DRAVP ID  DRAVPe02308

Peptide Name   1-Chol

Sequence  KKKKGSGIEPHDWTKNITDKIDQIIHDFVDK

Sequence Length  32

UniProt ID  No entry found

Taxon ID  None

Source  Synthetic construct

Validation   Experimentally Validated

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

Target Organism  EBOV

Assay  Not Available

Activity 

• [Ref:23962564]EBOV:IC50=50 microM

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

Cytotoxicity 

• [Ref:23962564]At certain concentrations, 1-Chol, a cholesterol-conjugated peptide inhibitor, demonstrates only a slight cell toxicity of approximately 20%, indicating a low level of toxicity within th

Binding Target  Glycoprotein.

Mechanism  1-Chol, a cholesterol-conjugated C-peptide inhibitor, disrupts Ebola virus cell entry by targeting the glycoprotein-mediated fusion process. Specifically, it binds to the GP2 C-heptad repeat region (CHR), hindering the formation of the six-helix bundle crucial for membrane fusion. Effective at a concentration of 40 microM, 1-Chol's cholesterol conjugation enhances its alpha-helical structure independently of concentration, contributing to its broad inhibitory activity against Ebola virus. The combined peptide and cholesterol components of 1-Chol play a vital role in its inhibition of viral entry

PDB ID  None

Predicted Structure Download 

Linear/Cyclic  Linear

N-terminal Modification  cholesterylation

C-terminal Modification  Free

Other Modification  In the peptide sequence, the cysteine residue at position 1 is modified with a cholesterol (Chol) moiety. This HIV-1 C-peptide conjugated to cholesterol contain covalent side chain-side chain crosslinks to promote an alpha-helical conformation. The cholesterol-conjugated C-peptides proved to be potent inhibitors of Ebola virus glycoprotein (GP)-mediated cell entry (~10^3-fold reduction in infection at 40 microM)

Stereochemistry  L

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