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HIV-1整合酶催化前病毒DNA整合进入宿主细胞基因组的过程是病毒复制必不可少的步骤,所以抑制HIV-1整合酶活性是治疗HIV-1感染的合理策略。目前已开发了大量HIV-1整合酶抑制剂,其中一些已进入临床研究阶段,从化学结构看,绝大多数已报道的HIV-1整合酶抑制剂属于二酮酸类或其生物电子等排体。该文对近3年来二酮酸类HIV-1整合酶抑制剂的研究进展做简要综述。
HIV-1 integrase, which catalyzes the integration of proviral DNA into the genome of a host cell, is an essential step in viral replication. Therefore, inhibition of HIV-1 integrase activity is a reasonable strategy for the treatment of HIV-1 infection. A number of HIV-1 integrase inhibitors have now been developed, some of which have entered the clinical research phase. From the chemical structure, the vast majority of reported HIV-1 integrase inhibitors belong to the class of diketonic acids or their bioisers body. This review summarizes the research progress of HIV-1 integrase inhibitors in the past three years.