DRAVP ID  DRAVPe00750

Peptide Name   IIQ

Sequence  IEEIQKKIEEIQKKIEEIQKKIEEIQKKIEEIQKKXX

Sequence Length  37

UniProt ID  No entry found

Source  Synthetic construct

Target Organism  MERS-CoV,H3N2,H1N1,HIV,EboV

Assay  MERS-CoV S Protein-Mediated Cell–Cell Fusion Assay

Activity 

• [Ref.30192544]MERS-CoV:inhibition of cell-cell fusion between 293T / MERS / EGPF cells and Huh-7 cells(EC50=0.11±0.02 μM);inhibition of pseudovirus infection in Huh-7 cells(IC50=0.13±0.1 μM);
• A/Puerto Rico/8/34 (H1N1):inhibition of virus infection in MDCK cells(EC50=1.73±0.81 μM);
• A/Hong Kong/8/68 (H3N2):inhibition of virus infection in MDCK cells(EC50=0.70±0.09 μM);
• HIV-1 inhibition of cell-cell fusion in TZM-bl cells(EC50=3.63 ±0.54 μM);
• Ebola virus (EboV):inhibition of pseudovirus infection in TZM-bl cells(EC50=1.02 ± 0.54 μM).

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

Cytotoxicity 

• [Ref.30192544]Huh-7 cell:CC50>100 μM;
• MDCK cell:CC50>100 μM;
• TZM-bl cell:CC50>100 μM.

Binding Target  membrane

Mechanism  The peptide can interact with both MERS-CoV and IAV NHR trimeric coiled coils to prevent virus–cell membrane fusion.

PDB ID  None

Predicted Structure Download  No predicted structure available

Linear/Cyclic  Linear

N-terminal Modification  Acetylation

C-terminal Modification  Amidation

Other Modification  The 'X' at 36 indicates β-alanine,the 'X' at 37 indicates Lys-C16(palmitic acid).

Stereochemistry  L

Literature 1

Title   De Novo Design of α-Helical Lipopeptides Targeting Viral Fusion Proteins: A Promising Strategy for Relatively Broad-Spectrum Antiviral Drug Discovery. 

Pubmed ID   30192544

Reference    J Med Chem. 2018 Oct 11;61(19):8734-8745.

Author   Wang C, Zhao L, Xia S, Zhang T, Cao R, Liang G, Li Y, Meng G, Wang W, Shi W, Zhong W, Jiang S, Liu K. 

DOI   10.1021/acs.jmedchem.8b00890