Cell-based enzymatic assays

Protein methylation is an understudied post-translational modification, but plays an integral role regulating signaling pathways implicated in tumorigenesis. Monitoring protein methyltransferase activity could provide valuable functional information for precision medicine and drug development. Functional testing could be especially powerful in tumors with low mutational burden or “undruggable” activating mutations such as ovarian cancer and KRAS-driven pancreatic cancer. To address this critical need, we are developing cell-deliverable synthetic peptide probes for facile live-cell measurement of endogenous methyltransferase activity.