PPIRE06777

Target Protein Information
Protein_Name Kelch-like ECH-associated protein 1
Protein_Sequence MQPDPRPSGAGACCRFLPLQSQCPEGAGDAVMYASTECKAEVTPSQHGNRTFSYTLEDHTKQAFGIMNELRLSQQLCDVTLQVKYQDAPAAQFMAHKVVLASSSPVFKAMFTNGLREQGMEVVSIEGIHPKVMERLIEFAYTASISMGEKCVLHVMNGAVMYQIDSVVRACSDFLVQQLDPSNAIGIANFAEQIGCVELHQRAREYIYMHFGEVAKQEEFFNLSHCQLVTLISRDDLNVRCESEVFHACINWVKYDCEQRRFYVQALLRAVRCHSLTPNFLQMQLQKCEILQSDSRCKDYLVKIFEELTLHKPTQVMPCRAPKVGRLIYTAGGYFRQSLSYLEAYNPSDGTWLRLADLQVPRSGLAGCVVGGLLYAVGGRNNSPDGNTDSSALDCYNPMTNQWSPCAPMSVPRNRIGVGVIDGHIYAVGGSHGCIHHNSVERYEPERDEWHLVAPMLTRRIGVGVAVLNRLLYAVGGFDGTNRLNSAECYYPERNEWRMITAMNTIRSGAGVCVLHNCIYAAGGYDGQDQLNSVERYDVETETWTFVAPMKHRRSALGITVHQGRIYVLGGYDGHTFLDSVECYDPDTDTWSEVTRMTSGRSGVGVAVTMEPCRKQIDQQNCTC
Organism_Source Homo sapiens
Functional_Classification ubiquitin ligase adaptor
Cellular_Localization Cytoplasm
Gene_Names KEAP1
UniProt_ID Q14145
Protein-Protein Interaction Networks
Peptide Basic Information
Peptide_Name c[GDPETGE]
Peptide_Sequence DPETGE
Peptide_Length 6
Peptide_SMILES C[C@@H](O)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CC(=O)O)C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)O
Chemical_Modification None
Cyclization_Method Main chain-main chain cyclization; D1<->E7; amide bond
Linear/Cyclic Cyclic
N-terminal_Modification None
C-terminal_Modification None
Amino_Acid_Distribution
Peptide Physicochemical
Molecular_Weight 646.61
Aliphatic_Index 0.00000
Aromaticity 0.00000
Average_Rotatable_Bonds 3.16667
Charge_at_pH_7 -2.99802
Isoelectric_Point 3.42471
Number_of_Hydrogen_Bond_Acceptors 11
Number_of_Hydrogen_Bond_Donors 10
Topological_Polar_Surface_Area 332.16000
X_logP_energy -4.45500
Interaction Information
Affinity KD=160 nM
Affinity_Assay fluorescence anisotropy
PDB_ID None
Type Inhibitor
Structure
Reference Information
Document_Type Research Articles
Title Recapitulating the Binding Affinity of Nrf2 for KEAP1 in a Cyclic Heptapeptide, Guided by NMR, X-ray Crystallography, and Machine Learning.
Release_Year 2021
PMID 33683866
DOI 10.1021/jacs.0c09799