Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives
Patent
1995-06-06
1998-02-03
Ulm, John
Organic compounds -- part of the class 532-570 series
Organic compounds
Carbohydrates or derivatives
435 71, 435 691, 4352523, 4353201, 530300, 530350, 536 231, 536 235, 536 241, C07H 2104
Patent
active
057145954
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.
REFERENCES:
Rottman et al., Molecular and Cellular Biology, 11:3814-3820 (1991).
Windom et al., Molecular and Cellular Biology, 12:3380-3389 (1992).
Karathansis: "Apolipoprotein AI gene regulation by members of the steroid/thyroid hormone . . . ", pp. 21-32 of High density lipoproteins and atherosclerosis III, (Miller et al. eds. 1992).
Ladias et al. (1991) Science. 251:561-565.
Karathanasis Sotirios K.
Mak Paul
American Cyanamid Company
Barnhar Elizabeth M.
Sorensen Kenneth A.
Tsevdos Estelle J.
Ulm John
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