Abstract
Benzopyran selective estrogen receptor beta agonist-1 (SERBA-1) shows potent, selective binding and agonist function in estrogen receptor beta (ERbeta) in vitro assays. X-ray crystal structures of SERBA-1 in ERalpha and beta help explain observed beta-selectivity of this ligand. SERBA-1 in vivo demonstrates involution of the ventral prostate in CD-1 mice (ERbeta effect), while having no effect on gonadal hormone levels (ERalpha effect) at 10x the efficacious dose, consistent with in vitro properties of this molecule.
MeSH terms
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Animals
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Binding Sites
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Crystallography, X-Ray
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Estrogen Receptor alpha / chemistry
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Estrogen Receptor beta / agonists*
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Estrogen Receptor beta / chemistry
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Estrogens
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Flavonoids / chemical synthesis*
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Flavonoids / chemistry
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Flavonoids / pharmacology
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Humans
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Ligands
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Male
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Mice
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Models, Molecular
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Molecular Structure
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Prostate / drug effects
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Prostate / pathology
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Prostatic Hyperplasia / drug therapy*
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Prostatic Hyperplasia / pathology
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Selective Estrogen Receptor Modulators / chemical synthesis*
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Selective Estrogen Receptor Modulators / chemistry
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Selective Estrogen Receptor Modulators / pharmacology
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Structure-Activity Relationship
Substances
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Estrogen Receptor alpha
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Estrogen Receptor beta
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Estrogens
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Flavonoids
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Ligands
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SERBA-1 compound
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Selective Estrogen Receptor Modulators