[Integrase inhibitor, CCR5 antagonist, fusion inhibitor].
Integrase inhibitors have a novel antiretroviral mechanism which prevents proviral DNA integration into the CD4+ cell chromosome. Promising results have been seen in clinical trials in treatment-naïve and -experienced infected individuals. CCR5 antagonists bind to CCR5, one of the second receptors of HIV-1, and inhibit HIV-1 entry into CD4+ cells. However, they cannot prevent the cell entry of HIV-1s which can use another second receptor, CXCR4. Fusion inhibitors are synthetic peptides which mimic a fragment of HIV-1 gp41. They can bind a counterpart portion of HIV-1 gp41 and prevent the fusion of viral and cellular membranes, one of the critical steps of HIV-1 entry into CD4+ cells.
Gatanaga
Hiroyuki
H
AIDS Clinical Center, International Medical Center of Japan.
D023581:HIV Fusion Inhibitors / Q000627:therapeutic use*; D015658:HIV Infections / Q000188:drug therapy*; D019428:HIV Integrase Inhibitors / Q000627:therapeutic use*; D015497:HIV-1; D006801:Humans; D019713:Receptors, CCR5 / Q000187:drug effects*
D023581:HIV Fusion Inhibitors; D019428:HIV Integrase Inhibitors; D019713:Receptors, CCR5