PPIRE10022
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 | J-G-Abz4-QWAVGHLM-NH2 |
|---|---|
| Peptide_Sequence | GXQWAVGHLM |
| Peptide_Length | 10 |
| Peptide_SMILES | CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=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)CNC(=O)CNC(=O)CN)C(C)C)C(=O)O |
| Chemical_Modification | X3=4-aminobenzyl; J1=4-aminophenylalanine |
| Cyclization_Method | None |
| Linear/Cyclic | Linear |
| N-terminal_Modification | Do3A-Ch2Co |
| C-terminal_Modification | amide |
| Amino_Acid_Distribution | |
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Peptide Physicochemical
| Molecular_Weight | 1112.27 |
|---|---|
| Aliphatic_Index | 70.90909 |
| Aromaticity | 0.09091 |
| Average_Rotatable_Bonds | 3.09091 |
| Charge_at_pH_7 | 0.08889 |
| Isoelectric_Point | 7.55032 |
|---|---|
| Number_of_Hydrogen_Bond_Acceptors | 15 |
| Number_of_Hydrogen_Bond_Donors | 15 |
| Topological_Polar_Surface_Area | 441.88000 |
| X_logP_energy | -3.79770 |
Interaction Information
| Affinity | IC50=18 nM |
|---|---|
| Affinity_Assay | Enzyme Inhibition Kinetics |
| PDB_ID | None |
| Type | Agonist |
| Structure | |
Reference Information
| Document_Type | Research Articles |
|---|---|
| Title | In Vitro Mouse and Human Serum Stability of a Heterobivalent Dual-Target Probe That Has Strong Affinity to Gastrin-Releasing Peptide and Neuropeptide Y1 Receptors on Tumor Cells. |
| Release_Year | 2017 |
| PMID | 28186846 |
| DOI | 10.1089/cbr.2016.2136 |