General Information


DRAVP ID  DRAVPe02204

Peptide Name   Peptidyl chloromethylketone

Sequence  RVKRCMK

Sequence Length  7

UniProt ID  No entry found

Taxon ID  None

Source  Synthetic construct

Validation   Experimentally Validated



Origin Information


Gene Name/ID  Not Available

GenBank  Not Available

Amino Acid position  Not Available

Domain Accession ID  Not Available

Nucleotide sequence ID  Not Available

Molecular Type  Not Available

Chromosomal Position  Not Available



Activity Information


Target Organism  EBOV

Assay  Endoproteolytic Cleavage Inhibition Assay. ≥90% (HPLC)

Activity 

  • [Ref:9576958]EBOV:IC50=25 microM or 80 microM

Hemolytic Activity  No hemolysis information or data found in the reference(s) presented in this entry

Cytotoxicity  No cytotoxicity information found in the reference(s) presented

Binding Target  Glycoprotein.

Mechanism  Peptidyl chloromethylketones, exemplified by decRVKR-cmk, function as potent inhibitors of the endoproteolytic cleavage of the Ebola virus glycoprotein. They operate by obstructing the cleavage of the glycoprotein specifically at a multibasic amino acid motif situated between positions 497 and 501 of the ORF. This cleavage is essential for the glycoprotein's maturation into its functional state. By impeding this cleavage process, peptidyl chloromethylketones hinder the glycoprotein's transformation into its mature form, thereby disrupting the viral replication cycle and potentially diminishing the virus's infectivity.



Structure Information


PDB ID  None

Predicted Structure Download 

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  Free

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C37H73N15O8S2

Absent amino acids  ANDQEGHILFPSTWYOU

Common amino acids  RK

Mass  920.2

Pl  11.01

Basic residues  4

Acidic residues  0

Hydrophobic residues  3

Net charge  4

Boman Index  4.75

Hydrophobicity  -1.171

Aliphatic Index  41.43

Half Life 

  •     Mammalian:1 hours
  •     Yeast:2 min
  •     E.coli:2 mins

Extinction Coefficient cystines  0

Absorbance 280nm  0

Polar residues  0



Literature Information


Literature 1

Title   Processing of the Ebola virus glycoprotein by the proprotein convertase furin

Pubmed ID   9576958

Reference   Proc Natl Acad Sci U S A. 1998;95(10):5762-7. 

Author   Volchkov VE, Feldmann H, Volchkova VA, et al.

DOI   10.1073/pnas.95.10.5762