Abstract
A series of 5-substituted 2-benzoylaminobenzoic acids has been synthesized and assayed for PPARalpha/gamma activity. Both dual activators and selective PPARgamma agonists have been identified. This class of compounds was shown to activate the PPARgamma receptor through interaction with a novel binding site.
MeSH terms
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Aminobenzoates / chemical synthesis*
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Aminobenzoates / pharmacology*
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Binding Sites
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Crystallography, X-Ray
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Humans
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Receptors, Cytoplasmic and Nuclear / agonists*
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Receptors, Cytoplasmic and Nuclear / genetics
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Structure-Activity Relationship
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Transcription Factors / agonists*
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Transcription Factors / genetics
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Transcriptional Activation / drug effects
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Transfection
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Tumor Cells, Cultured
Substances
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Aminobenzoates
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Receptors, Cytoplasmic and Nuclear
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Transcription Factors