Insights into PARP Inhibitors' Selectivity Using Fluorescence Polarization and Surface Plasmon Resonance Binding Assays

In this study, we describe the development and validation of binding assays based on fluorescence polarization (FP) and surface plasmon resonance (SPR) techniques. PARP-1, PARP-2, PARP-3, and TNKS-1 FP displacement assays are set up by employing ad hoc synthesized probes. These assays are suitable for high-throughput screening (HTS) and selectivity profiling, thus allowing the identification of NAD+ binding site selective inhibitors. The PARP-1 and PARP-2 complementary SPR binding assays confirm displacement data and the in-depth inhibitor characterization. Moreover, these formats have the potential to be broadly applicable to other members of the PARP family.

Source: Journal of Biomolecular Screening - August 5, 2014 Category: Molecular Biology Authors: Papeo, G., Avanzi, N., Bettoni, S., Leone, A., Paolucci, M., Perego, R., Quartieri, F., Riccardi-Sirtori, F., Thieffine, S., Montagnoli, A., Lupi, R. Tags: Technical Notes Source Type: research