Friday, March 30, 2012

Focus on: The Fluorosome Company Pgp Inhibition Screening Assay.

  Principle of the Fluorosome®-trans-pgp Assay
In a forthcoming issue of “The Journal of Pharmacological and Toxicological Methods,” GLSynthesis, parent of The Fluorosome Company, in collaboration with Merck and Company describe the study used to validate its new, innovative Pgp inhibition assay, Fluorosome®-trans-pgp. This unique new technology promises to revolutionize the Pgp screening process by employing the novel Fluorosome® platform for the testing of drug efflux transporters.

In its paper, “Determining P-glycoprotein-drug interactions: evaluation of reconstituted Pglycoprotein in a liposomal system and LLC-MDR1 polarized cell monolayers,” the authors describe the validation study for this fast, simple, highly specific method that provides more accurate, efficient and cost effective Pgp/drug interaction determinations to accelerate drug discovery.

Corresponding author, Donald Melchior, PhD, of GLSynthesis/The Fluorosome Company summarizes the validation results as follows: “For the first time, we publish validation of the high throughput transporter assay system that enables definitive measurement of Pgp activity and its inhibition in real time. The platform is simple to use, offers rapid throughput, has no requirement for sterility, consumes very small quantities of test drug and is amenable to robotics.”

“We have demonstrated that for a large panel of test compounds, IC50 values resulting from this assay are consistent with their binding affinities to Pgp and are in agreement both with data from cell monolayer-based assays and published results of human in vivo drug-drug interaction studies using digoxin. Fluorosome®-trans-pgp is the first of a series of drug transporter-lipid vesicle constructs that can be used for high throughput screening of drugs and potential drug candidates, and for research into the mechanisms of substrate transport and drug-drug interactions. It offers a cost-effective approach relative to cell culture methodologies, and obviates many of the inherent complications and ambiguities inherent in cell-based systems.”

In this paper, the NOVOstar with MARS software is used for this novel assay. The Fluorosome®-trans-pgp assay can also be measured with superior performance on the Omega Series and PHERAstar FS. You can also read more about this application performed on the FLUOstar Omega in BMG LABTECH’s Application Note 208: A Fast and Simple Method For Measuring P-Glycoprotein (Pgp) Inhibition.

For more information on this assay, read the application note at: http://www.bmglabtech.com/application-notes/fluorescence-intensity/fluorosome-pgp-fluostar-omega-208.cfm
or visit http://www.fluorosome.com

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