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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; in revised form: 17 June 2010 / Accepted: 19 June 2010 / Published: 25 June 2010
Abstract: 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
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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.
Métifiot M, Marchand C, Maddali K, Pommier Y. Resistance to Integrase Inhibitors. Viruses. 2010; 2(7):1347-1366.
Métifiot, Mathieu; Marchand, Christophe; Maddali, Kasthuraiah; Pommier, Yves. 2010. "Resistance to Integrase Inhibitors." Viruses 2, no. 7: 1347-1366.