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Protease inhibitors were the second class of antiretroviral drugs developed. The first members of this class, saquinavir , ritonavir , and indinavir , were approved in late 1995–1996. Within 2 years, annual deaths from AIDS in the United States fell from over 50,000 to approximately 18,000 [ 5 ] Prior to this the annual death rate had been ...
Protease inhibitors may be classified either by the type of protease they inhibit, or by their mechanism of action. In 2004 Rawlings and colleagues introduced a classification of protease inhibitors based on similarities detectable at the level of amino acid sequence. [ 4 ]
Potato carboxypeptidase inhibitor; Protease inhibitor (pharmacology) Proteinase inhibitors in plants; S. SSI protease inhibitor; Symplocamide A; T.
Protease inhibitors can alter adipocyte metabolism causing lipodystrophy, a common side effect associated with the use of most HIV protease inhibitors. Many mechanisms have been proposed, for example inhibition of adipocyte differentiation , triglyceride accumulation and increased lipolysis .
Other examples of these substrate mimics are the protease inhibitors, a therapeutically effective class of antiretroviral drugs used to treat HIV/AIDS. [43] [44] The structure of ritonavir, a peptidomimetic (peptide mimic) protease inhibitor containing three peptide bonds, as shown in the "competitive inhibition" figure above. As this drug ...
Epoxomicin is a naturally occurring selective inhibitor. [15] MG132 is a synthesized peptide commonly used for in vitro studies. Beta-hydroxy beta-methylbutyrate is a proteasome inhibitor in human skeletal muscle [16] [17] in vivo. [18] PI31 acts as a 20S proteasome inhibitor used for proteostasis that occurs naturally in the human body. [19]
Saquinavir is a protease inhibitor. Proteases are enzymes that cleave protein molecules into smaller fragments. HIV protease is vital for both viral replication within the cell and release of mature viral particles from an infected cell.
Examples of Kunitz-type protease inhibitors are aprotinin (bovine pancreatic trypsin inhibitor, BPTI), Alzheimer's amyloid precursor protein (APP), and tissue factor pathway inhibitor (TFPI). Kunitz STI protease inhibitor, the trypsin inhibitor initially studied by Moses Kunitz, was extracted from soybeans. Standalone Kunitz domains are used as ...