C - Chemistry – Metallurgy – 12 – N
Patent
C - Chemistry, Metallurgy
12
N
C12N 15/11 (2006.01) C07K 14/705 (2006.01) C07K 14/775 (2006.01) C12N 1/19 (2006.01) C12N 1/21 (2006.01) C12Q 1/34 (2006.01) C12Q 1/68 (2006.01) G01N 33/566 (2006.01)
Patent
CA 2112527
MECHANISM-BASED SCREEN FOR RETINOID X RECEPTOR AGONISTS AND ANTAGONISTS ABSTRACT OF THE DISCLOSURE The present invention describes a novel method for screening retinoid X receptor agonists or antagonists, said method comprising: using a retinoid X receptor expressed by a yeast expression system to screen a compound having retinoid X receptor agonist or antagonist activity. The invention further describes a screen for detecting a compound having retinoid X receptor agonist or antagonist activity, which comprises the steps of (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. Additionally, the invention includes mutated variants of apolipoprotein AI gene site A which respond selectively to the retinoid X receptor or respond to receptors other than RXR.alpha..
Karathanasis Sotirios K.
Mak Paul
American Cyanamid Company
Smart & Biggar
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