DRAVP ID  DRAVPe00416

Peptide Name   IBP02V4

Sequence  ELSGINASVVNLQKEIDRLNEVAKNLNESLIDLQEL

Sequence Length  36

UniProt ID  No entry found

Source  Synthetic construct(derived from HR2 region of SARS-CoV)

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

Assay 

Activity 

• [Ref.34344868]SARS-CoV-2:inhibition of SARS-CoV-2 S protein-mediated cell-cell fusion(IC50=0.3±0.02 nM);inhibition of SARS-CoV-2 pseudovirus infection in 293T/ACE2 cells(IC50=18.6 nM);inhibition of SARS-CoV-2 pseudovirus infection in Huh-7 cells(IC50=15.2 nM);
• SARS-CoV-2 D614G:inhibition of S protein-mediated cell-cell fusion(IC50=0.1±0.02 nM);inhibition of pseudovirus infection in 293T/ACE2 cells(IC50=29.2 nM);inhibition of pseudovirus infection in Huh-7 cells(IC50=26.3 nM);
• SARS-CoV:inhibition of pseudovirus infection in Huh-7 cells(IC50=63±1.7 nM);
• MERS-CoV:inhibition of pseudovirus infection in Huh-7 cells(IC50=22.4±2.2 nM);
• HCoV-NL63:inhibition of pseudovirus infection in Huh-7 cells(IC50=66.3±3.1 nM);
• HCoV-229E:inhibition of pseudovirus infection in Huh-7 cells(IC50=502±24.2 nM).

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

Cytotoxicity 

• [Ref.34344868]No significant cytotoxicity in both 293T/ACE2 and Huh-7 cells at a concentration of 10 μM.

Binding Target  membrane

Mechanism  A six-helical bundle structure is formed by two heptad repeat domains (HR1 and HR2) in S2, juxtaposing the viral and cellular membranes for fusion.The peptide derived from the HR2 sequence can competitively bind to the viral HR1 domain thus exerting antiviral activity.

PDB ID  None

Predicted Structure Download  DRAVPe00416

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  PEG8-K(Chol)

Other Modification  None

Stereochemistry  L

Literature 1

Title   SARS-CoV-2-derived fusion inhibitor lipopeptides exhibit highly potent and broad-spectrum activity against divergent human coronaviruses.

Pubmed ID   34344868

Reference   Signal Transduct Target Ther. 2021 Aug 3;6(1):294.

Author   Zhu Y, Yu D, Hu Y, Wu T, Chong H, He Y.

DOI   10.1038/s41392-021-00698-x