Small Molecule Activation of Procaspase-2 for the Selective Induction of Apoptotic Death in Breast Cancer Cells.

摘要

We have synthesized a library of compounds based on a previously identified procaspase-2 activator. These compounds were then tested for their ability to activate procaspase-2 in vitro. The results from these tests indicated that several of the compounds did indeed activate procaspase-2. Testing of these active compounds against a panel of enzymes then revealed, surprisingly, that the compounds are general enzyme activators. We have now explored this phenomena of general enzyme activation more thoroughly and have submitted a manuscript on the topic. The data and knowledge acquired through this work now allows us to move confidently to a high-throughput screen to identify truly specific procaspase-2 activators.