DRAVP ID  DRAVPe00401

Peptide Name   EK1

Sequence  SLDQINVTFLDLEYEMKKLEEAIKKLEESYIDLKEL

Sequence Length  36

UniProt ID  Q8BB25 

Taxon ID  2697049  

Source  Synthetic construct(derived from OC43-HR2P)

Validation   Experimentally Validated

Gene Name/ID  S2 (918758)

GenBank  MN908947.3,AY585229.1

Amino Acid position  EK1 peptide was individually fused to the 3′ end of the HR1 domain from SARS-CoV, MERS-CoV, and HCoV-229E (residues 892 to 970, 984 to 1062, and 785 to 873, respectively) 

Domain Accession ID  cd22380 pfam01601 

Nucleotide sequence ID  MN908947, AY585229 

Molecular Type  Genomic RNA

Chromosomal Position  Long arm (q) of chromosome 3 at position 13.33.

Target Organism  SARS-CoV-2,MERS-CoV,HCoV-229E,HCoV-NL63,CoV-WIV1

Assay  Cell fusion assay

Activity 

• [Ref.35087243]SARS-CoV-2 Omicron:inhibition of cell-cell fusion in Calu-3 cells(IC50=119.68 nM);inhibition of cell-cell infusion in Caco2 cells(IC50=74.99 nM);inhibition of infection(Pseudovirus)(IC50=309.4 nM);inhibition of infection(Authentic)(IC50=1138 nM);
• SARS-CoV-2 Delta:inhibition of cell-cell fusion(IC50=131.8 nM);inhibition of infection(Pseudovirus)(IC50=427.55 nM);
• SARS-CoV-2 D614G:inhibition of cell-cell fusion(IC50=314.6 nM);inhibition of infection(Pseudovirus)(IC50=414.85 nM).
• [Ref.32231345]SARS-CoV:ihibition of cell-cell fusion in Huh-7 cells(IC50=409.3 nM),inhibition of Pseudovirus (PsV) infection in 293T/ACE2 cells(IC50=3237 nM);
• MERS-CoV:ihibition of cell-cell fusion in Huh-7 cells(IC50=239.5 nM),inhibition of Pseudovirus (PsV) infection in Huh-7 cells(IC50=631.8 nM),inhibit the replication of MERS-CoV in VERO-E6 cells(IC50=802.1 nM);
• HCoV-OC43:ihibition of cell-cell fusion in Huh-7 cells(IC50=787.6 nM),inhibition of Pseudovirus (PsV) infection in 293T/ACE2 cells(IC50=1398 nM),inhibit the replication of HCoV-OC43 in RD cells(IC50=1554 nM);
• HCoV-229E:ihibition of cell-cell fusion in Huh-7 cells(IC50=207.4 nM),inhibition of Pseudovirus (PsV) infection in Huh-7 cells(IC50=3963 nM),inhibit the replication of HCoV-229E in Huh-7 cells(IC50=4375 nM);
• HCoV-NL63:ihibition of cell-cell fusion in Huh-7 cells(IC50=751.0 nM),inhibition of Pseudovirus (PsV) infection in Huh-7 cells(IC50=7666 nM),inhibit the replication of HCoV-NL63 in LLC-MK2 cells(IC50=3693 nM);
• CoV-WIV1:ihibition of cell-cell fusion in Huh-7 cells(IC50=265.7 nM),inhibition of Pseudovirus (PsV) infection in Huh-7 cells(IC50=5425 nM);
• CoV-Rs3367:ihibition of cell-cell fusion in Huh-7 cells(IC50=237.0 nM),inhibition of Pseudovirus (PsV) infection in Huh-7 cells(IC50=6014 nM);
• CoV-SHC014:ihibition of cell-cell fusion in Huh-7 cells(IC50=279.6 nM);
• SARS-CoV-2:ihibition of cell-cell fusion in 293T/ACE2 cells(IC50=286.7-315.0 nM),inhibition of Pseudovirus (PsV) infection in 293T/ACE2 cells(IC50=2375.0 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  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.

PDB ID  None

Predicted Structure Download  DRAVPe00401

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  Free

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