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These protease inhibitors prevent viral replication by selectively binding to viral proteases (e.g. HIV-1 protease) and blocking proteolytic cleavage of protein precursors that are necessary for the production of infectious viral particles. Protease inhibitors that have been developed and are currently used in clinical practice include:
Protease inhibitors and statins taken together may increase the blood levels of statins and increase the risk for muscle injury (myopathy). The most serious form of myopathy, rhabdomyolysis, can damage the kidneys and lead to kidney failure, which can be fatal.
Statine is a gamma amino acid that occurs twice in the sequence of pepstatin, a protease inhibitor that is active against pepsin and other acid proteases. [1] It is thought to be responsible for the inhibitory activity of pepstatin because it mimics the tetrahedral transition state of peptide catalysis. [2]
Specific protease inhibitors including atazanavir (when taken with ritonavir), lopinavir/ritonavir and simeprevir; Alcohol intake should be reduced while on rosuvastatin to decrease the risk of developing liver damage [4] Aluminum and magnesium hydroxide antacids should not be taken within two hours of taking rosuvastatin [4]
Pepstatin A is well known to be an inhibitor of aspartic proteases such as pepsin, cathepsins D and E. Except for its role as a protease inhibitor, however, the pharmacological action of pepstatin A upon cells remain unclear. Pepstatin A suppresses receptor activator of NF-κB ligand (RANKL)–induced osteoclast differentiation.
Pravastatin, sold under the brand name Pravachol among others, is a statin medication, used for preventing cardiovascular disease in those at high risk and treating abnormal lipids. [5] It is suggested to be used together with diet changes, exercise, and weight loss. [5] It is taken by mouth. [5]
Simvastatin, sold under the brand name Zocor among others, is a statin, a type of lipid-lowering medication. [4] It is used along with exercise, diet, and weight loss to decrease elevated lipid levels. [4] It is also used to decrease the risk of heart problems in those at high risk. [4] It is taken by mouth. [4]
Aloxistatin (loxistatin, E-64d, EST) is a drug which acts as a cysteine protease inhibitor and has anticoagulant effects. It is a synthetic analogue of E-64, a natural product derived from fungi.