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

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Jani M, Szabo P, Kis E, Molnar E, Glavinas H, Krajcsi P

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

Biol Pharm Bull. 2009 Mar;32(3):497-9.

PubMed ID

19252303 [ View in PubMed

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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 microM and 0.66 +/- 0.08 microM were obtained at pH 7.0 and pH 5.5, respectively.

DrugBank Data that Cites this Article

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Mitoxantrone	ATP-binding cassette sub-family G member 2	Protein	Humans	Unknown	Substrate	Details