Uptake Assay Design

Uptake Transporter-Expressing Cells


To determine if compounds are substrates of uptake transporters, their accumulation in transporter-expressing cells and control cells is measured. To determine if compounds are inhibitors of uptake transporters, the ability of the compound to block the uptake of probe substrates is measured. The test system is attachable host cells (HEK293 or S2 cells) transfected with vectors containing human transporter cDNA. Transport activity is evaluated by comparison of uptake between transporter-expressing cells and control cells. Transporter activity is evaluated by comparison with uptake into control cells.

Identification of a Substrate


Comparison of the uptake activity in the transport-expressing cells and control cells is used to investigate whether the candidate is a substrate of a SLC transporter or not. Km and Vmax are calculated from the relationship between substrate concentration and uptake activity.

         

Identification of an Inhibitor


The inhibitory effect of a drug candidate on the uptake of typical substrates is evaluated by calculating an IC50 determination (concentration causing 50% inhibition of transporter-mediated uptake of the typical substrate).


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SLC (Uptake) Transporters
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