PA200 Inhibitors

PA200 inhibitors are compounds designed to target the proteasome activator PA200, also known as PSME4. PA200 is a protein that binds to the 20S core particle of the proteasome, enhancing its peptidase activities independently of ubiquitination. It plays a crucial role in processes such as DNA repair, spermatogenesis, and the regulation of protein turnover by modulating the degradation of specific proteins. Inhibiting PA200 can influence proteasomal function, affecting the degradation of substrates and altering cellular processes dependent on protein degradation pathways.

The chemical class of PA200 inhibitors includes molecules engineered to interact specifically with functional domains of the PA200 protein. These compounds are designed to bind to regions critical for PA200's interaction with the 20S proteasome or its activation mechanisms. Development of these inhibitors involves techniques such as structure-based design, computational modeling, and high-throughput screening to identify molecules with high specificity and affinity for PA200. Researchers utilize these inhibitors as valuable tools to study the molecular mechanisms of proteasome regulation, protein degradation pathways, and the broader implications of PA200 activity in cellular physiology.