PPIRE14274
Target Protein Information
| Protein_Name | Glucagon-like peptide 1 receptor |
|---|---|
| Protein_Sequence | MAGAPGPLRLALLLLGMVGRAGPRPQGATVSLWETVQKWREYRRQCQRSLTEDPPPATDLFCNRTFDEYACWPDGEPGSFVNVSCPWYLPWASSVPQGHVYRFCTAEGLWLQKDNSSLPWRDLSECEESKRGERSSPEEQLLFLYIIYTVGYALSFSALVIASAILLGFRHLHCTRNYIHLNLFASFILRALSVFIKDAALKWMYSTAAQQHQWDGLLSYQDSLSCRLVFLLMQYCVAANYYWLLVEGVYLYTLLAFSVLSEQWIFRLYVSIGWGVPLLFVVPWGIVKYLYEDEGCWTRNSNMNYWLIIRLPILFAIGVNFLIFVRVICIVVSKLKANLMCKTDIKCRLAKSTLTLIPLLGTHEVIFAFVMDEHARGTLRFIKLFTELSFTSFQGLMVAILYCFVNNEVQLEFRKSWERWRLEHLHIQRDSSMKPLKCPTSSLSSGATAGSSMYTATCQASCS |
| Organism_Source | Homo sapiens |
| Functional_Classification | G protein-coupled receptor |
| Cellular_Localization | Plasma membrane |
| Gene_Names | GLP1R |
| UniProt_ID | P43220 |
| Protein-Protein Interaction Networks | |
Peptide Basic Information
| Peptide_Name | [Lys27(Ahx-DOTA-natGa)NH2]Ex(9-39) |
|---|---|
| Peptide_Sequence | DLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS |
| Peptide_Length | 31 |
| Peptide_SMILES | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)O |
| Chemical_Modification | X19=Ahx-DOTA-natGa |
| Cyclization_Method | None |
| Linear/Cyclic | Linear |
| N-terminal_Modification | Free |
| C-terminal_Modification | amide |
| Amino_Acid_Distribution | |
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Peptide Physicochemical
| Molecular_Weight | 3299.66 |
|---|---|
| Aliphatic_Index | 66.12903 |
| Aromaticity | 0.06452 |
| Average_Rotatable_Bonds | 3.35484 |
| Charge_at_pH_7 | -2.99477 |
| Isoelectric_Point | 3.98690 |
|---|---|
| Number_of_Hydrogen_Bond_Acceptors | 46 |
| Number_of_Hydrogen_Bond_Donors | 44 |
| Topological_Polar_Surface_Area | 1358.47000 |
| X_logP_energy | -14.47103 |
Interaction Information
| Affinity | IC50=137.2 nM |
|---|---|
| Affinity_Assay | Enzyme Inhibition Kinetics |
| PDB_ID | None |
| Type | antagonist |
| Structure | |
Reference Information
| Document_Type | Research Articles |
|---|---|
| Title | Approaches to Improve the Pharmacokinetics of Radiolabeled Glucagon-Like Peptide-1 Receptor Ligands Using Antagonistic Tracers. |
| Release_Year | 2016 |
| PMID | 27127218 |
| DOI | 10.2967/jnumed.115.168948 |