Development and Therapeutic Potential of Calpain Inhibitors

摘要: Publisher Summary This chapter presents evidence that calpain over activation may be a key component in number of disorders. The common theme for most these disorders is cellular Ca2+ overload. calpains can found the cytosolic compartment and also identified plasma membrane other organelle membranes. Both isoforms contain two subunits. Calpain appears to an ideal pharmaceutical target, as this protease active during pathological events. current challenge identify cell-permeable selective inhibitors evaluation various vivo disease models. As knowledge substrate specificity increasing from natural products screening programs are becoming available, more designed synthesized. At present there arsenal disposal. These include protein inhibitors, such calpastatin, irreversible peptide E64 analogs, reversible peptidyl α-keto amides, several nonpeptide inhibitors. With recent emergence goal understanding physiological roles possible achievable.