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Viruses 2010, 2(7), 1347-1366; doi:10.3390/v2071347

Resistance to Integrase Inhibitors

Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, 37 Convent Drive, Bethesda, MD 20892, USA
Author to whom correspondence should be addressed.
Received: 27 April 2010 / Revised: 17 June 2010 / Accepted: 19 June 2010 / Published: 25 June 2010
(This article belongs to the Special Issue HIV Drug Resistance 2010)


Integrase (IN) is a clinically validated target for the treatment of human immunodeficiency virus infections and raltegravir exhibits remarkable clinical activity. The next most advanced IN inhibitor is elvitegravir. However, mutant viruses lead to treatment failure and mutations within the IN coding sequence appear to confer cross-resistance. The characterization of those mutations is critical for the development of second generation IN inhibitors to overcome resistance. This review focuses on IN resistance based on structural and biochemical data, and on the role of the IN flexible loop i.e., between residues G140-G149 in drug action and resistance.
Keywords: AIDS; HIV-1 integrase; Raltegravir; Elvitegravir; GSK-1349572; GSK-1265744; interfacial inhibitors; resistance AIDS; HIV-1 integrase; Raltegravir; Elvitegravir; GSK-1349572; GSK-1265744; interfacial inhibitors; resistance

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Métifiot, M.; Marchand, C.; Maddali, K.; Pommier, Y. Resistance to Integrase Inhibitors. Viruses 2010, 2, 1347-1366.

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