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Screen for drugs targeted

This colorimetric technique is widely used to screen for drugs and metabolites. In EMIT, a complex between an enzyme and the target drug is created so that the enzyme retains its catalytic activity in a conversion reaction such... [Pg.125]

Figure 5, Primary screen far drugs targeted to the APP S untranslated region. In a screen of a library of 1,200 FDA-pre-approved compounds phenserine(ACHEi) and the potent intracellular iron chelator, desferrioxamine, were the validated positive control drugs that suppressed APP mRNA translation through APP 5 UTR sequences. In this transfection based screen several lead APP-5 UTR directed drugs were identified to limit luciferase gene expression driven by the APP 5 UTR. As an internal selectivity control for this screen, downstream dicistronic GFP gene expression (at the translational level by a viral internal ribosome entry site (IRES)) was unresponsive to drug action. Several leads (i,e, dimercaptopropanol) were identified to be chelators as described. Figure 5, Primary screen far drugs targeted to the APP S untranslated region. In a screen of a library of 1,200 FDA-pre-approved compounds phenserine(ACHEi) and the potent intracellular iron chelator, desferrioxamine, were the validated positive control drugs that suppressed APP mRNA translation through APP 5 UTR sequences. In this transfection based screen several lead APP-5 UTR directed drugs were identified to limit luciferase gene expression driven by the APP 5 UTR. As an internal selectivity control for this screen, downstream dicistronic GFP gene expression (at the translational level by a viral internal ribosome entry site (IRES)) was unresponsive to drug action. Several leads (i,e, dimercaptopropanol) were identified to be chelators as described.
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Drug Screens

Drugs screening

Drugs targeting

Screening for

Screening target

Targeted drugs

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