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Integrase Allosteric Pocket (HIV)
- Molecular classification
- Protein-protein interaction site
01
Overview
The integrase allosteric pocket in HIV-1 is a specific site on the viral integrase (IN) enzyme that serves as a binding region for allosteric inhibitors. This pocket overlaps with the binding site of the host cellular cofactor LEDGF/p75, which normally tethers integrase to chromatin and facilitates integration of viral DNA into the host genome. ALLINIs bind to this site, inducing aberrant multimerization of IN, disrupting normal assembly with viral DNA, and perturbing maturation of new virions. This results in defective virus particles unable to complete reverse transcription or integrate their genome. Targeting this site offers an alternative therapeutic strategy against HIV, especially for resistant strains.
- Other names
- HIV Integrase Allosteric SiteIntegrase-LEDGF/p75 binding siteIN allosteric pocket
02
Mechanism of action
Induces aberrant integrase multimerization, disrupts virion maturation, inhibits viral integration.
03
Biological functions
Viral integrationVirion maturationLEDGF/p75 bindingIntegrase multimerization
04
Disease associations
HIV infectionAIDS
05
Safety considerations
Potential for resistance developmentToxicity of inhibitors
06
Interacting drugs
ALLINIs
4 more in the full profile.
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