DRAVP ID  DRAVPs015

Peptide Name   P21S8ZF

Sequence  LDLTYEZLSLQXVVKXLNESF

Sequence Length  21

Original Sequence  DLTYEZLSLQAVVKALNESF

Source  Synthetic construct (From S2 unit of MERS-Cov)

Validation   Experimentally Validated

Target Organism  MERS-CoV

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

Activity 

• [Ref.29442512]MERS-CoV:inhibition of cell-cell fusion in Huh-7 cells(EC50=3.89 ± 0.8 μM).

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 peptide inhibits MERS-CoV infection and its spike (S) protein-mediated cell–cell fusion.

Linear/Cyclic  Cyclic

N-terminal Modification  Acetylation

C-terminal Modification  Carboxyamidation

Special Amino Acid and Stapling Position  ①The 'X' (position: 12 and 16) in sequence indicates S5 stapling amino acid. Note: S5 is (S)-pentenyl alanine. ②X (12) and X (16) are cross-linked by hydrocarbon stapling.,The 'Z' at position 7 indicates R8 ((R)-octenyl alanine)

Structure Description  Not Available

Stereochemistry  L

Literature 1

Title   Discovery of Hydrocarbon-Stapled Short α-Helical Peptides as Promising Middle East Respiratory Syndrome Coronavirus (MERS-CoV) Fusion Inhibitors

Pubmed ID   29442512

Reference   Journal of medicinal chemistry, 61(5), 2018–2026.

Author   Wang, C., Xia, S., Zhang, P., Zhang, T., Wang, W., Tian, Y., Meng, G., Jiang, S., & Liu, K. (2018).

DOI   10.1021/acs.jmedchem.7b01732