PPIRE06015
Target Protein Information
| Protein_Name | Melanocortin receptor 4 |
|---|---|
| Protein_Sequence | MVNSTHRGMHTSLHLWNRSSYRLHSNASESLGKGYSDGGCYEQLFVSPEVFVTLGVISLLENILVIVAIAKNKNLHSPMYFFICSLAVADMLVSVSNGSETIVITLLNSTDTDAQSFTVNIDNVIDSVICSSLLASICSLLSIAVDRYFTIFYALQYHNIMTVKRVGIIISCIWAACTVSGILFIIYSDSSAVIICLITMFFTMLALMASLYVHMFLMARLHIKRIAVLPGTGAIRQGANMKGAITLTILIGVFVVCWAPFFLHLIFYISCPQNPYCVCFMSHFNLYLILIMCNSIIDPLIYALRSQELRKTFKEIICCYPLGGLCDLSSRY |
| Organism_Source | Homo sapiens |
| Functional_Classification | G protein-coupled receptor |
| Cellular_Localization | Plasma membrane |
| Gene_Names | MC4R |
| UniProt_ID | P32245 |
| Protein-Protein Interaction Networks | |
Peptide Basic Information
| Peptide_Name | MBP5 |
|---|---|
| Peptide_Sequence | DXRWK |
| Peptide_Length | 5 |
| Peptide_SMILES | N=C(N)NCCC[C@H](NC(=O)CNC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)O |
| Chemical_Modification | X2=D-(2')naphthylalanine |
| Cyclization_Method | Side chain-side chain cyclization; D1<->K5; amide bond |
| Linear/Cyclic | Cyclic |
| N-terminal_Modification | Free |
| C-terminal_Modification | amide |
| Amino_Acid_Distribution | |
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Peptide Physicochemical
| Molecular_Weight | 660.73 |
|---|---|
| Aliphatic_Index | 0.00000 |
| Aromaticity | 0.20000 |
| Average_Rotatable_Bonds | 4.20000 |
| Charge_at_pH_7 | 0.99813 |
| Isoelectric_Point | 9.69502 |
|---|---|
| Number_of_Hydrogen_Bond_Acceptors | 9 |
| Number_of_Hydrogen_Bond_Donors | 12 |
| Topological_Polar_Surface_Area | 320.73000 |
| X_logP_energy | -2.44013 |
Interaction Information
| Affinity | Ki=0.28 nM |
|---|---|
| Affinity_Assay | competitive radioligand binding assay |
| PDB_ID | None |
| Type | antagonist |
| Structure | |
Reference Information
| Document_Type | Research Articles |
|---|---|
| Title | Selective, high affinity peptide antagonists of alpha-melanotropin action at human melanocortin receptor 4: their synthesis and biological evaluation in vitro. |
| Release_Year | 2001 |
| PMID | 11606131 |
| DOI | 10.1021/jm010165y |