Fostriecin (original) (raw)
Fostriecin is a type I polyketide synthase (PKS) derived natural product, originally isolated from the soil bacterium Streptomyces pulveraceus. It belongs to a class of natural products which characteristically contain a phosphate ester, an α,β-unsaturated lactam and a conjugated linear diene or triene chain produced by Streptomyces. This class includes structurally related compounds cytostatin and phoslactomycin. Fostriecin is a known potent and selective inhibitor of protein serine/threonine phosphatases, as well as DNA topoisomerase II. Due to its activity against protein phosphatases PP2A and PP4 (IC50 1.5nM and 3.0nM, respectively) which play a vital role in cell growth, cell division, and signal transduction, fostriecin was looked into for its antitumor activity in vivo and showed in
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dbo:abstract | Fostriecin is a type I polyketide synthase (PKS) derived natural product, originally isolated from the soil bacterium Streptomyces pulveraceus. It belongs to a class of natural products which characteristically contain a phosphate ester, an α,β-unsaturated lactam and a conjugated linear diene or triene chain produced by Streptomyces. This class includes structurally related compounds cytostatin and phoslactomycin. Fostriecin is a known potent and selective inhibitor of protein serine/threonine phosphatases, as well as DNA topoisomerase II. Due to its activity against protein phosphatases PP2A and PP4 (IC50 1.5nM and 3.0nM, respectively) which play a vital role in cell growth, cell division, and signal transduction, fostriecin was looked into for its antitumor activity in vivo and showed in vitro activity against leukemia, lung cancer, breast cancer, and ovarian cancer. This activity is thought to be due to PP2A's assumed role in regulating apoptosis of cells by activating cytotoxic T-lymphocytes and natural killer cells involved in tumor surveillance, along with human immunodeficiency virus-1 (HIV-1) transcription and replication. (en) |
dbo:casNumber | 87810-56-8 |
dbo:chEMBL | 17377 |
dbo:fdaUniiCode | ZO1648L551 |
dbo:pubchem | 6913994 |
dbo:thumbnail | wiki-commons:Special:FilePath/Fostriecin_Structure.svg?width=300 |
dbo:wikiPageID | 57552007 (xsd:integer) |
dbo:wikiPageLength | 11569 (xsd:nonNegativeInteger) |
dbo:wikiPageRevisionID | 1081466562 (xsd:integer) |
dbo:wikiPageWikiLink | dbr:Protein_phosphatase_2 dbr:Enzyme_inhibitor dbr:Epimer dbr:Molecule dbr:Natural_killer_cell dbr:Breast_cancer dbr:Cytochrome_P450 dbr:Cytotoxic_T_cell dbr:Dehydratase dbr:Dehydration_reaction dbr:In_vitro dbr:In_vivo dbr:Gene_cluster dbr:Natural_product dbr:Open_reading_frame dbr:Enzyme dbr:Lactam dbr:Lactone dbr:Apoptosis dbr:Leukemia dbr:Lung_cancer dbr:Malonic_acid dbr:Malonyl-CoA dbr:Streptomyces dbr:Bacteria dbr:Acyl_group dbr:Threonine dbr:Acyl_carrier_protein dbr:Alpha_and_beta_carbon dbr:Cell_division dbr:Cell_growth dbr:Diene dbr:Protein dbr:Redox dbr:Hydrolysis dbr:Thioesterase dbc:Polyketides dbr:Biosynthesis dbr:Homoserine_kinase dbr:Signal_transduction dbr:Modularity dbr:Phoslactomycin_B dbr:Human_immunodeficiency_virus_1 dbr:Antitumor dbr:DNA_topoisomerase_II dbr:Methylmalonyl-CoA dbr:Serine dbr:Malonate dbr:Phosphatase dbr:Phosphorylation dbr:Polyketide_synthase dbr:Nomenclature dbr:Ovarian_cancer dbr:Triene dbr:Streptomyces_pulveraceus dbr:File:Biosynthetic_Pathway_of_Fostriecin.gif |
dbp:c | 19 (xsd:integer) |
dbp:casNumber | 87810 (xsd:integer) |
dbp:chembl | 17377 (xsd:integer) |
dbp:chemspiderid | 4510160 (xsd:integer) |
dbp:h | 27 (xsd:integer) |
dbp:iupacName | -3613 (xsd:integer) |
dbp:o | 9 (xsd:integer) |
dbp:p | 1 (xsd:integer) |
dbp:pubchem | 6913994 (xsd:integer) |
dbp:smiles | CCO (en) |
dbp:stdinchi | 1 (xsd:integer) |
dbp:stdinchikey | ZMQRJWIYMXZORG-DSWNLJKISA-N (en) |
dbp:unii | ZO1648L551 (en) |
dbp:width | 200 (xsd:integer) |
dbp:wikiPageUsesTemplate | dbt:Infobox_drug |
dcterms:subject | dbc:Polyketides |
rdf:type | owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 dbo:Drug |
rdfs:comment | Fostriecin is a type I polyketide synthase (PKS) derived natural product, originally isolated from the soil bacterium Streptomyces pulveraceus. It belongs to a class of natural products which characteristically contain a phosphate ester, an α,β-unsaturated lactam and a conjugated linear diene or triene chain produced by Streptomyces. This class includes structurally related compounds cytostatin and phoslactomycin. Fostriecin is a known potent and selective inhibitor of protein serine/threonine phosphatases, as well as DNA topoisomerase II. Due to its activity against protein phosphatases PP2A and PP4 (IC50 1.5nM and 3.0nM, respectively) which play a vital role in cell growth, cell division, and signal transduction, fostriecin was looked into for its antitumor activity in vivo and showed in (en) |
rdfs:label | Fostriecin (en) |
owl:sameAs | wikidata:Fostriecin https://global.dbpedia.org/id/2Z3za |
prov:wasDerivedFrom | wikipedia-en:Fostriecin?oldid=1081466562&ns=0 |
foaf:depiction | wiki-commons:Special:FilePath/Biosynthetic_Pathway_of_Fostriecin.gif wiki-commons:Special:FilePath/Fostriecin_Structure.svg |
foaf:isPrimaryTopicOf | wikipedia-en:Fostriecin |
is dbo:wikiPageWikiLink of | dbr:List_of_drugs:_Fm–Ft dbr:Streptomyces_pulveraceus |
is foaf:primaryTopic of | wikipedia-en:Fostriecin |