Abstract
A small collection of marine natural product extracts was screened for compounds that would compensate lost tumor suppressor functionality in PTEN-deficient cells. From the most active extract, the previously unreported bromotyrosine derivative, psammaplysene A (1), was identified. Psammaplysene A compensates for PTEN loss by relocalizing the transcription factor FOXO1a to the nucleus.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Active Transport, Cell Nucleus / drug effects*
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Animals
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DNA-Binding Proteins / antagonists & inhibitors*
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Forkhead Box Protein O1
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Forkhead Transcription Factors
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Humans
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Indian Ocean
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Models, Molecular
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Molecular Structure
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Nuclear Magnetic Resonance, Biomolecular
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PTEN Phosphohydrolase
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Phosphoric Monoester Hydrolases / deficiency*
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Phosphoric Monoester Hydrolases / genetics
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Porifera / chemistry*
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Transcription Factors / antagonists & inhibitors*
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Tumor Suppressor Proteins / deficiency*
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Tumor Suppressor Proteins / genetics
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Tyrosine / analogs & derivatives*
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Tyrosine / chemistry
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Tyrosine / isolation & purification*
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Tyrosine / pharmacology
Substances
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DNA-Binding Proteins
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FOXO1 protein, human
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Forkhead Box Protein O1
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Forkhead Transcription Factors
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Transcription Factors
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Tumor Suppressor Proteins
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psammaplysene A
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Tyrosine
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Phosphoric Monoester Hydrolases
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PTEN Phosphohydrolase
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PTEN protein, human