PPIRE02884
Target Protein Information
| Protein_Name | Glucagon receptor |
|---|---|
| Protein_Sequence | MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRLGKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF |
| Organism_Source | Homo sapiens |
| Functional_Classification | receptor |
| Cellular_Localization | Plasma membrane |
| Gene_Names | GCGR |
| UniProt_ID | P47871 |
| Protein-Protein Interaction Networks | |
Peptide Basic Information
| Peptide_Name | [Pla6Glu9]glucagon(6?29)amide |
|---|---|
| Peptide_Sequence | XTSEYSKYLDSRRAQDFVQWLMNT |
| Peptide_Length | 24 |
| Peptide_SMILES | CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O |
| Chemical_Modification | X1=L-3-phenyllactic acid |
| 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 | 2896.18 |
|---|---|
| Aliphatic_Index | 48.75000 |
| Aromaticity | 0.16667 |
| Average_Rotatable_Bonds | 3.95833 |
| Charge_at_pH_7 | -0.00135 |
| Isoelectric_Point | 6.54220 |
|---|---|
| Number_of_Hydrogen_Bond_Acceptors | 42 |
| Number_of_Hydrogen_Bond_Donors | 46 |
| Topological_Polar_Surface_Area | 1281.01000 |
| X_logP_energy | -13.82076 |
Interaction Information
| Affinity | IC50=12 nM |
|---|---|
| Affinity_Assay | NMR chemical shift perturbation |
| PDB_ID | None |
| Type | Affinity ligand |
| Structure | |
Reference Information
| Document_Type | Research Articles |
|---|---|
| Title | Optimization of Truncated Glucagon Peptides to Achieve Selective, High Potency, Full Antagonists. |
| Release_Year | 2021 |
| PMID | 33821647 |
| DOI | 10.1021/acs.jmedchem.0c02069 |