PPIRE06602
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 | [Arg6,D-Trp7,9,NmePhe8]-substance P(6-11) |
|---|---|
| Peptide_Sequence | RwXwLM |
| Peptide_Length | 6 |
| Peptide_SMILES | CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)O |
| Chemical_Modification | X3=N-methylphenylalanine |
| Cyclization_Method | None |
| Linear/Cyclic | Linear |
| N-terminal_Modification | Free |
| C-terminal_Modification | Free |
| Amino_Acid_Distribution | |
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Peptide Physicochemical
| Molecular_Weight | 848.03 |
|---|---|
| Aliphatic_Index | 65.00000 |
| Aromaticity | 0.33333 |
| Average_Rotatable_Bonds | 4.00000 |
| Charge_at_pH_7 | 0.99798 |
| Isoelectric_Point | 10.55000 |
|---|---|
| Number_of_Hydrogen_Bond_Acceptors | 9 |
| Number_of_Hydrogen_Bond_Donors | 12 |
| Topological_Polar_Surface_Area | 302.30000 |
| X_logP_energy | 0.96417 |
Interaction Information
| Affinity | IC50=25 uM |
|---|---|
| Affinity_Assay | colony formation assay |
| PDB_ID | None |
| Type | antagonist |
| Structure | |
Reference Information
| Document_Type | Research Articles |
|---|---|
| Title | Increased gastrin-releasing peptide (GRP)receptor expression in tumour cells confers sensitivity to [Arg6,D-Trp7,9,NmePhe8]-substance P (6-11)-induced growth inhibition. |
| Release_Year | 2003 |
| PMID | 12771999 |
| DOI | 10.1038/sj.bjc.6600957 |