A fast and simple method for measuring P-glycoprotein (Pgp) inhibition

Donald L. Melchior (1), Frances J. Sharom (2), EJ Dell (3) (1) The Fluorosome Company, (2) University of Guelph, (3) BMG LABTECH 04/2010

P-glycoprotein (Pgp; ABCB1) is a member of the ATP binding cassette (ABC) transporters. It exports structurally diverse hydrophobic compounds from the cell driven by ATP hydrolysis. High Pgp expression is linked to the export of anticancer drugs, multidrug resistance and low oral absorption of drugs. Therefore, a novel compound needs to be examined regarding its effect on Pgp.


The Fluorosome®-trans-pgp fluorescent assay, together with BMG LABTECH's microplate readers, provide a rapid, sensitive and specific reconstituted Pgp liposome assay system for identification of compounds that interact with the transporter. The assay measures the ability of a compound to compete with a Pgp substrate for transport, and determines the IC50 value.

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