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A mass spectrometry based functional assay for the quantitative assessment of ABC transporter activity
Author(s) -
Katona Mária,
Kiss Katalin,
Angyal Vilmos,
Kucsma Nóra,
Sarkadi Balázs,
Takáts Zoltán,
Szakács Gergely
Publication year - 2009
Publication title -
rapid communications in mass spectrometry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.528
H-Index - 136
eISSN - 1097-0231
pISSN - 0951-4198
DOI - 10.1002/rcm.4259
Subject(s) - chemistry , transporter , chromatography , mass spectrometry , limiting , atp binding cassette transporter , electrospray ionization , high performance liquid chromatography , biochemistry , mechanical engineering , engineering , gene
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. Copyright © 2009 John Wiley & Sons, Ltd.