The Psammaplysenes, Specific Inhibitors of FOXO1a Nuclear Export

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 c...

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Veröffentlicht in:	Journal of natural products (Washington, D.C.) D.C.), 2005-04, Vol.68 (4), p.574-576
Hauptverfasser:	Schroeder, Frank C, Kau, Tweeny R, Silver, Pamela A, Clardy, Jon
Format:	Artikel
Sprache:	eng
Schlagworte:	Active Transport, Cell Nucleus - drug effects Animals Biological and medical sciences DNA-Binding Proteins - antagonists & inhibitors Forkhead Box Protein O1 Forkhead Transcription Factors General pharmacology Humans Indian Ocean Medical sciences Models, Molecular Molecular Structure Nuclear Magnetic Resonance, Biomolecular Pharmacognosy. Homeopathy. Health food Pharmacology. Drug treatments Phosphoric Monoester Hydrolases - deficiency Phosphoric Monoester Hydrolases - genetics Porifera - chemistry PTEN Phosphohydrolase Transcription Factors - antagonists & inhibitors Tumor Suppressor Proteins - deficiency Tumor Suppressor Proteins - genetics Tyrosine - analogs & derivatives Tyrosine - chemistry Tyrosine - isolation & purification Tyrosine - pharmacology
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Beschreibung
Zusammenfassung:	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.
ISSN:	0163-3864 1520-6025
DOI:	10.1021/np049624z