Proteasome inhibitor

Proteasome inhibitors are a class of drugs that block the action of proteasomes, large protein complexes that degrade unneeded or damaged proteins within cells. They are used in the treatment of cancer, particularly multiple myeloma and mantle cell lymphoma.

Mechanism of action

Proteasome inhibitors work by blocking the proteolytic activity of the 26S proteasome, a large protein complex that degrades unneeded or damaged proteins within cells. This leads to an accumulation of unwanted proteins in the cell, which can trigger apoptosis, or programmed cell death. This is particularly effective in cancer cells, which often rely on the proteasome to degrade proteins that would otherwise suppress tumor growth.

Clinical use

Proteasome inhibitors are used in the treatment of certain types of cancer. The first proteasome inhibitor to be approved by the FDA was Bortezomib, which is used in the treatment of multiple myeloma and mantle cell lymphoma. Other proteasome inhibitors that have been approved for use include Carfilzomib and Ixazomib.

Side effects

Like all drugs, proteasome inhibitors can have side effects. These can include fatigue, nausea, diarrhea, and peripheral neuropathy. In some cases, these side effects can be severe and may require the dose of the drug to be reduced or the treatment to be stopped.

Research

Research is ongoing into the use of proteasome inhibitors in the treatment of other types of cancer, as well as other diseases. For example, studies have suggested that proteasome inhibitors may be effective in the treatment of rheumatoid arthritis and Alzheimer's disease.

See also

• Chemotherapy
• Targeted therapy

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Proteasome_inhibitor

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  Bortezomib structure

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  Carfilzomib structure

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  Ixazomib structure