General Information


DRAVP ID  DRAVPe01778

Peptide Name   Alisporivir, Debio-025

Sequence  XxXVXAaXXXX

Sequence Length  11

UniProt ID  No entry found

Taxon ID  None

Source  Synthetic construct

Validation   Experimentally Validated



Origin Information


Gene Name/ID  Not Available

GenBank  Not Available

Amino Acid position  Not Available

Domain Accession ID  Not Available

Nucleotide sequence ID  Not Available

Molecular Type  Not Available

Chromosomal Position  Not Available



Activity Information


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



Structure Information


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)



Physicochemical Information


Formula  C8H-2N2O-6

Absent amino acids  CDEFGHIKLMNPQRSTWY

Common amino acids  X

Mass  0

Pl  0

Basic residues  0

Acidic residues  0

Hydrophobic residues  2

Net charge  0

Boman Index  585

Hydrophobicity  54.55

Aliphatic Index  35.45

Half Life 

  •     Mammalian:
  •     Yeast:
  •     E.coli:

Extinction Coefficient cystines  0

Absorbance 280nm  0

Polar residues  0



Literature Information


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