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MYP_081632
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Basic Information
Plitidepsin, Aplidine
Anticancer ▸ Cytotoxic anticancer activity ▸ Cytotoxic
Antimicrobial
Antiviral
Antiviral ▸ Anti-Coronavirus ▸ Anti-SARS-CoV-2
Antiviral ▸ Antiviral mechanism ▸ Viral replication inhibition
Membrane / Ion-channel modulation ▸ Sodium channel modulation ▸ Sodium channel inhibitor
Toxicity / Safety ▸ Cytotoxicity ▸ Cytotoxic
Venom / Toxin ▸ General toxin ▸ Cytotoxic
not Standard
8 amino acids
-
contains X representing unresolved or non-standard residue
Sequence
PXTXXLPX
Physicochemical Analysis
0.00 Da
0.00
0.00
0.00
0.00
0.00
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Residue Composition
Amino Acid Composition
Chemical Descriptors
Structural Visualization
3D PDB MODEL
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2D CHEMICAL STRUCTURE
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Experimental Records
RECORD: Rec_0004675 VERIFIED: YES
Provenance & Taxonomy
synthetic construct [Synthetic]
Synthetic peptide
32630
Structure & Mods
linear peptide [Linear]
mixed L/D amino-acid peptide [Mixed]
Pyruvoyl
None
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.; Pyruvoyl
Bio-Activity Profile
Antiviral Anti-SARS-CoV-2 Replication inhibition
SARS-CoV-2 D614G | E6 cells
0.0052 μM
IC50
Mammalian: >20 h; Yeast: >20 h; E. coli: ?
PaperUnraveling the antiviral activity of plitidepsin against SARS-CoV-2 by subcellular and morphological analysis. | 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. | Antiviral Res. 2022 Apr;200:105270. | DOI:10.1016/j.antiviral.2022.105270 | PMID:35231500 PMID35231500 Evidence URLhttps://pubmed.ncbi.nlm.nih.gov/35231500/
RECORD: Rec_0035139 VERIFIED: YES
Provenance & Taxonomy
synthetic construct [Synthetic]
32630
Structure & Mods
linear peptide [Linear]
mixed L/D amino-acid peptide [Mixed]
Pyruvoyl
None
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
Bio-Activity Profile
Antimicrobial Anti-SARS-CoV-2
SARS-CoV-2 Delta:inhibition of replication in Vero E6 cells
0.0039 μM
IC50
PMID35231500;33495306 Evidence URLhttps://pubmed.ncbi.nlm.nih.gov/35231500/
RECORD: Rec_0073420 VERIFIED: YES
Provenance & Taxonomy
synthetic construct [Synthetic]
Synthetic peptide
32630
Structure & Mods
linear peptide [Linear]
mixed L/D amino-acid peptide [Mixed]
Pyruvoyl
None
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.; Pyruvoyl
Bio-Activity Profile
Antiviral Replication inhibition
inhibition of replication In pneumocyte-like cells
0.00314 μM
IC90
Mammalian: >20 h; Yeast: >20 h; E. coli: ?
PaperPlitidepsin has potent preclinical efficacy against SARS-CoV-2 by targeting the host protein eEF1A. | 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, Garc | Science. 2021 Feb 26;371(6532):926-931. | DOI:10.1126/science.abf4058 | PMID:33495306 PMID33495306 Evidence URLhttps://pubmed.ncbi.nlm.nih.gov/33495306/
RECORD: Rec_0091980 VERIFIED: YES
Provenance & Taxonomy
synthetic construct [Synthetic]
Synthetic peptide
32630
Structure & Mods
linear peptide [Linear]
mixed L/D amino-acid peptide [Mixed]
Pyruvoyl
None
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.; Pyruvoyl
Bio-Activity Profile
Antiviral Replication inhibition
inhibition of replication In pneumocyte-like cells
0.00162 μM
IC50
Mammalian: >20 h; Yeast: >20 h; E. coli: ?
PaperPlitidepsin has potent preclinical efficacy against SARS-CoV-2 by targeting the host protein eEF1A. | 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, Garc | Science. 2021 Feb 26;371(6532):926-931. | DOI:10.1126/science.abf4058 | PMID:33495306 PMID33495306 Evidence URLhttps://pubmed.ncbi.nlm.nih.gov/33495306/
RECORD: Rec_0109980 VERIFIED: YES
Provenance & Taxonomy
synthetic construct [Synthetic]
32630
Structure & Mods
linear peptide [Linear]
mixed L/D amino-acid peptide [Mixed]
Pyruvoyl
None
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
Bio-Activity Profile
Antimicrobial Anti-SARS-CoV-2 Cytotoxic
PMID35231500;33495306 Evidence URLhttps://pubmed.ncbi.nlm.nih.gov/35231500/
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