General Information


DRAVP ID  DRAVPe00437

Peptide Name   EKL0P

Sequence  SLDQINVTFLDLEYEMKKLEEAIKKLEESYIDLKELGTYEYYVKWGSGK

Sequence Length  49

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=0.093±0.012 μmol/L),Inhibition of Pseudovirus(PsV) infection in 293T/ACE2 cells(IC50=0.619±0.341 μmol/L),Inhibition of Pseudovirus(PsV) infection in Caco-2 cells(IC50=0.176±0.019 μmol/L),inhibition of cell-cell fusion(IC50=0.083±0.009 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  DRAVPe00437

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  Palm

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C269H415N59O84S

Absent amino acids  CHPR

Common amino acids  E

Mass  5851.66

Pl  4.61

Basic residues  7

Acidic residues  11

Hydrophobic residues  15

Net charge  -4

Boman Index  -7814

Hydrophobicity  -61.63

Aliphatic Index  93.47

Half Life 

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

Extinction Coefficient cystines  12950

Absorbance 280nm  269.79

Polar residues  14



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