Skip to main content
. 2020 Dec 3;21(23):9226. doi: 10.3390/ijms21239226

Figure 3.

Figure 3

Schematic diagrams illustrating the different fluorescence-based assays developed over the past decade for high-throughput screening (HTS) of chemical libraries for the selection of inhibitors of either the AP-lyase activity [193] (A), the DNA glycosylase activity [197] (B) of DNA glycosylases, or of the interaction interface (C) between a DNA glycosylase (here, NTH1) and its cellular partner (YB1) [162]. FRET: Förster resonance energy transfer. In (A), X denotes a damaged base processed by DNA glycosylases. Cleavage by the AP lyase activity results in the release of the fluorophore-labeled lesion-containing strand and fluorescence emission (red F). In (B), release of a modified 8-oxo-G base (oG) linked to a quencher that specifically quenches the highly fluorescent DNA base analogue, tCo, covalently bound to the neighboring base, leads to fluorescence emission (red C). In (C), NTH1-YB1 complex formation is associated with high FRET levels, which are significantly reduced by inhibitors (red wedge) of the PPI interface.