dbacp02801
General Description
Peptide name : Dolastatin 10
Source/Organism : Wedge sea hare
Linear/Cyclic : Not found
Chirality : Not found
Sequence Information
Sequence : 2-[[2-(dimethylamino)-3-methylbutanoyl]amino]-N-[3-methoxy-1-[2-[1-methoxy-2-methyl-3-oxo-3-[[2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutaNAmide
Peptide length: Not available
C-terminal modification: Not found
N-terminal modification : Not found
Non-natural peptide information: None
Activity Information
Assay type : TUNEL assay
Assay time : 96h
Activity : IC50 : 0.5 nM
Cell line : DU-145
Cancer type : Prostate cancer
Other activity : Not found
Physicochemical Properties
Amino Acid Composition Bar Chart : Not available
Molecular mass : Not available
Aliphatic index : Not available
Instability index : Not available
Hydrophobicity (GRAVY) : Not available
Isoelectric point : Not available
Charge (pH 7) : Not available
Aromaticity : Not available
Molar extinction coefficient (cysteine, cystine): Not available
Hydrophobic/hydrophilic ratio : Not available
hydrophobic moment : Not available
Missing amino acid : Not available
Most occurring amino acid : Not available
Most occurring amino acid frequency : Not available
Least occurring amino acid : Not available
Least occurring amino acid frequency : Not available
Structural Information
3D-structure: Not available
Secondary structure fraction (Helix, Turn, Sheet): Not available
SMILES Notation: Not available
Secondary Structure :
| Method | Prediction |
|---|---|
| GOR | Not available |
| Chou-Fasman (CF) | Not available |
| Neural Network (NN) | Not available |
| Joint/Consensus | Not available |
Molecular Descriptors and ADMET Properties
Molecular descriptors: Not available
ADMET properties: Not available
Cross Referencing Databases databases
Pubmed Id : 9492845, .
Uniprot : Not available
CancerPPD : Not available
ApIAPDB : Not available
Reference
1 : Turner T, et al. Treatment of human prostate cancer cells with dolastatin 10, a peptide isolated from a marine shell-less mollusc. Prostate. 1998; 34:175-81. doi: 10.1002/(sici)1097-0045(19980215)34:3<175::aid-pros4>3.0.co;2-h
Literature
Paper title : Treatment of human prostate cancer cells with dolastatin 10, a peptide isolated from a marine shell-less mollusc.
Doi : https://doi.org/10.1002/(sici)1097-0045(19980215)34:3<175::aid-pros4>3.0.co;2-h
Abstract : BACKGROUND: Dolastatin 10 is an anticancer peptide isolated from the sea hare, Dolabela auricularia, which is currently in phase I trials. METHODS: The effects of dolastatin 10 on the DU-145 human prostate cancer cell line were studied both in tissue culture and in athymic nude mice. In tissue culture, after dolastatin 10 treatment, cell cycle kinetics were measured using propidum iodide, apoptosis was estimated using the TUNEL assay, and tubulin architecture studied by direct immunofluorescence. RESULTS: At concentrations of 1 nM (IC50 = 0.5 nM), dolastatin 10 completely inhibited the growth in tissue culture of human prostate cancer DU-145 cells. Growth inhibition was correlated with the arrest of these cells in G2/M and alpha-tubulin depolymerization. In athymic mice at a dose of 5 micrograms every 4 days i.p., dolastatin 10 blocked the diaphragmatic invasion of DU-145 tumor cells. CONCLUSIONS: Dolastatin 10 is a novel marine-derived compound with activity in the treatment of human prostate cancer in animals. The mechanism of action of this agent involves tubulin depolymerization but not the induction of apoptosis.