Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
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Kinetic Characterization of Sulfasalazine Transport by Human ATP-Binding Cassette G2
Márton JaniPál SzabóEmese KisÉva MolnárHristos GlavinasPéter Krajcsi
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2009 Volume 32 Issue 3 Pages 497-499

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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 μM and 0.66±0.08 μM were obtained at pH 7.0 and pH 5.5, respectively.

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© 2009 The Pharmaceutical Society of Japan
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