Proteasome inhibitor

Proteasome inhibitors (INN stem –zomib)^[1] are drugs that block the action of proteasomes. Proteasomes are large proteins complexes that are used to break down other proteins. These inhibitors are being studied for the treatment of cancer. Drugs such as bortezomib, carfilzomib, and ixazomib are already approved for use in treating multiple myeloma and mantle cell lymphoma. They also work as immunosuppressants and inhibit bone resorption.^[2]

Proteasome inhibitors are most commonly categorized into two different groups; Synthetic Analogs and Natural products. Synthetic inhibitors are compounds that are all peptide based such as peptide... benzamides, alpha-ketoamides, aldehydes, alpha-ketoaldehydes, vinyl sulfones, and boronic acids. The Natural product inhibitors do not have all of the same core structures and pharmacophores, these natural products are just as selective and potent as the synthetic inhibitors for example lactacystin.^[3] Lactacystin is a natural proteasome inhibitors, that was discovered because of its ability to inhibit the cell lines progression, by targeting the 20S proteasome.^[4] Another example of a natural inhibitor would be PI31, it natural occurs in the human body and is used to maintain proteostasis.^[5]