HIV protease
| HIV protease | ||
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Existing structural data: s. UniProt entry |
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| Mass / length primary structure | 99 amino acids | |
| Identifier | ||
| External IDs |
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| Enzyme classification | ||
| EC, category | 3.4.23.16 , aspartyl proteases | |
| MEROPS | A02.001 | |
| Substrate | Gag; Gag pole | |
The HIV protease (PR, HIV-Prot) is an enzyme from the group of aspartate proteases . Their genetic information in the RNA - genome of the HIV virus contained. It is necessary for the virus to multiply.
task
The task of the HIV protease is to hydrolytically cleave newly synthesized virus proteins at certain points in the polypeptide chain ( limited proteolysis ). In this way, the virus proteins are converted into their functional form; the proteins are referred to as maturation. Without the HIV protease, new infectious viruses cannot be formed. Therefore, inactivation of the HIV protease - for example by mutating the gene or an inhibitor - interrupts the life cycle of the HIV virus, which can no longer multiply and infect other cells.
Inhibitors
A heptapeptide, which is preferably split between phenylalanine and proline , is sufficient as a possible substrate . Diols as possible inhibitors can mimic the tetrahedral carboxyl hydrate intermediate state in hydrolysis. The active ingredient saquinavir , which is already used in HIV treatment, was developed from the heptapeptide, the alcoholic hydroxyl groups and an increase in the hydrophobic character of the side chains of the terminal amino acids .
Due to the rapid development of resistance in the HI virus, drugs are usually used as a combination (“cocktail”). Other points of attack for drug therapy of an HIV infection are the enzyme reverse transcriptase , preventing the virus from attaching to the cell membrane and fusing with it, as well as the assembly of new viruses in the infected cell.
research
Since the life cycle is interrupted without the HIV protease, the HIV protease is of great scientific interest as a possible starting point for drugs against AIDS . Among other things, the grid computing project FightAIDS @ Home is trying to find a drug that inhibits HIV protease.
literature
- Prevention of viral reproduction. on: nationalacademies.org
Individual evidence
- ^ Fight AIDS at Home. on: fightaidsathome.scripps.edu