Druggable epigenetic modulators undergo oncogenic mutation and are seen as attractive therapeutic targets. However, inhibition of some epigenetic targets results in a significantly delayed drug response that is not revealed by conventional, short term cell growth assays. To address this issue, we have established two- and three-dimensional assay conditions with extended assay duration to yield robust cell line profiling data. While this assay design was specifically developed with epigenetic targets in mind, other slow-acting therapeutics are likely to reveal themselves employing this extended protocol.
Advantages of OncoPanel™ services for epigenetic studies:
Figure 1. Detection of growth inhibition by EZH2 inhibitors requires extended assay duration
Sensitivity of EZH2 mutant cell lines to the EZH2 inhibitor, GSK343, is increased under an extended assay period, whereas the non-specific kinase inhibitor, staurosporine, shows no preference for EZH2 mutational status or assay duration.