PPIRE13100

Target Protein Information
Protein_Name Glucagon receptor
Protein_Sequence MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRLGKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF
Organism_Source Homo sapiens
Functional_Classification G protein-coupled receptor
Cellular_Localization Plasma membrane
Gene_Names GCGR
UniProt_ID P47871
Protein-Protein Interaction Networks
Peptide Basic Information
Peptide_Name BI-32169 methyl ester
Peptide_Sequence GLPPPCPSDWGWPNTIPAC
Peptide_Length 19
Peptide_SMILES CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)CN)[C@@H](C)O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CS)C(=O)O
Chemical_Modification None
Cyclization_Method Main chain-side chain cyclization; G1<->D9; amide bond; Side chain-side chain cyclization; C6<->C19; disulfide bond
Linear/Cyclic Cyclic
N-terminal_Modification Free
C-terminal_Modification methyl esterification
Amino_Acid_Distribution
Peptide Physicochemical
Molecular_Weight 2008.30
Aliphatic_Index 46.31579
Aromaticity 0.10526
Average_Rotatable_Bonds 2.47368
Charge_at_pH_7 -1.12552
Isoelectric_Point 3.74996
Number_of_Hydrogen_Bond_Acceptors 26
Number_of_Hydrogen_Bond_Donors 22
Topological_Polar_Surface_Area 686.81000
X_logP_energy -5.43240
Interaction Information
Affinity IC50=320 nM
Affinity_Assay functional cell-based assay
PDB_ID None
Type antagonist
Structure
Reference Information
Document_Type Research Articles
Title BI-32169, a bicyclic 19-peptide with strong glucagon receptor antagonist activity from Streptomyces sp.
Release_Year 2004
PMID 15387654
DOI 10.1021/np040093o