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

Inhibiting the HIV integration process: past, present, and the future / DI SANTO, Roberto. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 57:(2014), pp. 539-566. [10.1021/jm500961p]

Inhibiting the HIV integration process: past, present, and the future

DI SANTO, Roberto
2014

Abstract

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
2014
01 Pubblicazione su rivista::01a Articolo in rivista
Inhibiting the HIV integration process: past, present, and the future / DI SANTO, Roberto. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 57:(2014), pp. 539-566. [10.1021/jm500961p]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/682454
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