Kinetic Characterization of Sulfasalazine Transport by Human ATP-Binding Cassette G2(Pharmacology)

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概要

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• 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 up-take 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 K_m values of 0.70±0.03μM and 0.66±0.08μM were obtained at pH7.0 and pH5.5, respectively.

• 公益社団法人日本薬学会の論文
• 2009-03-01

著者

• Jani Marton

  Solvo Biotechnology

• SZABO Pal

  Chemical Research Centre, Hungarian Academy of Sciences

• KIS Emese

  Solvo Biotechnology

• MOLNAR Eva

  Solvo Biotechnology

• GLAVINAS Hristos

  Solvo Biotechnology

• KRAJCSI Peter

  Solvo Biotechnology

• Szabo Pal

  Chemical Research Centre Hungarian Academy Of Sciences

関連論文

• Kinetic Characterization of Sulfasalazine Transport by Human ATP-Binding Cassette G2(Pharmacology)

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