General Information

General Information

DRAVP ID DRAVPe00442

Peptide Name EK1-C16

Sequence SLDQINVTFLDLEYEMKKLEEAIKKLEESYIDLKELGSGSG

Sequence Length 41

UniProt ID No entry found

Source Synthetic construct(derived from EK1)

Activity Information

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

Assay pseudovirus inhibition assay

Activity

[Ref.35336956]SARS-CoV-2 WT:inhibition of pseudovirus (PsV) infection in Caco2 cells(IC50=0.48 μM);
SARS-CoV-2 Alpha:inhibition of pseudovirus (PsV) infection(IC50=0.19 μM);
SARS-CoV-2 Beta:inhibition of pseudovirus (PsV) infection(IC50=0.43 μM);
SARS-CoV-2 Gamma:inhibition of pseudovirus (PsV) infection(IC50=0.26 μM);
SARS-CoV-2 Delta:inhibition of pseudovirus (PsV) infection(IC50=0.11 μM);
SARS-CoV-2 Omicron:inhibition of pseudovirus (PsV) infection(IC50=0.23 μM);inhibition of authentic infection in Vero-E6-TMPRSS-2 cells(IC50=0.75 μM);
SARS-CoV:inhibition of pseudovirus (PsV) infection(IC50=0.17 μM);
SARSr-CoV WIV1:inhibition of pseudovirus (PsV) infection(IC50=0.15 μM);
SARSr-CoV Rs3367:inhibition of pseudovirus (PsV) infection(IC50=0.3 μM);
MERS-CoV:inhibition of pseudovirus (PsV) infection in Caco2 cells(IC50=0.10 μM);inhibition of cell-cell fusion(IC50=0.012 μM);
HCoV-OC43:inhibition of authentic infection in RD cells(IC50=0.07 μM);inhibition of cell-cell fusion(IC50=0.01 μM).

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

Cytotoxicity

[Ref.35336956]showed no significant cytotoxicity against RD cells at the concentration of 5 μM.

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 No predicted structure available

Linear/Cyclic Linear

N-terminal Modification Free

C-terminal Modification PEG4-C16(palmitic acid)

Other Modification None

Stereochemistry L

Physicochemical Information

Formula C208H336N48O71S

Absent amino acids CHPRW

Common amino acids EL

Mass 4677.29

Pl 4.36

Basic residues 5

Acidic residues 10

Hydrophobic residues 13

Net charge -5

Boman Index -6701

Hydrophobicity -44.88

Aliphatic Index 104.63

Half Life

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

Extinction Coefficient cystines 2980

Absorbance 280nm 74.5

Polar residues 11

Literature Information

Literature 1

Title A Palmitic Acid-Conjugated, Peptide-Based pan-CoV Fusion Inhibitor Potently Inhibits Infection of SARS-CoV-2 Omicron and Other Variants of Concern.

Pubmed ID 35336956

Reference Viruses. 2022 Mar 6;14(3):549.

Author Lan Q, Chan JF, Xu W, Wang L, Jiao F, Zhang G, Pu J, Zhou J, Xia S, Lu L, Yuen KY, Jiang S, Wang Q.

DOI 10.3390/v14030549