DRAVP ID  DRAVPe00441

Peptide Name   EKL1C

Sequence  NVTFLDLEYEMKKLEEAIKKLEESYIDLKELGTYEYGSGC

Sequence Length  40

UniProt ID  No entry found

Source  Synthetic construct(derived from EK1)

Target Organism  SARS-CoV-2,SARS-CoV,MERS-CoV,HCoV-NL63,HCoV-OC43

Assay  Cell fusion assay

Activity 

• [Ref.35087243]SARS-CoV-2 Omicron:inhibition of cell-cell fusion in Calu-3 cells(IC50=12.18 nM);inhibition of cell-cell infusion in Caco2 cells(IC50=5.52 nM);inhibition of infection(Pseudovirus)(IC50=26.14 nM);inhibition of infection(Authentic)(IC50=182.2 nM);
• SARS-CoV-2 Delta:inhibition of cell-cell fusion(IC50=14.42 nM);inhibition of infection(Pseudovirus)(IC50=31.99 nM);
• SARS-CoV-2 D614G:inhibition of cell-cell fusion(IC50=11.77 nM);inhibition of infection(Pseudovirus)(IC50=23.6 nM).
• [Ref.34367893]SARS-CoV-2:Inhibition of Pseudovirus(PsV) infection in Huh-7 cells(IC50=0.045±0.006 μmol/L),Inhibition of Pseudovirus(PsV) infection in 293T/ACE2 cells(IC50=0.037±0.009 μmol/L),Inhibition of Pseudovirus(PsV) infection in Caco-2 cells(IC50=0.040±0.005 μmol/L),inhibition of cell-cell fusion(IC50=0.008±0.001 μmol/L);inhibited authentic SARS-CoV-2 infection in Vero E6 cells(IC50=0.003±0.001 μmol/L);
• SARS-CoV-2 variants(inhibition of Pseudovirus(PsV) infection):V341L(IC50=0.047±0.013 μmol/L);F342L(IC50=0.026±0.007 μmol/L);V367F(IC50=0.066±0.012 μmol/L);R408I(IC50=0.148±0.012 μmol/L);N435D(IC50=0.135±0.013 μmol/L);G476S(IC50=0.065±0.008 μmol/L);V483A(IC50=0.078±0.011 μmol/L);N501Y(IC50=0.069±0.006 μmol/L);D614G(IC50=0.104±0.010 μmol/L);12 mutations(P.1)(IC50=0.046±0.006 μmol/L);K417N-E484K-N501Y(IC50=0.113±0.013 μmol/L);8 mutations(B.1.1.7)(IC50=0.120±0.009 μmol/L);wide type(IC50=0.049±0.007 μmol/L);
• inhibition of multiple HCoV Pseudovirus:SARS-CoV (IC50=0.076±0.014 μmol/L), MERS-CoV(IC50=0.048±0.006 μmol/L), HCoV-OC43(IC50=0.668±0.081 μmol/L), HCoV-NL63(IC50=0.035±0.003 μmol/L), SARSr-CoV-WIV1(IC50=0.218±0.013 μmol/L), and HCoV-Rs3367 (IC50=0.046±0.003 μmol/L),inhibition of authentic HCoV-OC43 infection in RD cells (IC50=0.281±0.018 μmol/L).

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

Cytotoxicity 

• [Ref.34367893]Huh-7 cells:CC50=10 μmol/L;Caco-2 cells:CC50=13.81 μmol/L;293T/ACE2 cells:CC50=8.49 μmol/L.

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  DRAVPe00441

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  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   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