Fluorosome R&D
Fluorosome-based assays for functional drug transporters inserted in the membrane are under active development. Specifically, Fluorosome-trans-pgp has been created to measure the extent to which drug candidates are inhibitors and/or substrates of the p-glycoprotein (MDR1, ABCB1) drug efflux pump. The p-glycoprotein is the dominant ATP-driven membrane transporter regulating drug distribution in the body. Currently, Fluorosome-trans-pgp is available for assaying inhibitors of p-glycoprotein at both the H and R drug transport sites.
Fluorosome-trans-pgp assay consists of Fluorosome-trans vesicles in which pgp has been reconstituted into the membrane bilayer (see Figure). The transbilayer active transport of a drug by pgp is measured in real time by fluorescence changes after addition of ATP. Inhibition at one or both sites is determined by reduction in the fluorescence change in the presence of a test compound.
The Fluorosome-trans-pgp system is being developed to measure active transport of test compounds, and additionally will be used to determine equilibrium parameters (Km, Ki) for substrates and inhibitors.
Scientists from GLSynthesis (Donald L. Melchior, George E. Wright and Steven E. Wright) and the University of Guelph, Guelph, Ontario (Frances J. Sharom and Rohngua Lui), presented a poster entitled "Reconstituted P-glycoprotein in Fluorosome® lipid bilayer vesicles - basis for an in vitro P-glycoprotein assay.” at the abcam sponsored “Mulitdrug Resistance and ABC Transporters Conference” in Baltimore, Maryland on November 5, 2008.
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