DRAVP ID  DRAVPe01778

Peptide Name   Alisporivir, Debio-025

Sequence  XxXVXAaXXXX

Sequence Length  11

UniProt ID  No entry found

Source  Synthetic construct

Target Organism  SARS-CoV-2

Assay  plaque assay

Activity 

• [Ref.32376613]SARS-CoV-2:Inhibition of infection in Vero E6 cells(EC50=0.46±0.04 µM,E90=3.10±1.40 μM).
• [Ref.32568027]SARS-CoV-2:Inhibition of infection in Vero E6 cells(EC50=4.9±1.3 µM);
• SARS-CoV:Inhibition of infection in Vero E6 cells(EC50=4.3±1.0 µM).

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

Cytotoxicity 

• [Ref.32376613]Vero E6 cells:CC50>20µM.

Binding Target  Not found

Mechanism  Comment: No comments found on DRAMP database

PDB ID  None

Predicted Structure Download  No predicted structure available

Linear/Cyclic  Cyclic

N-terminal Modification  No specific N-terminal

C-terminal Modification  No specific C-terminal

Other Modification  The 'X' at position 1 is alpha-aminobutyric acid,position 2 is N-methylalanine,the 'V' at position 3 is N-methylalanine,the 'X' at position 5,8,9 are N-methylleucine,the 'X' at position 10 is N-methylvaline and position 11 is N-methyl-(4R)-4-[(E)-but-2-enyl]-4-methyl-L-threonyl

Stereochemistry  Mixed(D-Ala7,D-meth-Ala2)

Literature 1

Title   Inhibition of SARS-CoV-2 Infection by the Cyclophilin Inhibitor Alisporivir (Debio 025).

Pubmed ID   32376613

Reference   Antimicrob Agents Chemother. 2020 Jun 23;64(7):e00876-20.

Author   Softic L, Brillet R, Berry F, Ahnou N, Nevers Q, Morin-Dewaele M, Hamadat S, Bruscella P, Fourati S, Pawlotsky JM, Ahmed-Belkacem A.

DOI   10.1128/AAC.00876-20

Literature 2

Title   SARS-coronavirus-2 replication in Vero E6 cells: replication kinetics, rapid adaptation and cytopathology.

Pubmed ID   32568027

Reference   J Gen Virol. 2020 Sep;101(9):925-940.

Author   Ogando NS, Dalebout TJ, Zevenhoven-Dobbe JC, Limpens RWAL, van der Meer Y, Caly L, Druce J, de Vries JJC, Kikkert M, Bárcena M, Sidorov I, Snijder EJ.

DOI   10.1099/jgv.0.001453