PERP (p53 apoptosis effector related to PMP22) Inhibitors

The PERP (p53 apoptosis effector related to PMP22) protein is a critical component in the p53-dependent apoptotic pathway. It is a member of the PMP-22/gas3 family of tetraspan membrane proteins and is transcriptionally activated by the tumor suppressor protein p53. PERP plays a pivotal role in mediating apoptosis, primarily in response to DNA damage and other stressors that activate p53. Its expression leads to changes in membrane integrity and cell-cell adhesion, promoting apoptotic cell death. PERP functions as a part of the intrinsic pathway of apoptosis, contributing to mitochondrial membrane permeabilization. The signaling through PERP is crucial for maintaining genomic stability and tumorigenesis by eliminating damaged cells.

Targeting PERP for disruption or inhibition using small molecules allows for detailed mechanistic studies of p53-mediated apoptosis. By inhibiting PERP, researchers can observe the consequences on apoptosis, particularly in cells where p53 is activated. This approach helps in understanding the precise role of PERP within the broader p53 signaling pathway. It also enables the investigation of PERP's interactions with other proteins involved in apoptosis and cell survival. Disrupting PERP function could elucidate its role in cancer development, where p53 pathways are often dysregulated.