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An illustration of HIV entry mechanism and mechanisms of action (MOA) of two entry inhibitor, 5-Helix and C37. An HIV virion binds to a CD4+ human cell. The two bottom pictures depict two proposed models of HIV fusion with the cell. They are used in combination therapy for the treatment of HIV infection.
Drugs that disrupt fusion of virus and target cell are termed entry inhibitors or fusion inhibitors. [citation needed] HIV binds to the host CD4+ cell receptor via the viral protein gp120; gp41, a viral transmembrane protein, then undergoes a conformational change that assists in the fusion of the viral membrane to the host cell membrane ...
Entry inhibitors (or fusion inhibitors) interfere with binding, fusion and entry of HIV-1 to the host cell by blocking one of several targets. Maraviroc, enfuvirtide and Ibalizumab are available agents in this class. Maraviroc works by targeting CCR5, a co-receptor located on human helper T-cells.
Antiretroviral drugs are used to manage HIV/AIDS. Multiple antiretroviral drugs are often combined into a single pill in order to reduce pill burden. Some of these combinations are complete single-tablet regimens; the others must be combined with additional pills to make a treatment regimen.
Since CD4 receptor binding is the most obvious step in HIV infection, gp120 was among the first targets of HIV vaccine research. Efforts to develop HIV vaccines targeting gp120, however, have been hampered by the chemical and structural properties of gp120, which make it difficult for antibodies to bind to it. gp120 can also easily be shed from the surface of the virus and captured by T cells ...
Maraviroc is an entry inhibitor.Specifically, maraviroc is a negative allosteric modulator of the CCR5 receptor, which is found on the surface of certain human cells. The chemokine receptor CCR5 is an essential co-receptor for most HIV strains and necessary for the entry process of the virus into the host cell.
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