Resistance to Integrase Inhibitors

被引：83

作者：

Metifiot, Mathieu ^{[1
]}

Marchand, Christophe ^{[1
]}

Maddali, Kasthuraiah ^{[1
]}

Pommier, Yves ^{[1
]}

机构：

[1] NCI, Mol Pharmacol Lab, Ctr Canc Res, NIH, Bethesda, MD 20892 USA

来源：

VIRUSES-BASEL | 2010年 / 2卷 / 07期

关键词：

AIDS; HIV-1; integrase; Raltegravir; Elvitegravir; GSK-1349572; GSK-1265744; interfacial inhibitors; resistance; IMMUNODEFICIENCY-VIRUS TYPE-1; TREATMENT-NAIVE PATIENTS; LONG TERMINAL REPEAT; HIV-1; INTEGRASE; STRAND TRANSFER; ACTIVE-SITE; DIKETO ACID; RALTEGRAVIR RESISTANCE; CONCERTED INTEGRATION; RETROVIRAL INTEGRASE;

D O I：

10.3390/v2071347

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

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.

引用

页码：1347 / 1366

页数：20

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