Fostriecin (original) (raw)

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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
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dbp:c 19 (xsd:integer)
dbp:casNumber 87810 (xsd:integer)
dbp:chembl 17377 (xsd:integer)
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dbp:o 9 (xsd:integer)
dbp:p 1 (xsd:integer)
dbp:pubchem 6913994 (xsd:integer)
dbp:smiles CCO (en)
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dbp:stdinchikey ZMQRJWIYMXZORG-DSWNLJKISA-N (en)
dbp:unii ZO1648L551 (en)
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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)
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foaf:depiction wiki-commons:Special:FilePath/Biosynthetic_Pathway_of_Fostriecin.gif wiki-commons:Special:FilePath/Fostriecin_Structure.svg
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