PPIRE04560

Target Protein Information
Protein_Name Neutrophil elastase
Protein_Sequence MTLGRRLACLFLACVLPALLLGGTALASEIVGGRRARPHAWPFMVSLQLRGGHFCGATLIAPNFVMSAAHCVANVNVRAVRVVLGAHNLSRREPTRQVFAVQRIFENGYDPVNLLNDIVILQLNGSATINANVQVAQLPAQGRRLGNGVQCLAMGWGLLGRNRGIASVLQELNVTVVTSLCRRSNVCTLVRGRQAGVCFGDSGSPLVCNGLIHGIASFVRGGCASGLYPDAFAPVAQFVNWIDSIIQRSEDNPCPHPRDPDPASRTH
Organism_Source Homo sapiens
Functional_Classification serine proteases
Cellular_Localization Extracellular
Gene_Names ELANE
UniProt_ID P08246
Protein-Protein Interaction Networks
Peptide Basic Information
Peptide_Name 22a
Peptide_Sequence VXX
Peptide_Length 3
Peptide_SMILES CC(C)[C@H](N)C(=O)NCC(=O)NCC(=O)O
Chemical_Modification X2=N-(2,3-dihydro-1H-inden-2-yl)glycine; X3=a,a-difluoromethylene ketone derivative of L-phenylalanine
Cyclization_Method None
Linear/Cyclic Linear
N-terminal_Modification P-[P-Cl(C6H4)So2Nhco](C6H4)Co
C-terminal_Modification ethyl ester
Amino_Acid_Distribution
Peptide Physicochemical
Molecular_Weight 231.25
Aliphatic_Index 96.66667
Aromaticity 0.00000
Average_Rotatable_Bonds 2.00000
Charge_at_pH_7 -0.00202
Isoelectric_Point 6.10000
Number_of_Hydrogen_Bond_Acceptors 4
Number_of_Hydrogen_Bond_Donors 4
Topological_Polar_Surface_Area 121.52000
X_logP_energy -1.71330
Interaction Information
Affinity IC50=5 uM
Affinity_Assay Enzyme Inhibition Kinetics
PDB_ID None
Type Inhibitor
Structure
Reference Information
Document_Type Research Articles
Title Fluorocyclopropyl quinolones. 1. Synthesis and structure-activity relationships of 1-(2-fluorocyclopropyl)-3-pyridonecarboxylic acid antibacterial agents.
Release_Year 1992
PMID 8230135
DOI 10.1021/jm00074a027