Mechanism

HIV integrase

Assets acting on this target.

Class
Integrase strand transfer inhibitor (INSTI)

HIV integrase is a viral enzyme that the human immunodeficiency virus requires to insert its genetic material into the DNA of an infected cell. After HIV enters a cell and its RNA genome is converted into DNA by another viral enzyme (reverse transcriptase), that DNA must be permanently spliced into the host chromosome for the virus to establish infection and direct the cell to produce new viral particles. Integrase catalyzes this splicing step. Because integrase has no close human counterpart and performs a function essential to the viral life cycle, it is an attractive and highly selective drug target. Integrase strand transfer inhibitors block the final catalytic step of this insertion process, preventing viral DNA from becoming a permanent part of the host genome. This halts the infection cycle at a point after entry and reverse transcription but before productive integration, complementing drug classes that act earlier or later in the cycle. This mechanism is central to modern antiretroviral therapy, where combinations of drugs acting on distinct viral targets reduce viral replication and lower the likelihood that resistant virus emerges. The approach has also been explored for long-acting prevention strategies against HIV acquisition.

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