PPIRE07460
Target Protein Information
| Protein_Name | Cholecystokinin receptor type A |
|---|---|
| Protein_Sequence | MSHSPARQHLVESSRMDVVDSLLMNGSNITPPCELGLENETLFCLDQPQPSKEWQSALQILLYSIIFLLSVLGNTLVITVLIRNKRMRTVTNIFLLSLAVSDLMLCLFCMPFNLIPNLLKDFIFGSAVCKTTTYFMGTSVSVSTFNLVAISLERYGAICRPLQSRVWQTKSHALKVIAATWCLSFTIMTPYPIYSNLVPFTKNNNQTANMCRFLLPSDAMQQSWQTFLLLILFLLPGIVMVVAYGLISLELYQGIKFDASQKKSAKEKKPSTGSSTRYEDSDGCYLQKSRPPRKLELQQLSSGSGGSRLNRIRSSSSAANLIAKKRVIRMLIVIVVLFFLCWMPIFSANAWRAYDTVSAEKHLSGTPISFILLLSYTSSCVNPIIYCFMNKRFRLGFMATFPCCPNPGPPGVRGEVGEEEDGRTIRALLSRYSYSHMSTSAPPP |
| Organism_Source | Rattus norvegicus |
| Functional_Classification | G protein-coupled receptor |
| Cellular_Localization | Plasma membrane |
| Gene_Names | Cckar |
| UniProt_ID | P30551 |
| Protein-Protein Interaction Networks | |
Peptide Basic Information
| Peptide_Name | DOTA-[Nle]-cCCK |
|---|---|
| Peptide_Sequence | XEXXDFK |
| Peptide_Length | 7 |
| Peptide_SMILES | NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)CN)C(=O)O |
| Chemical_Modification | X1=norleucine; X4=norleucine |
| Cyclization_Method | Side chain-side chain cyclization; E2<->K7; amide bond |
| Linear/Cyclic | Cyclic |
| N-terminal_Modification | Dota |
| C-terminal_Modification | amide |
| Amino_Acid_Distribution | |
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Peptide Physicochemical
| Molecular_Weight | 708.73 |
|---|---|
| Aliphatic_Index | 0.00000 |
| Aromaticity | 0.14286 |
| Average_Rotatable_Bonds | 3.42857 |
| Charge_at_pH_7 | -1.00009 |
| Isoelectric_Point | 4.18441 |
|---|---|
| Number_of_Hydrogen_Bond_Acceptors | 11 |
| Number_of_Hydrogen_Bond_Donors | 11 |
| Topological_Polar_Surface_Area | 338.54000 |
| X_logP_energy | -4.08750 |
Interaction Information
| Affinity | IC50=1.7 nM |
|---|---|
| Affinity_Assay | competitive radioligand binding assay |
| PDB_ID | None |
| Type | antagonist |
| Structure | |
Reference Information
| Document_Type | Research Articles |
|---|---|
| Title | An assessment tumor targeting ability of (177)Lu labeled cyclic CCK analogue peptide by binding with cholecystokinin receptor. |
| Release_Year | 2016 |
| PMID | 27430985 |
| DOI | 10.1016/j.jphs.2016.06.006 |