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Updated: Jun 20, 2026

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Published on: November 29, 2014
A mass spectrometry based functional assay for the quantitative assessment of ABC transporter activity
Mária Katona1, Katalin Kiss, Vilmos Angyal
1Institute of Enzymology, Hungarian Academy of Sciences, H-1113 Budapest, Hungary.
Abstract:
ATP-Binding Cassette (ABC) transporters are highly expressed in pharmacological barriers limiting the access of drugs to their targets. Since characterization of a compound as a transporter substrate or inhibitor bears significant consequences in drug development, there is a great need for reliable tools that enable the rapid analysis of the transport susceptibility of drugs. Here we describe a simple but very efficient high-performance liquid chromatography/mass spectrometry (HPLC/MS) assay for measuring the ABC transporter-dependent vesicular transport of compounds. In addition, we provide evidence that the requirement for sample preparation can be minimized using desorption electrospray ionization (DESI)-MS, paving the way for a direct, high-throughput investigation of drug-transporter interactions.
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