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Some of the most well known are antiviral drugs widely used to treat HIV/AIDS, hepatitis C and COVID-19. 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.
List of sulfonamides; Author of The Demon Under the Microscope, a history of the discovery of the sulfa drugs; A History of the Fight Against Tuberculosis in Canada (Chemotherapy) Presentation speech, Nobel Prize in Physiology and Medicine, 1939; The History of WW II Medicine "Five Medical Miracles of the Sulfa Drugs".
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]
Thymidine analogue inhibitor Efavirenz: HIV Mylan: NNRTI 1998 Elvitegravir: 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 ...
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.
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.
Antiretroviral drugs are used to manage HIV/AIDS. Multiple antiretroviral drugs are often combined into a single pill in order to reduce pill burden. Some of these combinations are complete single-tablet regimens; the others must be combined with additional pills to make a treatment regimen.
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