Yusenko, Maria; Jakobs, Anke; Klempnauer, Karl-Heinz: A novel cell-based screening assay for small-molecule MYB inhibitors identifies podophyllotoxins teniposide and etoposide as inhibitors of MYB activity
Inhalt
- Designing a cell-based screening system for inhibitors of human MYB.
- Screening of a natural compound library.
- Teniposide induces myeloid differentiation of NB4 cells in a MYB-dependent manner.
- Figure 1 Development of a luciferase-based MYB reporter cell line.
- Figure 2 Screening the “Natural product set III” with Hek-Myb-Luc cells.
- Figure 3 Myb-inhibitory activity of selected compounds.
- Figure 4 Analysis of teniposide-induced differentiation and cell death of NB4 cells.
- Figure 5 Teniposide down-regulates MYB expression in myeloid leukemia cell lines.
- Discussion
- Figure 6 Inhibition of MYB activity by teniposide is mediated by DNA-damage signaling.
- Methods
- Cells and compounds.
- Construction of the Hek-Myb-Luc and Hek-Luc reporter cell lines.
- Transfections.
- Lentiviral infection.
- Viability assays.
- Flow cytometry.
- Protein and RNA analysis.
- Acknowledgements