DRAVP ID  DRAVPe00407

Peptide Name   EK1C4

Sequence  SLDQINVTFLDLEYEMKKLEEAIKKLEESYIDLKELGSGSG

Sequence Length  41

UniProt ID  No entry found

Source  Synthetic construct(derived from EK1)

Target Organism  SARS-CoV-2,SARS-CoV,MERS-CoV,HCoV-OC43,HCoV-229E

Assay  pseudovirus inhibition assay

Activity 

• [Ref.35087243]SARS-CoV-2 Omicron:inhibition of cell-cell fusion in Calu-3 cells(IC50=3.32 nM);inhibition of cell-cell infusion in Caco2 cells(IC50=0.88 nM);inhibition of infection(Pseudovirus)(IC50=8.63 nM);inhibition of infection(Authentic)(IC50=85.38 nM);
• SARS-CoV-2 Delta:inhibition of cell-cell fusion(IC50=4.04 nM);inhibition of infection(Pseudovirus)(IC50=9.83 nM);
• SARS-CoV-2 D614G:inhibition of cell-cell fusion(IC50=2.57 nM);inhibition of infection(Pseudovirus)(IC50=5.58 nM).
• [Ref.32231345]SARS-CoV:ihibition of cell-cell fusion in Huh-7 cells(IC50=4.3 nM),inhibition of Pseudovirus (PsV) infection in 293T/ACE2 cells(IC50=11.7 nM);
• MERS-CoV:ihibition of cell-cell fusion in Huh-7 cells(IC50=2.5 nM),inhibition of Pseudovirus (PsV) infection in Huh-7 cells(IC50=11.1 nM),inhibit the replication of MERS-CoV in VERO-E6 cells(IC50=4.2 nM);
• HCoV-OC43:ihibition of cell-cell fusion in Huh-7 cells(IC50=7.7 nM),inhibition of Pseudovirus (PsV) infection in 293T/ACE2 cells(IC50=37.7 nM),inhibit the replication of HCoV-OC43 in RD cells(IC50=24.8 nM);
• HCoV-229E:ihibition of cell-cell fusion in Huh-7 cells(IC50=5.2 nM),inhibition of Pseudovirus (PsV) infection in Huh-7 cells(IC50=12.4 nM),inhibit the replication of HCoV-229E in Huh-7 cells(IC50=101.5 nM);
• HCoV-NL63:ihibition of cell-cell fusion in Huh-7 cells(IC50=21.4 nM),inhibition of Pseudovirus (PsV) infection in Huh-7 cells(IC50=76.6 nM),inhibit the replication of HCoV-NL63 in LLC-MK2 cells(IC50=187.6 nM);
• CoV-WIV1:ihibition of cell-cell fusion in Huh-7 cells(IC50=4.5 nM),inhibition of Pseudovirus (PsV) infection in Huh-7 cells(IC50=30.8 nM);
• CoV-Rs3367:ihibition of cell-cell fusion in Huh-7 cells(IC50=8.1 nM),inhibition of Pseudovirus (PsV) infection in Huh-7 cells(IC50=66.9 nM);
• CoV-SHC014:ihibition of cell-cell fusion in Huh-7 cells(IC50=4.3 nM);
• SARS-CoV-2:ihibition of cell-cell fusion in 293T/ACE2 cells(IC50=1.3 nM),inhibition of Pseudovirus (PsV) infection in 293T/ACE2 cells(IC50=15.8 nM),inhibit the replication of MERS-CoV in VERO-E6 cells(IC50=2468 nM).

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

Cytotoxicity 

• [Ref.32231345]<10% cytotoxicity against VERO-E6 cells, RD cells, LLC-MK2 cells, Huh-7 cells up to 10000 nM.

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.

PDB ID  None

Predicted Structure Download  DRAVPe00407

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  PEG4-Chol

Other Modification  None

Stereochemistry  L

Literature 1

Title   Peptide-based pan-CoV fusion inhibitors maintain high potency against SARS-CoV-2 Omicron variant.

Pubmed ID   35087243

Reference   Cell Res. 2022 Apr;32(4):404-406.

Author   Xia S, Chan JF, Wang L, Jiao F, Chik KK, Chu H, Lan Q, Xu W, Wang Q, Wang C, Yuen KY, Lu L, Jiang S.

DOI   10.1038/s41422-022-00617-x

Literature 2

Title   Inhibition of SARS-CoV-2 (previously 2019-nCoV) infection by a highly potent pan-coronavirus fusion inhibitor targeting its spike protein that harbors a high capacity to mediate membrane fusion.

Pubmed ID   32231345

Reference   Cell Res. 2020 Apr;30(4):343-355.

Author   Xia S, Liu M, Wang C, Xu W, Lan Q, Feng S, Qi F, Bao L, Du L, Liu S, Qin C, Sun F, Shi Z, Zhu Y, Jiang S, Lu L.

DOI   10.1038/s41422-020-0305-x