Abstract
Three novel (1-3) and two known (4-5) scalarane sesterterpenes were isolated from a marine sponge of the genus Spongia. The isolated compounds showed potent inhibition of transactivation for the nuclear hormone receptor, FXR (farnesoid X-activated receptor), which is a promising drug target to treat hypercholesterolemia in humans.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Cell Line
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Cell Proliferation / drug effects
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Chlorocebus aethiops
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DNA-Binding Proteins / antagonists & inhibitors*
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DNA-Binding Proteins / biosynthesis
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DNA-Binding Proteins / genetics
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Magnetic Resonance Spectroscopy / methods
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Magnetic Resonance Spectroscopy / standards
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Molecular Conformation
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Porifera / chemistry*
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Receptors, Cytoplasmic and Nuclear / antagonists & inhibitors*
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Receptors, Cytoplasmic and Nuclear / biosynthesis
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Receptors, Cytoplasmic and Nuclear / genetics
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Reference Standards
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Sesterterpenes
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Stereoisomerism
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Structure-Activity Relationship
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Terpenes / chemistry
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Terpenes / pharmacology*
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Transcription Factors / antagonists & inhibitors*
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Transcription Factors / biosynthesis
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Transcription Factors / genetics
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Transcriptional Activation / drug effects*
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Transfection
Substances
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DNA-Binding Proteins
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Receptors, Cytoplasmic and Nuclear
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Sesterterpenes
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Terpenes
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Transcription Factors
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farnesoid X-activated receptor