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G140S/Q148R and N155H mutations render HIV-2 Integrase resistant to Raltegravir whereas Y143C does not

机译:G140S / Q148R和N155H突变使HIV-2整合酶对Raltegravir产生抗性而Y143C不

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摘要

BackgroundHIV-2 is endemic in West Africa and has spread throughout Europe. However, the alternatives for HIV-2-infected patients are more limited than for HIV-1. Raltegravir, an integrase inhibitor, is active against wild-type HIV-2, with a susceptibility to this drug similar to that of HIV-1, and is therefore a promising option for use in the treatment of HIV-2-infected patients. Recent studies have shown that HIV-2 resistance to raltegravir involves one of three resistance mutations, N155H, Q148R/H and Y143C, previously identified as resistance determinants in the HIV-1 integrase coding sequence. The resistance of HIV-1 IN has been confirmed in vitro for mutated enzymes harboring these mutations, but no such confirmation has yet been obtained for HIV-2.
机译:背景HIV-2在西非流行,并已在整个欧洲传播。但是,HIV-2感染患者的替代方案比HIV-1受限制的方案更多。 Raltegravir是整合酶抑制剂,对野生型HIV-2具有活性,对这种药物的敏感性与HIV-1类似,因此是治疗HIV-2感染患者的有前途的选择。最近的研究表明,HIV-2对raltegravir的耐​​药性涉及三个耐药突变之一,即N155H,Q148R / H和Y143C,这些突变先前已被确定为HIV-1整合酶编码序列中的耐药决定因素。已在体外确认了具有这些突变的突变酶对HIV-1 IN的耐药性,但尚未获得对HIV-2的此类证实。

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