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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;
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]
HIV Gilead Sciences Integrase inhibitor 2012 (Fixed-dose combo Stribild) 2014 (single pill) 2015 ; Emtricitabine: HIV Gilead Sciences NRTI 2003 Enfuvirtide: HIV Entry inhibitor 2003 Ensitrelvir: COVID-19: Shionogi: 3C-like protease inhibitor Entecavir: HIV NRTI 2005 Etravirine (Intelence) [8] HIV NNRTI 2008 Famciclovir: Herpes Zoster: Guanosine ...
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.
The first HIV protease inhibitor approved by the FDA was saquinavir, which was designed to target wild-type HIV-1 protease. [27] However, this inhibitor is no longer effective due to resistance-causing mutations on the HIV-1 protease structure. The HIV genome has high plasticity, so has been able to become resistant to multiple HIV-1 protease ...
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