Proteasome Inhibitors

A drug can be classified by the type of chemical of the energetic ingredient or by the nature in which it is used in treating a particular ailment. Each drug can classified into one or more drug classes. Proteasome is defined as a multi-unit enzyme complex found in the cytoplasm as well as the nucleus of all eukaryotic cells. It is responsible for degradation of damaged or unneeded intracellular proteins by proteolysis that is a chemical reaction that helps break peptide bonds. Proteins, which are to be destroyed, are easily recognized by proteasomes because of the existence of ubiquitin conjugated to the targeted protein. The ubiquitin-proteasome pathways play a crucial part in regulating concentration of the intracellular of specific proteins, thus maintaining homeostasis within the cells. Proteasome inhibitors help to avoid decomposition of these proteins, which can affect multiple signaling cascades within the cell. This form of disruptions of normal homeostasis mechanisms can lead to cell death. Inhibition of Proteasome also presents a very promising approach to cancer therapy by targeting the proteasome function in tumor cells specifically. These inhibitors can also be used alone or together with other cancer therapies in order to sensitize tumor cells and improve therapeutic benefits.

Proteasome Inhibitors Drugs

Below you will find a list of drugs that fall under the class of Proteasome Inhibitors

  • Lactacystin
  • Bortezomib/ PS-341
  • Velcade
  • Ritonavir
  • Kyprolis
  • Disulfiram
  • Salinosporamide A
  • Epigallocatechin-3-gallate
  • carfilzomib
  • CEP-18770
  • ONX 0912
  • MLN9708

Proteasome Inhibitors Uses

The functions of proteasome inhibitors include;

  • Digestion of unassembled proteins
  • Generation of peptides identifiable by the immune system
  • Digestion of unassembled proteins
  • Regulation of the cellular lifespan regulatory proteins such as those that control the cell cycle.

Proteasome Inhibitors Side Effects

Proteasome can have some common side effects such as;

  • Fatigue, weakness
  • Nausea
  • Weight loss
  • Fever
  • Diarrhoea
  • Constipation
  • Anaemia
  • Low platelet counts

Others include;

  • Affect processes of metabolism in patients, with unpredictable results such as high blood sugar and subsequent development of diabetes.
  • Alters with how the body absorb nutrients including fats. This process is called lipodystrophy and results in altered fat distribution.
  • Increased levels of fat in the blood stream with results such as cardiovascular disease or pancreatitis
  • Liver toxicity for those with those existing with liver disease like chronic viral hepatitis.

Proteasome Inhibitors Interactions

Proteasome inhibitor Bortezomib is known to interact contrary to high-risk myelodysplastic syndrome (MDS) cells in vitro and vivo. The result is that Bortezomib could induce growth arrest and also apoptosis in high-risk MDS cells in vitro and vivo. Also, it has a synergistic effect with AraC and DNR which are the two chemotherapeutic agents.

Similarly, Proteasome inhibitor bortezomib can be interacted with other apoptotic stimuli, including cytotoxic chemotherapy and tumor necrosis factor-related apoptosis-inducing ligand in prostate cancer. The result is that Bortezomib induces death of cells of androgen-dependent and independent prostate cancer lines.

Main Proteasome Inhibitors Drugs

Velcade Bortezomib

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