PPIRE08431
Target Protein Information
| Protein_Name | Gastrin-releasing peptide receptor |
|---|---|
| Protein_Sequence | MALNDCFLLNLEVDHFMHCNISSHSADLPVNDDWSHPGILYVIPAVYGVIILIGLIGNITLIKIFCTVKSMRNVPNLFISSLALGDLLLLITCAPVDASRYLADRWLFGRIGCKLIPFIQLTSVGVSVFTLTALSADRYKAIVRPMDIQASHALMKICLKAAFIWIISMLLAIPEAVFSDLHPFHEESTNQTFISCAPYPHSNELHPKIHSMASFLVFYVIPLSIISVYYYFIAKNLIQSAYNLPVEGNIHVKKQIESRKRLAKTVLVFVGLFAFCWLPNHVIYLYRSYHYSEVDTSMLHFVTSICARLLAFTNSCVNPFALYLLSKSFRKQFNTQLLCCQPGLIIRSHSTGRSTTCMTSLKSTNPSVATFSLINGNICHERYV |
| Organism_Source | Homo sapiens |
| Functional_Classification | G protein-coupled receptor |
| Cellular_Localization | Plasma membrane |
| Gene_Names | GRPR |
| UniProt_ID | P30550 |
| Protein-Protein Interaction Networks | |
Peptide Basic Information
| Peptide_Name | NODAGA-AR |
|---|---|
| Peptide_Sequence | fQWAVGHXL |
| Peptide_Length | 9 |
| Peptide_SMILES | CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)C(=O)O |
| Chemical_Modification | X8=statine |
| Cyclization_Method | None |
| Linear/Cyclic | Linear |
| N-terminal_Modification | Peg4 |
| C-terminal_Modification | amide |
| Amino_Acid_Distribution | |
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Peptide Physicochemical
| Molecular_Weight | 1014.15 |
|---|---|
| Aliphatic_Index | 86.66667 |
| Aromaticity | 0.22222 |
| Average_Rotatable_Bonds | 3.22222 |
| Charge_at_pH_7 | 0.08889 |
| Isoelectric_Point | 7.55032 |
|---|---|
| Number_of_Hydrogen_Bond_Acceptors | 12 |
| Number_of_Hydrogen_Bond_Donors | 13 |
| Topological_Polar_Surface_Area | 383.68000 |
| X_logP_energy | -1.54050 |
Interaction Information
| Affinity | IC50=25 nM |
|---|---|
| Affinity_Assay | in vitro autoradiography |
| PDB_ID | None |
| Type | antagonist |
| Structure | |
Reference Information
| Document_Type | Research Articles |
|---|---|
| Title | Bombesin antagonist-based radioligands for translational nuclear imaging of gastrin-releasing peptide receptor-positive tumors. |
| Release_Year | 2011 |
| PMID | 22080443 |
| DOI | 10.2967/jnumed.111.094375 |