High-throughput flow cytometry to detect selective inhibitors of ABCB1, ABCC1, and ABCG2 transporters

Assay and Drug Development Technologies
Irena Ivnitski-SteeleBruce S Edwards

Abstract

Up-regulation of pump (transporter) expression and selection of resistant cancer cells result in cancer multidrug resistance to diverse substrates of these transporters. While more than 48 members of the ATP binding cassette (ABC) transporter superfamily have been identified, up to now only three human ABC transporters-ABCB1, ABCC1, and ABCG2-have unambiguously been shown to contribute to cancer multidrug resistance. The use of low-toxicity and high-specificity agents as a targeted transporter inhibition strategy is necessary to effectively overcome multiple drug resistance. An objective of the present studies was to develop and validate HyperCyt (IntelliCyt, Albuquerque, NM) flow cytometry high-throughput screeening assays to assess the specificity of test compounds that inhibited transporters as an integral part of the screen. Two separate duplex assays were constructed: one in which ABCB1 and ABCG2 transporters were evaluated in parallel using fluorescent J-aggregate-forming lipophilic cation 5,5',6,6'-tetrachloro-1,1',3,3'-tetraethylbenzimidazolcarbocyanine iodide as substrate, and the other in which ABCB1 and ABCC1 transporters were evaluated in parallel using fluorescent calcein acetoxymethyl ester as substrate. ABCB1-exp...Continue Reading

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Citations

Jun 25, 2009·Assay and Drug Development Technologies·Kyle R BrimacombeKing-Leung Fung
Feb 4, 2009·Assay and Drug Development Technologies·Mark M HammerPeter O Krutzik
Nov 6, 2010·Assay and Drug Development Technologies·Christopher B BlackR Terry Dunlay
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