General Information

General Information

DRAVP ID DRAVPe00431

Peptide Name EKL1

Sequence NVTFLDLEYEMKKLEEAIKKLEESYIDLKELGTYEY

Sequence Length 36

UniProt ID No entry found

Source Synthetic construct(derived from EK1)

Activity Information

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

Assay

Activity

[Ref.34367893]SARS-CoV-2:Inhibition of Pseudovirus(PsV) infection in Huh-7 cells(IC50=0.622±0.089 μmol/L),Inhibition of Pseudovirus(PsV) infection in 293T/ACE2 cells(IC50>5 μmol/L),Inhibition of Pseudovirus(PsV) infection in Caco-2 cells(IC50=0.746±0.152 μmol/L),inhibition of cell-cell fusion(IC50=0.220±0.034 μmol/L);inhibited authentic SARS-CoV-2 infection in Vero E6 cells(IC50=1.407±0.189 μmol/L);
inhibition of multiple HCoV Pseudovirus:SARS-CoV (IC50=6.716±5.937 μmol/L), MERS-CoV(IC50=4.086±0.345 μmol/L), HCoV-OC43(IC50=10.530±3.778 μmol/L), HCoV-NL63(IC50=3.700±0.222 μmol/L), SARSr-CoV-WIV1(IC50=30.270±4.713 μmol/L), and HCoV-Rs3367 (IC50=88.300±24.600 μmol/L),inhibition of authentic HCoV-OC43 infection in RD cells (IC50=20.290±1.092 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 DRAVPe00431

Linear/Cyclic Linear

N-terminal Modification Free

C-terminal Modification Free

Other Modification None

Stereochemistry L

Physicochemical Information

Formula C201H312N42O65S

Absent amino acids CHPQRW

Common amino acids E

Mass 4388.99

Pl 4.39

Basic residues 5

Acidic residues 10

Hydrophobic residues 11

Net charge -5

Boman Index -6393

Hydrophobicity -64.72

Aliphatic Index 97.5

Half Life

Mammalian:1.4 hour
Yeast:3 min
E.coli:>10 hour

Extinction Coefficient cystines 5960

Absorbance 280nm 170.29

Polar residues 9

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