Mechanism-based screen for retinoid X receptor agonists and anta

Chemistry: molecular biology and microbiology – Measuring or testing process involving enzymes or... – Involving antigen-antibody binding – specific binding protein...

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435 691, 4352523, 4353201, 530300, 530350, 536 231, 536 235, 536 241, G01N 33566

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057006504

ABSTRACT:
A method is described for screening retinoid X receptor agonists or antagonists using a retinoid X receptor expressed by a yeast expression system to screen a compound having a retinoid X receptor agonist or antagonist activity. Another screen is described for detecting a compound having retinoid X receptor agonist or antagonist activity by: (1) providing a yeast strain which expresses the retinoic acid receptor and activates a reporter plasmid containing apolipoprotein AI gene site A or a mutated variant thereof; (2) incubating the compound in suitable media and a colorless chromogenic substrate; and (3) examining the media for development of color. Mutated variants of apolipoprotein AI gene site A which respond selectively to the retinoid X receptor or respond to receptors other than RXR.alpha. are also described.

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Rottman et al., Molecular and Cellular Biology, 11:3814-3820 (1991).
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Karathansis: "Apolipoprotein Al gene regulation by members of the steroid/thyroid hormone . . . ", pp. 21-32 of High density lipoproteins and atherosclerosis III, (Miller et al. eds. 1992).

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