | Successful Target | ||||
| Gene Name | GIPR | ||||
| Biochemical Class | GPCR secretin | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: L-glutamic acid | Ligand Info | |||||
| Structure Description | Cryo-EM structure of the GIPR/GLP-1R/GCGR triagonist peptide 20-bound human GIPR-Gs complex | PDB:7FIN | ||||
| Method | Electron microscopy | Resolution | 3.10 Å | Mutation | Yes | [1] |
| PDB Sequence |
QTAGELYQRW
39 ERYRRECQET49 LAAAACNGSF65 DMYVCWDYAA75 PNATARASCP85 WYLPWHHHVA 95 AGFVLRQCGS105 DGQWGLWRDH115 TQCENPEKNE125 AFLDQRLILE135 RLQVMYTVGY 145 SLSLATLLLA155 LLILSLFRRL165 HCTRNYIHIN175 LFTSFMLRAA185 AILSRDRLLP 195 RPGPYLGDQA205 LALWNQALAA215 CRTAQIVTQY225 CVGANYTWLL235 VEGVYLHSLL 245 VLVGGSEEGH255 FRYYLLLGWG265 APALFVIPWV275 IVRYLYENTQ285 CWERNEVKAI 295 WWIIRTPILM305 TILINFLIFI315 RILGILLSKL325 RTRQMRCRDY335 RLRLARSTLF 345 LVPLLGVHEV355 VFAPVTEEQA365 RGALRFAKLG375 FEIFLSSFQG385 FLVSVLYCFI 395 NKEVQSEIRR405 GWHHCRLRRS415
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| Ligand Name: Alpha-Aminoisobutyric Acid | Ligand Info | |||||
| Structure Description | cryo-EM structure of human Gastric inhibitory polypeptide receptor GIPR bound to tirzepatide | PDB:7RBT | ||||
| Method | Electron microscopy | Resolution | 3.08 Å | Mutation | No | [2] |
| PDB Sequence |
GQTAGELYQR
38 WERYRRECQE48 TLAAAEPPSG58 LACNGSFDMY68 VCWDYAAPNA78 TARASCPWYL 88 PWHHHVAAGF98 VLRQCGSDGQ108 WGLWRDHTQC118 ENPEKNEAFL128 DQRLILERLQ 138 VMYTVGYSLS148 LATLLLALLI158 LSLFRRLHCT168 RNYIHINLFT178 SFMLRAAAIL 188 SRDRLLPRPG198 PYLGDQALAL208 WNQALAACRT218 AQIVTQYCVG228 ANYTWLLVEG 238 VYLHSLLVLV248 GGSEEGHFRY258 YLLLGWGAPA268 LFVIPWVIVR278 YLYENTQCWE 288 RNEVKAIWWI298 IRTPILMTIL308 INFLIFIRIL318 GILLSKLRTR328 DYRLRLARST 343 LTLVPLLGVH353 EVVFAPVTEE363 QARGALRFAK373 LGFEIFLSSF383 QGFLVSVLYC 393 FINKEVQSEI403 RRGWHHCR
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Cholesterol | Ligand Info | |||||
| Structure Description | Structural basis of ligand selectivity conferred by the human glucose-dependent insulinotropic polypeptide receptor | PDB:7DTY | ||||
| Method | Electron microscopy | Resolution | 2.98 Å | Mutation | No | [3] |
| PDB Sequence |
TAGELYQRWE
40 RYRRECQETA60 CNGSFDMYVC70 WDYAAPNATA80 RASCPWYLPW90 HHHVAAGFVL 100 RQCWRDHTQC118 ENPEKNEAFL128 DQRLILERLQ138 VMYTVGYSLS148 LATLLLALLI 158 LSLFRRLHCT168 RNYIHINLFT178 SFMLRAAAIL188 SRDRLLPRPG198 PYLGDQALAL 208 WNQALAACRT218 AQIVTQYCVG228 ANYTWLLVEG238 VYLHSLLVLV248 GGSEEGHFRY 258 YLLLGWGAPA268 LFVIPWVIVR278 YLYENTQCWE288 RNEVKAIWWI298 IRTPILMTIL 308 INFLIFIRIL318 GILLSKLRTR328 QMRCRDYRLR338 LARSTLFLVP348 LLGVHEVVFA 358 PVTEEQARGA368 LRFAKLGFEI378 FLSSFQGFLV388 SVLYCFINKE398 VQSEIRRGWH 408 HCRLRRS
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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 .CLR or .CLR2 or .CLR3 or :3CLR;style chemicals stick;color identity;select .R:133 or .R:137 or .R:140 or .R:171 or .R:174 or .R:175 or .R:178 or .R:182 or .R:214 or .R:217 or .R:218 or .R:221 or .R:225 or .R:235 or .R:239 or .R:242 or .R:247 or .R:260 or .R:262 or .R:264 or .R:266 or .R:269 or .R:270 or .R:273 or .R:279 or .R:294 or .R:297 or .R:298 or .R:301 or .R:305 or .R:309 or .R:311 or .R:313 or .R:314 or .R:315 or .R:318 or .R:322 or .R:343 or .R:356 or .R:368 or .R:371 or .R:372 or .R:375 or .R:376 or .R:379; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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ILE133
3.730
LEU137
4.531
MET140
3.635
TYR171
4.471
ILE174
4.340
ASN175
3.540
THR178
3.749
LEU182
4.364
ALA214
4.943
ARG217
3.733
THR218
3.616
ILE221
4.154
TYR225
3.638
LEU235
4.415
VAL239
4.105
HIS242
3.834
LEU247
4.606
LEU260
3.712
LEU262
4.346
TRP264
3.417
ALA266
3.729
LEU269
4.619
PHE270
4.803
PRO273
4.752
TYR279
4.265
ALA294
4.451
TRP297
3.508
ILE298
3.756
THR301
3.693
MET305
3.765
ILE309
4.014
PHE311
4.955
ILE313
4.837
PHE314
4.027
ILE315
4.796
LEU318
3.753
LEU322
3.709
THR343
4.947
VAL356
3.809
ALA368
3.527
PHE371
3.678
ALA372
3.508
GLY375
3.806
PHE376
4.791
PHE379
3.585
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: 2-fluoro-4-[(1R)-6-methoxy-1-methyl-2-{(1S)-1-[4-(propan-2-yl)phenyl]ethyl}-1,2,3,4-tetrahydroisoquinolin-5-yl]-6-[(2-methylpropyl)amino]phenol | Ligand Info | |||||
| Structure Description | cryo-EM structure of human Gastric inhibitory polypeptide receptor GIPR bound to tirzepatide | PDB:7RBT | ||||
| Method | Electron microscopy | Resolution | 3.08 Å | Mutation | No | [2] |
| PDB Sequence |
GQTAGELYQR
38 WERYRRECQE48 TLAAAEPPSG58 LACNGSFDMY68 VCWDYAAPNA78 TARASCPWYL 88 PWHHHVAAGF98 VLRQCGSDGQ108 WGLWRDHTQC118 ENPEKNEAFL128 DQRLILERLQ 138 VMYTVGYSLS148 LATLLLALLI158 LSLFRRLHCT168 RNYIHINLFT178 SFMLRAAAIL 188 SRDRLLPRPG198 PYLGDQALAL208 WNQALAACRT218 AQIVTQYCVG228 ANYTWLLVEG 238 VYLHSLLVLV248 GGSEEGHFRY258 YLLLGWGAPA268 LFVIPWVIVR278 YLYENTQCWE 288 RNEVKAIWWI298 IRTPILMTIL308 INFLIFIRIL318 GILLSKLRTR328 DYRLRLARST 343 LTLVPLLGVH353 EVVFAPVTEE363 QARGALRFAK373 LGFEIFLSSF383 QGFLVSVLYC 393 FINKEVQSEI403 RRGWHHCR
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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 .41Y or .41Y2 or .41Y3 or :341Y;style chemicals stick;color identity;select .R:311 or .R:314 or .R:344 or .R:347 or .R:348 or .R:352 or .R:353 or .R:355 or .R:356 or .R:379 or .R:380 or .R:381 or .R:383 or .R:384 or .R:386 or .R:387 or .R:391; 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 | Structural insights into multiplexed pharmacological actions of tirzepatide and peptide 20 at the GIP, GLP-1 or glucagon receptors. Nat Commun. 2022 Feb 25;13(1):1057. | ||||
| REF 2 | Structural determinants of dual incretin receptor agonism by tirzepatide. Proc Natl Acad Sci U S A. 2022 Mar 29;119(13):e2116506119. | ||||
| REF 3 | Structural insights into hormone recognition by the human glucose-dependent insulinotropic polypeptide receptor. Elife. 2021 Jul 13;10:e68719. | ||||
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