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Integrase inhibitors (INIs) are a class of antiretroviral drug designed to block the action of integrase, a viral enzyme that inserts the viral genome into the DNA of the host cell. Since integration is a vital step in retroviral replication, blocking it can halt further spread of the virus.
Structural depiction of the HIV catalytic core domain based on the works of Feng, L. and Kvaratskhelia, M. from the protein database. HIV integrase is a 32kDa viral protein consisting of three domains- N-terminus, catalytic core domain, and C-terminus, which each have distinct properties and functions contributing to the efficacy of HIV ...
Raltegravir is an INSTI integrase inhibitor which inhibits both HIV-1 and HIV-2 replication. It is more potent than other previously known integrase inhibitors as well as causing less side effects. Raltegravir, Elvitegravir, Dolutegravir, Bictegravir and Cabotegravir are the only HIV-1 integrase inhibitor being used to treat HIV infections S ...
The integration of HIV DNA can occur either in dividing or resting cells, and the HIV integrase enzyme can exist in the form of a monomer, dimer, tetramer, and possibly even higher-order forms (such as octomers). Each HIV particle has an estimated 40 to 100 copies of the integrase enzyme.
Integrase inhibitors (also known as integrase nuclear strand transfer inhibitors or INSTIs) inhibit the viral enzyme integrase, which is responsible for integration of viral DNA into the DNA of the infected cell. There are several integrase inhibitors under clinical trial, [when?] and raltegravir became the first to receive FDA approval in ...
Elvitegravir (EVG) is an integrase inhibitor used to treat HIV infection. It was developed [ 1 ] by the pharmaceutical company Gilead Sciences , which licensed EVG from Japan Tobacco in March 2008. [ 2 ] [ 3 ] [ 4 ] The drug gained approval by the U.S. Food and Drug Administration on August 27, 2012, for use in adult patients starting HIV ...
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