General Information


DRAVP ID  DRAVPe02312

Peptide Name   5-Link

Sequence  YGRKKRRQRRRGSGIEPHDWTKNITCKIOQIIHDFVDK

Sequence Length  38

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  Not Available

Activity 

  • [Ref:23962564]EBOV:IC50=15 microM

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

Cytotoxicity 

  • [Ref:23962564]Vero cells incubated with concentrations of 5-Link exceeding 15 microM showed signs of toxicity by visual inspection, which prevented assessment of antiviral activity at higher concentra

Binding Target  Glycoprotein.

Mechanism  5-Link displayed antiviral activity against vesicular stomatitis virus particles containing the Ebola virus glycoprotein (VSV-GP), inhibiting infection at concentrations below 15 microM. It exhibited broad antiviral activity against both VSV-GP and VSV-G at lower concentrations, but induced toxicity in Vero cells at concentrations exceeding 15 microM, limiting further assessment. The peptide's specificity towards VSV-GP over VSV-G suggests a mechanism involving interference with viral entry, similar to its action against VSV-GP particles, thereby inhibiting Ebola virus infection. This indicates 5-Link's potential as a therapeutic agent targeting viral entry mediated by the Ebola virus glycoprotein.



Structure Information


PDB ID  None

Predicted Structure Download 

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  Acetylation

Other Modification  The peptide sequence features N-terminal acetylation (Ac-), which enhances stability by protecting it from enzymatic degradation and making it more resistant to proteolysis. To further enhance the peptide's structure and function, alpha-helical stabilization can be introduced through covalent side chain-side chain cross-links. This is achieved by linking Cys at position 26 (C) with another suitable residue i.e., Ornithine (Orn) Ornithine (Orn) at position 29 (i.e., i and i+3). These cross-links

Stereochemistry  L



Physicochemical Information


Formula  C210H343N71O55S1

Absent amino acids  ALMU

Common amino acids  R

Mass  4774.54

Pl  10.6

Basic residues  11

Acidic residues  4

Hydrophobic residues  8

Net charge  7

Boman Index  None

Hydrophobicity  -1.384

Aliphatic Index  58.95

Half Life 

  •     Mammalian:2.8hours
  •     Yeast:10min
  •     E.coli:2min

Extinction Coefficient cystines  6990

Absorbance 280nm  1.464

Polar residues  25



Literature Information


Literature 1

Title   C-peptide inhibitors of Ebola virus glycoprotein-mediated cell entry: effects of conjugation to cholesterol and side chain-side chain crosslinking

Pubmed ID   23962564

Reference   Bioorg Med Chem Lett. 2013;23(19):5356-60.

Author   Higgins CD, Koellhoffer JF, Chandran K

DOI   10.1016/j.bmcl.2013.07.056