Kinetic characterization of sulfasalazine transport by human ATP-binding cassette G2

Márton Jani, Pál Szabó, Emese Kis, Éva Molnár, Hristos Glavinas, Péter Krajcsi

Research output: Article

27 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)497-499
Number of pages3
JournalBiological and Pharmaceutical Bulletin
Volume32
Issue number3
DOIs
Publication statusPublished - márc. 2009

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ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

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