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触及HIV-1耐药性的核心:手指在聚合酶活性位点处靠近dNTP。

Touching the heart of HIV-1 drug resistance: the fingers close down on the dNTP at the polymerase active site.

作者信息

Sarafianos S G, Das K, Ding J, Boyer P L, Hughes S H, Arnold E

机构信息

Center for Advanced Biotechnology and Medicine (CABM), Rutgers University Chemistry Department, 679 Hoes Lane, Piscataway, NJ 08854-5638, USA.

出版信息

Chem Biol. 1999 May;6(5):R137-46. doi: 10.1016/s1074-5521(99)80071-4.

Abstract

Comparison of the recently solved structure of HIV-1 reverse transcriptase (RT)-DNA-dNTP ternary complex with the previously solved structure of RT-DNA binary complex suggests mechanisms by which the HIV-1 RT becomes resistant to nucleoside-analog inhibitors, drugs currently used in the treatment of AIDS.

摘要

将最近解析出的HIV-1逆转录酶(RT)-DNA-dNTP三元复合物结构与之前解析出的RT-DNA二元复合物结构进行比较,揭示了HIV-1逆转录酶对核苷类似物抑制剂产生耐药性的机制,核苷类似物抑制剂是目前用于治疗艾滋病的药物。

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