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New functional assay of P-glycoprotein activity using Hoechst 33342

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2007

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Müller, Henrik
Klinkhammer, Werner
Globisch, Christoph
Kassack, Matthias
Pajeva, Ilza K.
Wiese, Michael

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https://doi.org/10.1016/j.bmc.2007.07.024
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Bioorganic & Medicinal Chemistry. 2007, 15(23), pp. 7470-7479. ISSN 0968-0896. eISSN 1464-3391. Available under: doi: 10.1016/j.bmc.2007.07.024

Zusammenfassung

In this study we describe a simplified, HTS-capable functional assay for the multidrug resistance (MDR) transporter P-glycoprotein (P-gp) based on its substrate Hoechst 33342. The physicochemical properties of Hoechst 33342 and the enormous milieu dependency of its fluorescence intensity allowed performing the assay in a homogeneous manner. This new assay served as an effective tool to estimate the potency of 10 well recognized P-gp substrates and modulators. Further, the potency of these compounds was also estimated in the calcein AM assay. The Hoechst 33342 and calcein AM assays yielded significantly comparable results for all compounds tested. Principal component analysis (PCA) applied to literature data on inhibition of P-gp activity and our results obtained in the Hoechst 33342 and calcein AM assay indicated similarity of compared functional transport assays. However, no correlation could be detected between these functional assays and the ATPase activity assay.

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540 Chemie

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ISO 690MÜLLER, Henrik, Werner KLINKHAMMER, Christoph GLOBISCH, Matthias KASSACK, Ilza K. PAJEVA, Michael WIESE, 2007. New functional assay of P-glycoprotein activity using Hoechst 33342. In: Bioorganic & Medicinal Chemistry. 2007, 15(23), pp. 7470-7479. ISSN 0968-0896. eISSN 1464-3391. Available under: doi: 10.1016/j.bmc.2007.07.024
BibTex
@article{Muller2007-12funct-38289,
  year={2007},
  doi={10.1016/j.bmc.2007.07.024},
  title={New functional assay of P-glycoprotein activity using Hoechst 33342},
  number={23},
  volume={15},
  issn={0968-0896},
  journal={Bioorganic & Medicinal Chemistry},
  pages={7470--7479},
  author={Müller, Henrik and Klinkhammer, Werner and Globisch, Christoph and Kassack, Matthias and Pajeva, Ilza K. and Wiese, Michael}
}
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