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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:
Pages in category "HIV protease inhibitors" The following 16 pages are in this category, out of 16 total. This list may not reflect recent changes. A. Amprenavir;
HIV protease inhibitors work by specifically binding to the active site by mimicking the tetrahedral intermediate of its substrate and essentially becoming “stuck,” disabling the enzyme. After assembly and budding, viral particles lacking active protease cannot mature into infectious virions.
Tipranavir is a nonpeptidic HIV-1 protease inhibitor [11] and reached the market in 2005. [18] Unlike other HIV protease inhibitors on the market, tipranavir was developed from a nonpeptidic coumarin template and its antiprotease activity was discovered by high-throughput screening. [23]
Protease inhibitors block the viral protease enzyme necessary to produce mature virions upon budding from the host membrane. Particularly, these drugs prevent the cleavage of gag and gag/pol precursor proteins. [16] Virus particles produced in the presence of protease inhibitors are defective and mostly non-infectious.
Pepstatin is an inhibitor of aspartate proteases. [1] Classification. Five superfamilies (clans) ... HIV-1 protease – a major drug-target for treatment of HIV;
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.
It is of the protease inhibitor (PI) class and works by blocking HIV protease. [2] Atazanavir was approved for medical use in the United States in 2003. [2] It is on the World Health Organization's List of Essential Medicines. [9] It is available as a generic medication. [10]
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