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US 5,700,682 AGranted
Mechanism based screen for retinoid X receptor agonists and antagonists
AssigneeAmerican Cyanamid Company
InventorsPaul Mak, Sotirios K. Karathanasis
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AssigneeAmerican Cyanamid Company
InventorsPaul Mak, Sotirios K. Karathanasis
Estimating the term…
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.
A prokaryotic or eukaryotic host cell stably transformed or transfected by an expression vector containing a cDNA sequence encoding a retinoid X receptor and a reporter plasmid containing an apolipoprotein AI gene site A mutant comprising a nucleotide sequence selected from the group consisting of SEQ ID NOS:
An HB101 strain of E. coli carrying the reporter plasmid identified as M6!-41AI.CAT, having the ATCC designation number 69169.
An HB101 strain of E. coli carrying the reporter plasmid identified as M4!-41AI.CAT, having the ATCC designation number 69170.
An HB101 strain of E. coli carrying the reporter plasmid identified as M3!-41AI.CAT, having the ATCC designation number 69168.
A gene sequence comprising a nucleotide sequence comprising two TGACC imperfect direct repeats separated by the trinucleotide spacer CCT having the nucleotide sequence of SEQ ID NO:
A gene sequence comprising a nucleotide sequence comprising two TGACC imperfect direct repeats separated by the trinucleotide spacer TTT having the nucleotide sequence of SEQ ID NO:
Dependencies are inferred from the claim text.