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Updated: Jun 25, 2026

Characterization of Membrane Transporters by Heterologous Expression in E. coli and Production of Membrane Vesicles
Published on: December 31, 2019
Kinetic characterization of sulfasalazine transport by human ATP-binding cassette G2
Márton Jani1, Pál Szabó, Emese Kis
1Solvo Biotechnology, Budaors, Hungary.
Abstract:
The pharmacokinetics of sulfasalazine, an anti-inflammatory drug is influenced by ATP-binding cassette G2 (ABCG2) (breast cancer resistance protein (BCRP), mitoxantrone resistance protein (MXR)) both in vitro and clinically. Due to its low passive permeability, the intracellular concentration of sulfasalazine is dependent on uptake transporters, rendering the characterization of transporter specific interactions in cell based experimental systems difficult. Applying membrane assays a detailed kinetic analysis of sulfasalazine ABCG2 interaction was conducted and Km values of 0.70 +/- 0.03 microM and 0.66 +/- 0.08 microM were obtained at pH 7.0 and pH 5.5, respectively.
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