Abstract
Fluorinated trienoic acid analogues of the RXR selective modulator 1 (LG101506) were synthesized, and tested for their ability to bind RXRalpha and activate RXR homo and heterodimers. Potency and efficacy were observed to be dependent upon the position of fluorination, and improvement in pharmacological profile was demonstrated in some cases.
MeSH terms
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Animals
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Drug Design
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Fluorine Compounds / chemical synthesis*
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Fluorine Compounds / metabolism*
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Fluorine Compounds / pharmacology
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Male
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Mice
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Mice, Inbred ICR
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Receptors, Retinoic Acid / metabolism*
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Retinoid X Receptors
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Retinoids / chemical synthesis
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Retinoids / metabolism
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Retinoids / pharmacology
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Transcription Factors / metabolism*
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Tretinoin / chemical synthesis*
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Tretinoin / metabolism*
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Tretinoin / pharmacology
Substances
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Fluorine Compounds
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Receptors, Retinoic Acid
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Retinoid X Receptors
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Retinoids
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Transcription Factors
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Tretinoin