Abstract
Estrogen receptor ERalpha and ERbeta heterodimerization has been implicated in cancer chemoprevention. The discovery, structural elucidation, and total synthesis of a new natural product, actinopolymorphol A (1), from Actinopolymorpha rutilus (YIM45725) that preferentially induces ERalpha/beta heterodimerization is reported. Total synthesis of 1 has allowed us to determine its absolute stereochemistry and that of a previously known deacetylated congener, and 1 represents the first member of a new class of natural products not previously recognized to modulate ER function.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetates / chemical synthesis*
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Acetates / chemistry
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Acetates / pharmacology*
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Actinomycetales / chemistry*
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Estrogen Receptor Modulators / chemical synthesis*
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Estrogen Receptor Modulators / chemistry
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Estrogen Receptor Modulators / pharmacology*
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Estrogen Receptor alpha / metabolism*
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Estrogen Receptor beta / metabolism*
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Molecular Structure
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Phenols / chemical synthesis*
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Phenols / chemistry
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Phenols / pharmacology*
Substances
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Acetates
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Estrogen Receptor Modulators
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Estrogen Receptor alpha
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Estrogen Receptor beta
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Phenols
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actinopolymorphol A