Abstract
The first small molecule agonists of the estrogen-related receptors have been identified. GSK4716 (3) and GSK9089 (4) show binding to ERRgamma with remarkable selectivity over the classical estrogen receptors. Notably, in cell-based reporter assays, 3 mimics the protein ligand PGC-1alpha in activation of human ERRbeta and ERRgamma.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Binding, Competitive
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Estrogen Receptor beta / agonists*
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Estrogen Receptor beta / genetics
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Fluorescence Resonance Energy Transfer
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Genes, Reporter
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HeLa Cells
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Heat-Shock Proteins / biosynthesis
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Humans
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Hydrazines / chemical synthesis*
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Hydrazines / chemistry
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Hydrazines / pharmacology
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Ligands
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Molecular Mimicry
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Peroxisome Proliferator-Activated Receptor Gamma Coactivator 1-alpha
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Phenols / chemical synthesis*
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Phenols / chemistry
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Phenols / pharmacology
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Receptors, Estrogen / agonists*
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Receptors, Estrogen / genetics
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Structure-Activity Relationship
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Transcription Factors / biosynthesis
Substances
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Estrogen Receptor beta
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Heat-Shock Proteins
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Hydrazines
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Ligands
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PPARGC1A protein, human
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Peroxisome Proliferator-Activated Receptor Gamma Coactivator 1-alpha
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Phenols
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Receptors, Estrogen
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Transcription Factors
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estrogen receptor gamma