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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:
Ritonavir is a protease inhibitor, though it now mainly serves to boost the potency of other protease inhibitors. [8] [9] It may also be used in combination with other medications to treat hepatitis C and COVID-19. [10] [11] It is taken by mouth. [8]
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. Theories considering the effect of protease inhibitors ...
Potato carboxypeptidase inhibitor; Protease inhibitor (pharmacology) Proteinase inhibitors in plants; S. SSI protease inhibitor; Symplocamide A; T.
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 ]
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 ...
In competitive inhibition, the inhibitor binds to the active site, thus preventing enzyme-substrate interaction. In non-competitive inhibition, the inhibitor binds to an allosteric site, which alters the active site and makes it inaccessible to the substrate. Examples of protease inhibitors include: Serpins; Stefins; IAPs
The protease inhibitor ABT-493 and the next-generation NS5A inhibitor ABT-530 are considered active against all HCV genotypes, including the hard to treat genotype 3. [ 42 ] [ 59 ] In vitro, ABT-530 showed potency against the resistance associated variants which are immune to the first generations of NS5A inhibitors, including ledipasvir ...
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