Inhibiting the HIV Integration Process: Past, Present, and the Future
HIV integrase (IN) catalyzes the insertion into the genome of the infected
human cell of viral DNA produced by the retrotranscription process. The discovery of
raltegravir validated the existence of the IN, which is a new target in the field of anti-HIV
drug research. The mechanism of catalysis of IN is depicted, and the characteristics of the
inhibitors of the catalytic site of this viral enzyme are reported. The role played by the
resistance is elucidated, as well as the possibility of bypassing this problem. New approaches
to block the integration process are depicted as future perspectives, such as development of
allosteric IN inhibitors, dual inhibitors targeting both IN and other enzymes, inhibitors of
enzymes that activate IN, activators of IN activity, as well as a gene therapy approach.
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