PPIRE00965

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 (Psi-12,13, Leu14)BN
Peptide_Sequence XQRLGNQWAVGHLL
Peptide_Length 14
Peptide_SMILES CC(C)C[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)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)CN)C(C)C)C(=O)O
Chemical_Modification X1=pyroglutamate
Cyclization_Method None
Linear/Cyclic Linear
N-terminal_Modification Pyroglutamate
C-terminal_Modification amide
Amino_Acid_Distribution
Peptide Physicochemical
Molecular_Weight 1548.77
Aliphatic_Index 111.42857
Aromaticity 0.07143
Average_Rotatable_Bonds 3.57143
Charge_at_pH_7 1.08889
Isoelectric_Point 10.55176
Number_of_Hydrogen_Bond_Acceptors 20
Number_of_Hydrogen_Bond_Donors 23
Topological_Polar_Surface_Area 677.26000
X_logP_energy -6.23143
Interaction Information
Affinity IC50=90 nM
Affinity_Assay radioligand binding assay
PDB_ID None
Type antagonist
Structure
Reference Information
Document_Type Research Articles
Title Small cell lung cancer bombesin receptors are antagonized by reduced peptide bond analogues.
Release_Year 1989
PMID 2536883
DOI 10.1016/0024-3205(89)90231-2