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New functional assay of P-glycoprotein activity using Hoechst 33342 by Henrik Müller; Werner Klinkhammer; Christoph Globisch; Matthias U. Kassack; Ilza K. Pajeva; Michael Wiese is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is New functional assay of P-glycoprotein activity using Hoechst 33342 about?
In this study we describe a simplified, HTS-capable functional assay for the multidrug resistance (MDR) transporter Pglycoprotein (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.
Who reads New functional assay of P-glycoprotein activity using Hoechst 33342?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Henrik Müller; Werner Klinkhammer; Christoph Globisch; Matthias U. Kassack; Ilza K. Pajeva; Michael Wiese
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)
- Published
- 2007
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)