General Information


DRAVP ID  DRAVPe00440

Peptide Name   EKL3P

Sequence  LDLEYEMKKLEEAIKKLEESYIDLKELGTYEYYVKWGSGK

Sequence Length  40

UniProt ID  No entry found

Source  Synthetic construct(derived from EK1)



Activity Information


Target Organism  SARS-CoV-2

Assay 

Activity 

  • [Ref.34367893]SARS-CoV-2:Inhibition of Pseudovirus(PsV) infection in Huh-7 cells(IC50=3.987±0.682 μmol/L),Inhibition of Pseudovirus(PsV) infection in 293T/ACE2 cells(IC50>5 μmol/L),Inhibition of Pseudovirus(PsV) infection in Caco-2 cells(IC50=2.214±0.371 μmol/L),inhibition of cell-cell fusion(IC50=0.193±0.021 μmol/L).

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  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  DRAVPe00440

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  Palm

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C223H344N48O69S

Absent amino acids  CFHNPQR

Common amino acids  E

Mass  4833.52

Pl  4.76

Basic residues  7

Acidic residues  10

Hydrophobic residues  11

Net charge  -3

Boman Index  -6813

Hydrophobicity  -83.75

Aliphatic Index  87.75

Half Life 

  •     Mammalian:5.5 hour
  •     Yeast:3 min
  •     E.coli:2 min

Extinction Coefficient cystines  12950

Absorbance 280nm  332.05

Polar residues  11



Literature Information


Literature 1

Title   A highly potent and stable pan-coronavirus fusion inhibitor as a candidate prophylactic and therapeutic for COVID-19 and other coronavirus diseases.

Pubmed ID   34367893

Reference   Acta Pharm Sin B. 2021 Aug 2.

Author   Zhou J, Xu W, Liu Z, Wang C, Xia S, Lan Q, Cai Y, Su S, Pu J, Xing L, Xie Y, Lu L, Jiang S, Wang Q.

DOI   10.1016/j.apsb.2021.07.026