Abstract
Aromatic retinoids having a meta-substituted aromatic ring bridge, such as 4-[3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)phenyl]benzo ic acid and its 3,5-diaryl-substituted 4,5-dihydroisoxazole analogue, function as retinoid receptor panagonists by activating both retinoic acid and retinoid X receptors to induce gene transcription, and thereby provide novel scaffolds for retinoid drug development. Both classes of these ligand-inducible transcription factors are involved in mediating the inhibitory effects of retinoids on cancer cell growth.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Benzoates / chemistry
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Benzoates / pharmacology*
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Heterocyclic Compounds / chemistry
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Heterocyclic Compounds / pharmacology*
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Humans
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Naphthalenes / chemistry
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Naphthalenes / pharmacology*
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Receptors, Retinoic Acid / agonists*
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Retinoid X Receptors
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Transcription Factors / agonists*
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Tumor Cells, Cultured
Substances
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4-(3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)phenyl)benzoic acid
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Benzoates
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Heterocyclic Compounds
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Naphthalenes
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Receptors, Retinoic Acid
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Retinoid X Receptors
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Transcription Factors