Definition

A cell penetrating and interfering peptide composed of a cell-penetrating part that delivers the peptide into the cellular cytosol and an interfering part that inhibits the interaction between the proteins intracellular caspase-9 and protein phosphatase 2A (PP2A) proteins, with potential antineoplastic activity. Upon administration, the cell-penetrating part of capsase-9-PP2A interaction inhibitor PEP-010 delivers the peptide into the cellular cytosol and the interfering part of PEP-010 disrupts the interaction between intracellular caspase-9 and PP2A. This leads to the release and the activation of caspase-9, thereby restoring tumor cell apoptosis. Activated caspase-9 is involved in the induction of caspase-dependent apoptosis. PP2A, a serine/threonine phosphatase, plays a key role in the control of cell growth and DNA damage repair.