General Information


DRAVP ID  DRAVPe00442

Peptide Name   EK1-C16

Sequence  SLDQINVTFLDLEYEMKKLEEAIKKLEESYIDLKELGSGSG

Sequence Length  41

UniProt ID  No entry found

Taxon ID  None

Source  Synthetic construct(derived from EK1)

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  SARS-CoV-2,SARS-CoV,MERS-CoV,HCoV-OC43

Assay  pseudovirus inhibition assay

Activity 

  • [Ref.35336956]SARS-CoV-2 WT:inhibition of pseudovirus (PsV) infection in Caco2 cells(IC50=0.48 μM);
  • SARS-CoV-2 Alpha:inhibition of pseudovirus (PsV) infection(IC50=0.19 μM);
  • SARS-CoV-2 Beta:inhibition of pseudovirus (PsV) infection(IC50=0.43 μM);
  • SARS-CoV-2 Gamma:inhibition of pseudovirus (PsV) infection(IC50=0.26 μM);
  • SARS-CoV-2 Delta:inhibition of pseudovirus (PsV) infection(IC50=0.11 μM);
  • SARS-CoV-2 Omicron:inhibition of pseudovirus (PsV) infection(IC50=0.23 μM);inhibition of authentic infection in Vero-E6-TMPRSS-2 cells(IC50=0.75 μM);
  • SARS-CoV:inhibition of pseudovirus (PsV) infection(IC50=0.17 μM);
  • SARSr-CoV WIV1:inhibition of pseudovirus (PsV) infection(IC50=0.15 μM);
  • SARSr-CoV Rs3367:inhibition of pseudovirus (PsV) infection(IC50=0.3 μM);
  • MERS-CoV:inhibition of pseudovirus (PsV) infection in Caco2 cells(IC50=0.10 μM);inhibition of cell-cell fusion(IC50=0.012 μM);
  • HCoV-OC43:inhibition of authentic infection in RD cells(IC50=0.07 μM);inhibition of cell-cell fusion(IC50=0.01 μM).

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

Cytotoxicity 

  • [Ref.35336956]showed no significant cytotoxicity against RD cells at the concentration of 5 μM.

Binding Target  membrane

Mechanism  The 6-HB structure formed by HR1 and HR2 regions in the S2 subunit of HCoVs plays a key role during the viral membrane fusion process,peptides derived from the HR2 regions can competitively inhibit viral 6-HB formation, thereby preventing viral fusion and entry into host cells.



Structure Information


PDB ID  None

Predicted Structure Download  No predicted structure available

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  PEG4-C16(palmitic acid)

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C208H336N48O71S

Absent amino acids  CHPRW

Common amino acids  EL

Mass  4677.29

Pl  4.36

Basic residues  5

Acidic residues  10

Hydrophobic residues  13

Net charge  -5

Boman Index  -6701

Hydrophobicity  -44.88

Aliphatic Index  104.63

Half Life 

  •     Mammalian:1.9 hour
  •     Yeast:>20 hour
  •     E.coli:>10 hour

Extinction Coefficient cystines  2980

Absorbance 280nm  74.5

Polar residues  11



Literature Information


Literature 1

Title   A Palmitic Acid-Conjugated, Peptide-Based pan-CoV Fusion Inhibitor Potently Inhibits Infection of SARS-CoV-2 Omicron and Other Variants of Concern.

Pubmed ID   35336956

Reference   Viruses. 2022 Mar 6;14(3):549.

Author   Lan Q, Chan JF, Xu W, Wang L, Jiao F, Zhang G, Pu J, Zhou J, Xia S, Lu L, Yuen KY, Jiang S, Wang Q.

DOI   10.3390/v14030549