General Information

    • DRAMP ID

    • DRAMP29234

    • Peptide Name

    • Plitidepsin, Aplidine

    • Source

    • Synthetic construct

    • Family

    • Not found

    • Gene

    • Not found

    • Sequence

    • PxTXXLPX

    • Sequence Length

    • 8

    • UniProt Entry

    • No entry found

    • Protein Existence

    • Not found

Activity Information

    • Biological Activity

    • Antimicrobial, Antiviral(SARS-CoV-2)

    • Target Organism

      • [Ref.33495306]Virus:SARS-CoV-2:inhibition of replication In Vero E6 cells(IC50=0.70 nM,IC90=1.76 nM);inhibition of replication In hACE2-HEK293T cells(IC50=0.73 nM,IC90=0.88 nM);inhibition of replication In pneumocyte-like cells(IC50=1.62 nM,IC90=3.14 nM).
      • [Ref.35231500]Virus:
      • SARS-CoV-2 D614G:inhibition of replication in Vero E6 cells(IC50=5.2 nM);
      • SARS-CoV-2 Delta:inhibition of replication in Vero E6 cells(IC50=3.9 nM);
      • SARS-CoV-2 Omicron:inhibition of replication in Vero E6 cells(IC50=4.3 nM).

    • Hemolytic Activity

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

    • Cytotoxicity

      • [Ref.33495306]Vero E6 cells:CC10=0.36 nM,CC50=1.99 nM;hACE2-293T cells:CC10=2.00 nM,CC50>200 nM;pneumocyte-like cells:CC10=20.88 nM,CC50=65.43 nM.

    • Binding Target

    • Not found

Structure Information

    • Linear/Cyclic

    • Linear

    • N-terminal Modification

    • Pyruvoyl

    • C-terminal Modification

    • Free

    • Nonterminal Modifications and Unusual Amino Acids

    • The 'X' at position 2 is N-methylleucine,position 4 is 4-amino-3-hydroxy-5-methyl-Heptanoic acid, position 5 is Hydroxyisovalerylpropionyl, and position 8 is N-methyl-4-methyl-tyrosine.There is a Sidechain-Mainchain Bond between position 3 and 8.

    • Stereochemistry

    • Mixed(D-meth-Leu2)

    • Structure

    • Not found

    • Structure Description

    • Not found

    • Helical Wheel Diagram

    • DRAMP29234 helical wheel diagram

    • PDB ID

    • None

    • Predicted Structure

    • There is no predicted structure for DRAMP29234.

Physicochemical Information

    • Formula

    • Absent Amino Acids

    • ACDEFGHIKMNQRSVWY

    • Common Amino Acids

    • Mass

    • 0

    • PI

    • 0

    • Basic Residues

    • 0

    • Acidic Residues

    • 0

    • Hydrophobic Residues

    • 1

    • Net Charge

    • 0

    • Boman Index

    • 235

    • Hydrophobicity

    • -0.013

    • Aliphatic Index

    • 48.75

    • Half Life

      • Mammalian:
      • Yeast:
      • E.coli:

    • Extinction Coefficient Cystines

    • 0

    • Absorbance 280nm

    • 0

    • Polar Residues

    • 1

DRAMP29234

Comments Information

    • Mechanism of action

    • The antiviral activity of plitidepsin against SARS-CoV-2 is mediated through inhibition of the known target eEF1A (eukaryotic translation elongation factor 1A).

Literature Information

  • ·Literature 1

    • Title

    • Unraveling the antiviral activity of plitidepsin against SARS-CoV-2 by subcellular and morphological analysis.

    • Reference

    • Antiviral Res. 2022 Apr;200:105270.

    • Author

    • Sachse M, Tenorio R, Fernández de Castro I, Muñoz-Basagoiti J, Perez-Zsolt D, Raïch-Regué D, Rodon J, Losada A, Avilés P, Cuevas C, Paredes R, Segalés J, Clotet B, Vergara-Alert J, Izquierdo-Useros N, Risco C.
  • ·Literature 2

    • Title

    • Plitidepsin has potent preclinical efficacy against SARS-CoV-2 by targeting the host protein eEF1A.

    • Reference

    • Science. 2021 Feb 26;371(6532):926-931.

    • Author

    • White KM, Rosales R, Yildiz S, Kehrer T, Miorin L, Moreno E, Jangra S, Uccellini MB, Rathnasinghe R, Coughlan L, Martinez-Romero C, Batra J, Rojc A, Bouhaddou M, Fabius JM, Obernier K, Dejosez M, Guillén MJ, Losada A, Avilés P, Schotsaert M, Zwaka T, Vignuzzi M, Shokat KM, Krogan NJ, García-Sastre A.