Protease inhibitors broadly refer to substances that bind to some functional groups on the active center of protease molecules, causing a decrease or even disappearance of protease activity, but do not cause denaturation of enzyme proteins. Leucopeptin, analgesic, chymotrypsin, elastasin aldehyde, pepsin, and phosphoramide were isolated from the fermentation broth of actinomycetes, which can respectively inhibit various proteases such as trypsin, papain, chymotrypsin, elastase, pepsin, and metalloproteinase. All belong to protease inhibitors.
The characteristics of protease inhibitors:
It is a peptide based compound that either competitively inhibits protease activity or acts as an inhibitor of complementary protease activity sites. Such drugs can inhibit the activity of protease, which mainly acts on the later stage of AIDS virus replication. Because protease is inhibited, DNA formed from infected CD4 nuclei cannot be aggregated and released.
The mechanism of action of protease inhibitors:
The precursor proteins encoded by H IV retroviral genes need to be cleaved into functional structural proteins under the action of proteases in order to assemble into complete viral particles. Protease inhibitors can bind with viral protease catalytic genes to inhibit enzyme activity, leading to the inability of protein precursors to lyse and form mature viral bodies.
Interaction of protease inhibitors:
This product can be used in combination with ritonavir to enhance its efficacy, and is used to treat H IV that is ineffective with other antiretroviral therapies.
When breaking cells to extract proteins, proteases can be released, which need to be rapidly inhibited to keep the proteins from being degraded. During the protein extraction process, protease inhibitors need to be added to prevent protein hydrolysis. Here are 5 commonly used protease inhibitors and their respective characteristics of action, as the sensitivity of each protease to different proteins varies, it is necessary to adjust the concentration of each protease. Due to the extremely low solubility of protease inhibitors in liquid, it is particularly important to mix well when adding protease inhibitors to the buffer to reduce the precipitation of protease inhibitors.
anti-viral drug screening TMPRSS2 protease inhibitor test
