General Information


DRAVP ID  DRAVPe01766

Peptide Name   EK1-GSGSGC

Sequence  SLDQINVTFLDLEYEMKKLEEAIKKLEESYIDLKELGSGSGC

Sequence Length  42

UniProt ID  Q8BB25 

Source  Synthetic construct



Activity Information


Target Organism  SARS-CoV-2

Assay  Cell-cell fusion assay,infectivity assay

Activity 

  • [Ref.33082259]SARS-CoV-2:ihibition of cell-cell fusion in 293T cells(IC50=293±60 nM,IC90>900 nM),inhibition of infection in Vero E6 cells(IC50~ 41 nM);
  • SARS-CoV-2_D614G:ihibition of cell-cell fusion in 293T cells(IC50=261±136 nM,IC90=892±100 nM);
  • SARS-CoV-2_S943P:ihibition of cell-cell fusion in 293T cells(IC50=286±104 nM,IC90>1000 nM);
  • SARS-CoV-2_S247R:ihibition of cell-cell fusion in 293T cells(IC50=194±107 nM,IC90=893±77 nM);
  • MERS-CoV:ihibition of cell-cell fusion in 293T cells(IC50>1000 nM,IC90>1000 nM),inhibition of infection in Vero E6 cells(IC50~ 2 nM);
  • SARS-CoV-1:ihibition of cell-cell fusion in 293T cells(IC50=36±5 nM,IC90>1000 nM).

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

Cytotoxicity 

  • [Ref.33082259]Human embryonic kidney HEK293T cells:<5% Cytotoxicity at 10 µM;Vero E6 cells:18% Cytotoxicity at 10 µM.

Binding Target  membrane

Mechanism  The lipopeptide is derived from the C-terminal heptad repeat (HRC) domain of SARS-CoV-2 S that potently inhibits infection by SARS-CoV-2.



Structure Information


PDB ID  None

Predicted Structure Download  No predicted structure available

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  Free

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C211H341N49O72S2

Absent amino acids  HPRW

Common amino acids  EL

Mass  4780.43

Pl  4.36

Basic residues  5

Acidic residues  10

Hydrophobic residues  13

Net charge  -5

Boman Index  -6573

Hydrophobicity  -37.86

Aliphatic Index  102.14

Half Life 

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

Extinction Coefficient cystines  2980

Absorbance 280nm  72.68

Polar residues  12



Literature Information


Literature 1

Title   Inhibition of Coronavirus Entry In Vitro and Ex Vivo by a Lipid-Conjugated Peptide Derived from the SARS-CoV-2 Spike Glycoprotein HRC Domain.

Pubmed ID   33082259

Reference   mBio. 2020 Oct 20;11(5):e01935-20.

Author   Outlaw VK, Bovier FT, Mears MC, Cajimat MN, Zhu Y, Lin MJ, Addetia A, Lieberman NAP, Peddu V, Xie X, Shi PY, Greninger AL, Gellman SH, Bente DA, Moscona A, Porotto M.

DOI   10.1128/mBio.01935-20