Target Binding Site Detail
Target General Information | Top | ||||
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Target ID | T36075 | Target Info | |||
Target Name | Glucagon-like peptide 1 receptor (GLP1R) | ||||
Synonyms | GLP-1R; GLP-1-R; GLP-1 receptor | ||||
Target Type | Successful Target | ||||
Gene Name | GLP1R | ||||
Biochemical Class | GPCR secretin | ||||
UniProt ID |
Ligand General Information | Top | ||||
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Ligand Name | Alpha-Aminoisobutyric Acid | Ligand Info | |||
Canonical SMILES | CC(C)(C(=O)O)N | ||||
InChI | 1S/C4H9NO2/c1-4(2,5)3(6)7/h5H2,1-2H3,(H,6,7) | ||||
InChIKey | FUOOLUPWFVMBKG-UHFFFAOYSA-N | ||||
PubChem Compound ID | 6119 |
Drug Binding Sites of Target | Top | |||||
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PDB ID: 7VBH Cryo-EM structure of the GIPR/GLP-1R/GCGR triagonist peptide 20-bound human GLP-1R-Gs complex | ||||||
Method | Electron microscopy | Resolution | 3.00 Å | Mutation | Yes | [1] |
PDB Sequence |
ATVSLWETVQ
37 KWREYRRQCQ47 RSLTEDPPPA57 TDLFCNRTFD67 EYACWPDGEP77 GSFVNVSCPW 87 YLPWASSVPQ97 GHVYRFCTAE107 GLWLQKDNSS117 LPWRDLSECE127 ESEEQLLFLY 145 IIYTVGYALS155 FSALVIASAI165 LLGFRHLHCT175 RNYIHLNLFA185 SFILRALSVF 195 IKDAALKWMY205 STAAQQHQWD215 GLLSYQDSLS225 CRLVFLLMQY235 CVAANYYWLL 245 VEGVYLYTLL255 AFSVLSEQWI265 FRLYVSIGWG275 VPLLFVVPWG285 IVKYLYEDEG 295 CWTRNSNMNY305 WLIIRLPILF315 AIGVNFLIFV325 RVICIVVSKL335 KADIKCRLAK 351 STLTLIPLLG361 THEVIFAFVM371 DEHARGTLRF381 IKLFTELSFT391 SFQGLMVAIL 401 YCFVNNEVQL411 EFRKSWERWR421 LE
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PDB ID: 7KI0 Semaglutide-bound Glucagon-Like Peptide-1 (GLP-1) Receptor in Complex with Gs protein | ||||||
Method | Electron microscopy | Resolution | 2.50 Å | Mutation | No | [2] |
PDB Sequence |
TVSLWETVQK
38 WREYRRQCQR48 SLTEDPPPAT58 DLFCNRTFDE68 YACWPDGEPG78 SFVNVSCPWY 88 LPWASSVPQG98 HVYRFCTAEG108 LWLQKDNSSL118 PWRDLSECEE128 SPEEQLLFLY 145 IIYTVGYALS155 FSALVIASAI165 LLGFRHLHCT175 RNYIHLNLFA185 SFILRALSVF 195 IKDAALKWMY205 STAAQQHQWD215 GLLSYQDSLS225 CRLVFLLMQY235 CVAANYYWLL 245 VEGVYLYTLL255 AFSVFSEQWI265 FRLYVSIGWG275 VPLLFVVPWG285 IVKYLYEDEG 295 CWTRNSNMNY305 WLIIRLPILF315 AIGVNFLIFV325 RVICIVVSKL335 KANLDIKCRL 349 AKSTLTLIPL359 LGTHEVIFAF369 VMDEHARGTL379 RFIKLFTELS389 FTSFQGLMVA 399 ILYCFVNNEV409 QLEFRKSWER419 WRLE
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References | Top | ||||
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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 | Structure and dynamics of semaglutide- and taspoglutide-bound GLP-1R-Gs complexes. Cell Rep. 2021 Jul 13;36(2):109374. |
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