论文部分内容阅读
HIV-1整合酶是病毒复制所必需的酶[1]。在临床上,使用HIV-1整合酶(integrase,IN)抑制剂来治疗HIV感染被证明是非常有益的。目前,FDA批准上市的第一个HIV-1整合酶抑制剂raltegravir已作为一线药物用于临床[2-3]。与raltegravir作用机制相同的另外一个药物elvitegravir目前正处于III期临床试验阶段[4]。Raltegravir和elvitegravir作为第一代整合酶抑制剂,其作用机制是抑制HIV-1整合酶链转移反应[5-6],因此,它们被称为链转移反应抑制剂
HIV-1 integrase is an enzyme necessary for viral replication [1]. Clinically, the use of HIV-1 integrase (IN) inhibitors to treat HIV infection has proven to be very beneficial. At present, raltegravir, the first HIV-1 integrase inhibitor approved by the FDA, has been used as a first-line drug in clinical practice [2-3]. Elvitegravir, another drug with the same mechanism of action as raltegravir, is currently in Phase III clinical trials [4]. Raltegravir and elvitegravir, as first generation integrase inhibitors, have a mechanism of action that inhibits HIV-1 integrase chain transfer [5-6] and are therefore referred to as chain transfer reaction inhibitors