PPIRE05808

Target Protein Information
Protein_Name Furin
Protein_Sequence MELRPWLLWVVAATGTLVLLAADAQGQKVFTNTWAVRIPGGPAVANSVARKHGFLNLGQIFGDYYHFWHRGVTKRSLSPHRPRHSRLQREPQVQWLEQQVAKRRTKRDVYQEPTDPKFPQQWYLSGVTQRDLNVKAAWAQGYTGHGIVVSILDDGIEKNHPDLAGNYDPGASFDVNDQDPDPQPRYTQMNDNRHGTRCAGEVAAVANNGVCGVGVAYNARIGGVRMLDGEVTDAVEARSLGLNPNHIHIYSASWGPEDDGKTVDGPARLAEEAFFRGVSQGRGGLGSIFVWASGNGGREHDSCNCDGYTNSIYTLSISSATQFGNVPWYSEACSSTLATTYSSGNQNEKQIVTTDLRQKCTESHTGTSASAPLAAGIIALTLEANKNLTWRDMQHLVVQTSKPAHLNANDWATNGVGRKVSHSYGYGLLDAGAMVALAQNWTTVAPQRKCIIDILTEPKDIGKRLEVRKTVTACLGEPNHITRLEHAQARLTLSYNRRGDLAIHLVSPMGTRSTLLAARPHDYSADGFNDWAFMTTHSWDEDPSGEWVLEIENTSEANNYGTLTKFTLVLYGTAPEGLPVPPESSGCKTLTSSQACVVCEEGFSLHQKSCVQHCPPGFAPQVLDTHYSTENDVETIRASVCAPCHASCATCQGPALTDCLSCPSHASLDPVEQTCSRQSQSSRESPPQQQPPRLPPEVEAGQRLRAGLLPSHLPEVVAGLSCAFIVLVFVTVFLVLQLRSGFSFRGVKVYTMDRGLISYKGLPPEAWQEECPSDSEEDEGRGERTAFIKDQSAL
Organism_Source Homo sapiens
Functional_Classification proprotein convertases
Cellular_Localization Cytoplasm
Gene_Names FURIN
UniProt_ID P09958
Protein-Protein Interaction Networks
Peptide Basic Information
Peptide_Name inhibitor 1
Peptide_Sequence RRRVR
Peptide_Length 5
Peptide_SMILES CC(C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O
Chemical_Modification None
Cyclization_Method None
Linear/Cyclic Linear
N-terminal_Modification Free
C-terminal_Modification 4-amidinobenzylamide
Amino_Acid_Distribution
Peptide Physicochemical
Molecular_Weight 741.90
Aliphatic_Index 58.00000
Aromaticity 0.00000
Average_Rotatable_Bonds 5.20000
Charge_at_pH_7 3.99797
Isoelectric_Point 12.97715
Number_of_Hydrogen_Bond_Acceptors 10
Number_of_Hydrogen_Bond_Donors 18
Topological_Polar_Surface_Area 427.32000
X_logP_energy -4.95342
Interaction Information
Affinity KD=0.0337 nM
Affinity_Assay Enzyme Inhibition Kinetics
PDB_ID 6EQX
Type Inhibitor
Structure
Reference Information
Document_Type Research Articles
Title Design, Synthesis, and Characterization of Macrocyclic Inhibitors of the Proprotein Convertase Furin.
Release_Year 2018
PMID 30680958
DOI 10.1002/cmdc.201800807